RSC - RSC Med. Chem. latest articles

Targeting DNA-PK: medicinal chemistry insights into small-molecule inhibitor discovery and optimisation

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00119J, Review Article

Open Access

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Elle Watson, Jack R. R. Hutchinson, Suzannah J. Harnor, Luke Gaughan, Celine Cano
Since Wortmannin's discovery, DNA-PK inhibitors have expanded to optimised scaffolds, including chromen-4-ones (e.g. NU5455) and purinones (e.g. AZD7648). This review covers their synthesis and pharmacology from early hits to clinical candidates.
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Recent advances in piperine and its derivatives as potential anticancer agents

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00223D, Review Article

Open Access

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Qi-Hua Yu, Zhiyan Liu, Jiazheng Liu, Li-Ping Bai
This review identified piperine as a promising anticancer agent, demonstrating that the structural modification of its amide region can significantly improve the anticancer activity.
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Triarylphosphonium-conjugated Sn(IV)-porphyrins for antimicrobial photodynamic therapy: impact of substituents on lipophilicity, aggregation, and photoantibacterial activity

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00300A, Research Article

Open Access

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Gayathri MP, Nandhakumar Muruganandam, Sutharsan Govindarajan, Balaji Babu
Antimicrobial photodynamic therapy is an effective approach to counteract bacterial infections that are not possible to be treated through antibiotics.
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Novel Hydroxytyrosol Esters as Potential Anti-Amyloid and Neuroprotective Agents for Alzheimer's Disease

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00265J, Research Article

Open Access

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Ioanna Kalpaktsi, Anthi Panara, Barbara Mavroidi, Garcia Niforos, Amalia D Kalampaliki, Ioanna C Vlachogianni, Eleftheria A Georgiou, Elizabeth Fragopoulou, Anthony Tarbopoulos, AL Skaltsounis, Maria Pelecanou, K Palikaras, Evagelos Gikas, Ioannis K. Kostakis
Alzheimer's disease (AD) is associated with the aggregation of β-amyloid (Aβ) peptides and oxidative stress, two interconnected processes that contribute to neuronal dysfunction and cognitive decline. Natural polyphenols such as...
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Synthetic routes towards antiviral agents from the houttuynoid family: structure–activity relationships and antiviral efficacy against herpes simplex virus type 1

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00158K, Review Article

Adarsh Krishna T. P, Ajeesh Krishna T. P, Reshma Rajan, Laxman Kota, Prasobh K. Mohan
This review delineates the total synthesis of houttuynoids, highlighting a diverse chemical toolkit and their structure–activity relationships (SARs) and antiviral efficacy.
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Synthesis, molecular modelling and evaluation of (-)-isopulegolbased 2,4-diaminopyrimidines as promising Aurora kinase inhibitors

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00278A, Research Article

Open Access

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Tam Minh Le, Nikoletta Szemerédi, Gabriella Spengler, Minh Canh Nguyen, Huynh Nguyen Khanh Tran , Khac-Minh Thai, Zsolt Szakonyi
A library of (-)-isopulegol based 2,4-diaminopyrimidines was prepared from commercially available (-)-isopulegol. Aminodiols, derived from (-)-isopulegol according to literature methods, were added to 5-substituted 2,4dichloropyrimidines, then the resulting products were...
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Novel Urea- and Piperazine-Functionalized Alepterolic Acid Derivatives: Synthesis, Anticancer Activity, and Mechanism of Action

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00275G, Research Article

Binbin Zhang, Yating Jia, Siyu Qiu, Yanchun Sun, Lian Ma, Peixin Wang, Zixuan Tong, Fengjiao Wang, Guozheng Huang, Jianguo Cao
Lung cancer remains the leading cause of both cancer incidence and mortality worldwide, rendering it a primary focus in oncology research. This pressing global health challenge has created an urgent...
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A Bakuchiol-Linked Tetrazole Exhibits Narrow-spectrum Activity Against Streptococcus pneumoniae

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00230G, Research Article

Neha Sengar, Vidyadhar Pratap, Tuhin Sarkar, Vishnu Kriplani, Astha Gupta, Sanjay Mandal, Prasad V. Bharatam, Dulal Panda, Inder Pal Singh
Natural product-based amphiphilic phenolic terpenoid antimicrobial agents were rationally designed by integrating the meroterpenoid bakuchiol with a tetrazole moiety through a fragment-based drug design strategy. A library of 30 bakuchiol-linked...
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Identification and structure–activity relationship analysis of minimal fusion inhibitors targeting measles virus F protein

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00211K, Research Article

Open Access

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Kazuya Kobayashi, Yuki Yamaguchi, Mizuki Itahara, Kazushige Hirata, Keisuke Aoki, Naoya Iwamoto, Hironori Hayashi, Eiichi Kodama, Shinya Oishi
Optimization of a measles virus HR2-derived fusion inhibitor yielded a short peptide with potent antiviral activity and revealed key residues governing interactions with HR1.
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3-Hydroxypyrimidine-2,4-dione derivatives as monkeypox virus resolvase (Mpr) inhibitors

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00285D, Research Article

Muhammad Syafiq Bin Shahari, Jacob P Mahoney, Ziyue Wang, Anil Pant, Ajit Jagtap, Roshan Katekar, Jiashu Xie, Zhilong Yang, Zhengqiang Wang
Holliday junction resolvase plays an important role in poxvirus genome replication and viral maturation. Recently, we developed the first in vitro assay measuring the activity of orthopoxvirus resolvases, particularly monkeypox...
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Structure–activity relationships in a series of dihydrouracil–JQ1 conjugates: discovery of highly potent BRD4 degraders

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00259E, Research Article

Oleh Shyshlyk, Vladyslav Stadnichenko, Oleksandr Diachenko, Iryna Chernysh, Anna Beshtynarska, Diana Alieksieieva, Diana Khotinets, Oleksii Oleksiak, Dmytro Lesyk, Yelyzaveta Yeremenko, Angelina V. Biitseva, Petro Borysko, Volodymyr Yarmolchuk, Ganna M. Tolstanova, Oleksandr O. Grygorenko
Comprehensive SAR studies in a series of phenyl dihydrouracil (PDHU)-derived PROTACs led to the discovery of novel nanomolar BRD4 degraders.
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Bismuth drug as antibiotic adjuvant to inhibit biofilm formation via a dual mechanism

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00204H, Research Article

Jingru Li, Peng Gao, Richard Yi-Tsun Kao, Hongyan Li, Hongzhe Sun
Burkholderia cepacia (B. cepacia) exhibits intrinsic resistance to many conventional antibiotics. A key factor contributing to this resistance is its ability to form biofilms, which hinder antibiotic penetration and make...
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Solvent and Catalyst-Free Mechanochemical Synthesis of Indenyl-Derived Thiazolone imine, Thiazolidin-4-one and Thiazolidin-4-ol Hybrids: Anticancer Evaluation and Molecular Modeling Studies

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00178E, Research Article

Sanket Shantaram Mohite, Vikas Madhukar Bangade, Ambareen Shaikh, Bhushan Bhagwantrao Popatkar
To shed light on the significance of indenyl-derived thiazole derivatives in the advancement of cancer medication and to contribute to therapeutic innovation, we wish to disclose a facile, effective and...
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Synthesis-guided design and discovery of alkylated indoles with antibacterial activity against MRSA

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00221H, Research Article

Auqib Rashid, Vishwani Jamwal, Bilal A. Bhat, Kuljit Singh, Showkat Rashid
This research work presents a framework for rational design, synthesis, and detailed biological evaluation of a series of C-3 alkylated indole derivatives as potential antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA).
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Investigation of 2,3-diaryl-1,3-thiazolidin-4-ones as promising agents for reducing lipid accumulation in liver cells through AMPK activation: synthesis, in vitro, in silico and lipidomic studies

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00226A, Research Article

Arnatchai Maiuthed, Nichawadee Sandech, Meng Chieh Yang, Sucheewin Krobthong, Pattarawit Rukthong, Kittisak Sripha, Witcha Imaram, Chaiyawat Aonsri
A series of 2,3-diaryl-1,3-thiazolidin-4-ones was synthesized and identified as promising AMP-activated protein kinase (AMPK) activators with potential lipid-lowering activity.
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Light-controlled inhibition of Gram-positive bacteria by photoswitchable amphiphilic lipids (PALs)

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00096G, Research Article

Open Access

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Guilherme F. S. Fernandes, Seong-Heun Kim, Charlotte K. Hind, Jessica Furner-Pardoe, Janis Romanopulos, Christian D. Lorenz, A. James Mason, J. Mark Sutton, Daniele Castagnolo
Photoswitchable amphiphilic lipids (PALs) enable reversible light-controlled inhibition of Gram-positive bacteria. Azobenzene photoisomerization modulates membrane insertion, switching antibacterial activity on or off depending on alkyl chain length.
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Design, synthesis, and anticancer evaluation of novel pyrrole–pyrazoline/chalcone hybrids: in vitro and computational insights into EGFR inhibition

RSC Med. Chem., 2026, 17,2667-2691
DOI: 10.1039/D5MD00800J, Research Article

Open Access

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Mansour S. Alturki, Marwa F. Ahmed, Abdulaziz H. Al Khzem, Mohamed S. Gomaa, Mohammad Sarafroz, Nada Tawfeeq, Mashael M. Alharbi, Abdulaziz K. Al Mouslem, Mohammed F. Aldawsari, Wajin R. Alruwili, Shah Alam Khan, Radwan El-Haggar, Atiah H. Almalki
Design, synthesis, and biological evaluation of pyrazoline–pyrrole hybrids led to the identification of compound 6b as a potent EGFR inhibitor with significant antiproliferative activity against MCF-7 cells.
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Lead optimization of 5jc21 (CG13250), a quinolin-2(1H)-one-based inhibitor of the BRD4 member of the bromodomain and extraterminal (BET) family of proteins

RSC Med. Chem., 2026, 17,2630-2643
DOI: 10.1039/D5MD01082A, Research Article

Jay Chauhan, Sarah Pogash, Makoto Yoshioka, Mithun Raje, Daniel Van Eker, Jeffrey W. Strovel, Steven Fletcher
4,6-Disubstituted quinolinones are potent BRD4 inhibitors.
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Pyrazole–triazole hybrids as kinase-triad inhibitors: a triple-target strategy for synergistic anticancer therapy

RSC Med. Chem., 2026, 17,2360-2386
DOI: 10.1039/D6MD00022C, Research Article

Mahmoud S. Elkotamy, Mohamed K. Elgohary, Mariam M. Fakhry, Mohamed E. Albakri, Abdelrahman A. Naglah, Abdulrahman A. Almehizia, Ahmed M. Naglah, Mohamed Fares, Haytham O. Tawfik, Wagdy M. Eldehna, Hatem A. Abdel-Aziz
The ongoing issue of drug resistance and the lack of specificity in existing cancer treatments highlight the necessity for innovative multi-target agents.
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Diverse ring architectures of cyclic peptidomimetics targeting melanocortin receptors

RSC Med. Chem., 2026, 17,2326-2346
DOI: 10.1039/D6MD00115G, Review Article

Wenxiao K. Yue, Nicholas Barlow, Philip E. Thompson
A review of the many types of macrocyclic melanocortin peptides. We show that there is a historical gap in the evaluation of these architectures in terms of their influence upon potency, selectivity and pharmacokinetics.
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Structure-based design of potent pyrazolo[1,5-a]pyrimidine CDK4/6 inhibitors: biological evaluation and computational validation

RSC Med. Chem., 2026, 17,2566-2587
DOI: 10.1039/D5MD01147G, Research Article

Faizah A. Binjubair, Mahmoud S. Elkotamy, Amr A. Mattar, Bjad K. Almutairy, Sara T. Al-Rashood, Mohamed M. Eldesouki, Jalloul Bouajila, Hatem A. Abdel-Aziz, Mariam M. Fakhry
Structure-based design yielded potent CDK4/6 inhibitor 19i, inducing G1 cell-cycle arrest and apoptosis in HCT-116 cells, supported by enzymatic inhibition and molecular docking/dynamics studies.
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Discovery of novel BCAT2 inhibitors: design, synthesis, in vitro evaluation, and molecular modeling studies

RSC Med. Chem., 2026, 17,2549-2565
DOI: 10.1039/D6MD00019C, Research Article

Dong Xu, Wenxiu Weng, Huining Cao, Chao Zhang, Yudi Zhang, Yan Li, Junhai Xiao, Hua Xie, Jialin Guo, Guoliang Chen
Structure-based rational design yielded novel potent BCAT2 inhibitors C10 (IC₅₀ = 44 nM) and C11 (IC₅₀ = 54 nM), which exhibit 8–10-fold selectivity over BCAT1 and form stable, key interactions within the BCAT2 active pocket.
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Decoding the association of polycystic ovary syndrome with metabolic-associated fatty liver: insights into CK18 and LC3II/ATG7/P62 autophagy axis and adjunct therapeutics of metformin and levothyroxine

RSC Med. Chem., 2026, 17,2508-2537
DOI: 10.1039/D5MD00819K, Research Article

Sameeah Mejbel Hamad Algenabi, Anwar Nather Seiwan, Maha Hussein Hashem Sabra, Doaa I. Mohamed, Lobna Fouad Abd ElAziz Bassyouni, Dalia Alaa El-Din Aly El-Waseef, Samar F. Ezzat, Omnyah A. El-Kharashi, Hanaa F. Abd El-Kareem, Hyfa A. Alzahrani, Fawzyah Obeedallah Albaldi, Ahmed Shokry Elharoun, Mansour Altayyar, Amal Fahmy Dawood, Hebatallah H. Abo Nahas, Ahmed Abdel-Salam M. Elmelegy
Metformin–levothyroxine synergistically treats PCOS-MAFLD. Reduced body/liver weight, ALT/AST/TSH/lipids, testosterone/LH/HOMA-IR. Increased estradiol. Suppressed autophagy (LC3II/ATG7/p62/CK18) and improved histology.
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Phenoxyacetic acid scaffold as a platform for dual anticonvulsant and anti-inflammatory drug design

RSC Med. Chem., 2026, 17,2486-2507
DOI: 10.1039/D6MD00097E, Research Article

Mohamed K. Elgohary, Mahmoud Abdelrahman Alkabbani, Aya Mohamed Ahmed Ibrahim, Ahmed Elsonbaty, Mayada H. Mohamed, Abdulrahman A. Almehizia, Ahmed M. Naglah, Mohamed Fares, Hatem A. Abdel-Aziz
Neuroinflammation is increasingly recognized as a critical contributor to epileptogenesis and antiepileptic drug resistance, emphasizing the need for multi-target therapeutic strategies.
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Beyond acrylamide: a structure-guided investigation of covalent warheads in the development of CDK7 inhibitors

RSC Med. Chem., 2026, 17,2692-2713
DOI: 10.1039/D6MD00088F, Research Article

Yu Cao, Yiqing Huang, Yunlong Pan, Jialuo Mao, Lixin Gao, Jiankang Zhang, Huajian Zhu, Shourong Liu, Rangxiao Zhuang, Yang Liu, Yubo Zhou, Jiaan Shao
To achieve covalent CDK7 inhibitors with superior antiproliferative activity and enhanced selectivity, we designed and synthesized a series of covalent CDK7 inhibitors bearing diverse warheads based on the THZ1 scaffold.
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Recent advances towards BACE1 drug discovery and therapeutics design

RSC Med. Chem., 2026, 17,2306-2325
DOI: 10.1039/D5MD01095K, Review Article

Open Access

This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.

Saim Imran, Meera Patel, Meissam Noroozifar, Kagan Kerman
We explored the latest developments in modulators, antibody therapy, and gene therapy targeting β-site amyloid precursor protein cleaving enzyme 1 (BACE1) to combat Alzheimer's disease.
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Bicyclic monoterpenoid-based orthopoxvirus inhibitors: design, synthesis, and biological assessment of a novel amide series

RSC Med. Chem., 2026, 17,2605-2629
DOI: 10.1039/D6MD00217J, Research Article

Serafim A. Tishchenko, Anastasiya S. Sokolova, Valeriya V. Samsonova, Julia G. Pushkareva, Nikolay I. Bormotov, Ivan A. Moskalev, Daria. E. Solomina, Artem D. Rogachev, Alina V. Fatyanova, Sophia S. Borisevich, Olga I. Yarovaya, Olga A. Serova, Alena S. Ovchinnikova, Alexander A. Sergeev, Larisa N. Shishkina, Artemiy A. Sergeev, Alexander P. Agafonov, Nariman F. Salakhutdinov
This study reports the design, synthesis, and comprehensive biological evaluation of a new class of orthopoxvirus inhibitors utilizing natural bicyclic monoterpenoid scaffolds as strategic replacements for synthetic polycyclic cores.
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Quinoline/thiazole compounds as selective acetylcholinesterase inhibitors: synthesis and biological assessment

RSC Med. Chem., 2026, 17,2404-2412
DOI: 10.1039/D6MD00165C, Research Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Berkant Kurban, Derya Osmaniye, Serkan Levent, Yusuf Özkay, Zafer Asım Kaplancıklı
Acetylcholine (ACh), acetylcholinesterase enzyme (AChE), and AChE inhibition are of great importance in the treatment of neurodegenerative diseases.
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Redefining the role of the thiol-based agent N-acetylcysteine in human health and disease and elucidating potential advantages of its amide derivative

RSC Med. Chem., 2026, 17,2183-2196
DOI: 10.1039/D5MD01173F, Review Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Hui-Qi Qu, Charlly Kao, Hakon Hakonarson
N-Acetylcysteine amide (NACA) reduces polarity and ionization relative to NAC, improving membrane permeability and intracellular exposure while preserving thiol-mediated redox activity and glutathione support.
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Design, synthesis, and biological evaluation of quinoline derivatives as dual-target inhibitors of chitin synthase and glucosamine-6-phosphate synthase

RSC Med. Chem., 2026, 17,2588-2604
DOI: 10.1039/D5MD01001B, Research Article

Nan Wang, Lige Liu, Tao Liu, Hong Luo, Yan Long, Xinlong Yang, Youli Zhang, Qinggang Ji
This study designed and synthesized a series of glycine methyl ester quinoline derivatives as dual-target inhibitors of CHS and GlmS, followed by biological evaluation including enzyme inhibition assays and in vitro antifungal activity testing.
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Novel zerumbone-amide-triazole hybrids as potential NF-κB pathway inhibitors: design, synthesis, cytotoxicity evaluation, computational studies, and mechanistic insights

RSC Med. Chem., 2026, 17,2387-2403
DOI: 10.1039/D6MD00148C, Research Article

Pham The Chinh, Pham Thi Tham, Vu Thi Lien, Dao Thi Nhung, Le Thi Thuy Loan, Khieu Thi Tam, Vu Tuan Kien, Cao Thanh Hai, Phan Thanh Phuong, Truong Thi Thao, Vuong Truong Xuan, Le Thi Lien
A series of fifteen novel zerumbone-amide-triazole hybrids 12a–i and 15a–f were successfully designed and synthesized from azazerumbone II (2) via click reaction.
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D-Galactose-conjugated pyrimidine thioureas as potent antimicrobial agents: rapid green synthesis, structure–activity relationships and molecular modelling

RSC Med. Chem., 2026, 17,2644-2666
DOI: 10.1039/D6MD00026F, Research Article

Nguyen Dinh Thanh, Vu Ngoc Toan, Ngo Hong Anh Thu, Nguyen Minh Tri, Duong Ngoc Toan, Hoang Thi Kim Van
D-Galactose–pyrimidine thioureas were synthesized via a recyclable ionic liquid–microwave method in high yields. Several derivatives showed broad-spectrum antimicrobial activity, and docking with ADMET predicted strong binding and drug-like properties.
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Design, synthesis and biological evaluation of benzoyl hydrazone derivatives as anticancer agents inducing ROS-associated mitochondrial apoptosis

RSC Med. Chem., 2026, 17,2413-2427
DOI: 10.1039/D5MD01046B, Research Article

Rongbin Wei, Xin Wang, Yamin Ding, Suting Zhu, Richmond Kwame Frimpong Asiedu, Muzi Li, Haitao Qian, Yifei Gu, Bailing Jiang
Compound Q-11 shows potent nanomolar antiproliferative activity in gastric cancer cells and induces ROS accumulation, mitochondrial dysfunction and cytoskeletal disruption.
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Beyond infection control: exploring the therapeutic potential of antimicrobials in oncology and their synthetic perspectives

RSC Med. Chem., 2026, 17,2270-2305
DOI: 10.1039/D6MD00084C, Review Article

Rahul Kumar, Mohd Yeshab Ansari
This review explores the burgeoning potential of antimicrobial agents in oncology, highlighting their roles in reducing infection-related mortality, enhancing therapeutic effectiveness, and improving the overall quality of life in cancer patients.
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Rational discovery of novel phenylindole-bisamide derivatives as potent P-glycoprotein inhibitors for cancer multidrug resistance

RSC Med. Chem., 2026, 17,2455-2472
DOI: 10.1039/D6MD00030D, Research Article

Zhikun Yang, Jiajia Han, Yanhong Yang, Xue Yang, Yijing Du, Zimeng Huang, Leyi Ying, Xin Yu, Yi Hua, Qihao Wu, Xiaozhou Mou, Hong Wang
P-gp-mediated MDR hinders cancer chemotherapy. Our phenylindole-bisamide l1 shows potent MDR reversal, low cytotoxicity, broad chemosensitization. It inhibits P-gp efflux and suppresses 3D tumor growth with doxorubicin, a promising P-gp inhibitor.
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Exploration of a benzothiophene scaffold for use as adjuvants with β-lactam antibiotics against methicillin-resistant Staphylococcus aureus

RSC Med. Chem., 2026, 17,2444-2454
DOI: 10.1039/D5MD01109D, Research Article

Open Access

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Monica A. Stefaniak, Vijay S. Gondil, Emily P. Gillis, Ansley M. Nemeth, Allen G. Oliver, Roberta J. Melander, Paul M. Dunman, Christian Melander
Rising antibiotic resistance coupled with diminishing investment in antibiotic development has led to limited treatment options for multi drug-resistant bacterial infections.
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Pharmacological landscape of carbolines: a holistic view

RSC Med. Chem., 2026, 17,2197-2269
DOI: 10.1039/D6MD00057F, Review Article

Yao Zhang, Fule Wu, Muneeb Ur Rehman, Sihui Long
This review comprehensively explores the design, synthesis, and pharmacological activities of carboline isomers reported between 2000 and 2025, with a particular emphasis on their key bioactivities, encompassing anticancer, neuroprotective, antiparasitic, and antimicrobial.
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Hypoxia-triggered dichloroacetate delivery with effective reversal of cancer cell reprogramming

RSC Med. Chem., 2026, 17,2538-2548
DOI: 10.1039/D5MD00911A, Research Article

Rensong Sun, Lei Wang, Ziang Liu, Hao Wu, Wanwan Wang, Yang Wang, Xiao Qian, Engin U. Akkaya
The 3-methyl-2-nitroimidazole dichloroacetate derivative studied in this work is a prodrug version of dichloroacetate, and it is active at lower concentrations in hypoxic cell cultures and suppresses tumor progression significantly in vivo.
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Triclosan–isatin hybrids as potent anti-proliferative agents inducing S-phase arrest via DNA gyrase inhibition in triple-negative breast cancer

RSC Med. Chem., 2026, 17,2473-2485
DOI: 10.1039/D6MD00013D, Research Article

Shekhar, Asif Raza, Sukhmanpreet kaur, Amit Anand, Arun K. Sharma, Vipan Kumar
A series of 1H-1,2,3-triazole-tethered TCS–isatin hybrid compounds were synthesized and evaluated for their antiproliferative activity against triple-negative breast cancer (TNBC).
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Introducing CLipPA lipid chemodiversity to enzymatically truncated polymyxin B: a soft drug strategy to combat Gram-negative pathogens

RSC Med. Chem., 2026, 17,2347-2359
DOI: 10.1039/D5MD01141H, Research Article

Tae-Ung Na, Yann O. Hermant, Andrew Siow, Jeremy G. Owen, Susanna T. S. Chan, Gavin F. Painter, Cameron C. Hanna, Zillah Daysh, Beatrix L. Goggin, Jane R. Allison, Veronika Sander, Alan J. Davidson, Georgia Campbell, Scott A. Ferguson, Gregory M. Cook, Paul W. R. Harris, Margaret A. Brimble, Alan J. Cameron
An efficient strategy to tune the activity and stability of semi-synthetic lipopeptides is presented, enabled by the CLipPA thiol–ene reaction.
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From bolinaquinone, a marine hydroxyquinone sesquiterpene, to naphthoquinones with clathrin inhibitory effects

RSC Med. Chem., 2026, 17,2428-2443
DOI: 10.1039/D5MD00900F, Research Article

Nicholas S. O'Brien, Azadeh Ghods, Jing Xue, Mary J. Garson, Ken W. L. Yong, Jennette A. Sakoff, Jayne Glibert, Megan Chircop, Uwe Fink, Volker Haucke, Phillip J. Robinson, Adam McCluskey
Bolinaquinone (1) is cited as a clathrin inhibitor; applying a DFT approach, naphthoquinones with similar electronic properties were designed and shown to be potent inhibitors of the clathrin N-terminal domain–amphiphysin interaction, e.g.23.
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Design, synthesis, in-silico and in-vitro evaluation of Novel Complex Naphthalimide-Ciprofloxacin Hybrids as next-generation antimicrobial agents

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00193A, Research Article

Arunava Manna, Dharmendra singh, Ankita Singh, Harikesh Kumar Gupta, Sajida Banoo, Sumit Maurya, Vishwakarma Krishna Ramesh, Khushbu Khushbu, Ambrish Kumar, Jyoti Kumari, Avisek Mahapa, Shruti Trivedi, Rajnish Kumar, Shashikala Verma
A series of ciprofloxacin-naphthalimide hybrid drugs as novel antibacterial agents were synthesized and screened for their antibacterial property against gram-positive and gram-negative bacterial strains, including drug-resistant clinical isolates. Minimum inhibitory...
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Twenty Years of Quinazolines as Tubulin Polymerisation Inhibitors

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D5MD01035G, Review Article

Nicholas O'Brien, Adam McCluskey
Over the past two decades, the quinazoline scaffold has emerged as a privileged framework in the development of small molecule tubulin polymerisation inhibitors. Here we map the chemical space of...
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Computational approaches for flavivirus drug discovery: targeting structural and non-structural proteins

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00108D, Review Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Mayasah Al-Nema, Mariana Manzano Rendeiro, Daniella Liao, Marwan Abdelmahmoud Abdelkarim Maki
Schematic overview of an integrative computational pipeline for drug discovery.
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Regioselective triclocarban-catalyzed synthesis of spiroindeno- and spirooxindolo-pyrrolizidines with apoptosis induction in MCF-7 cells

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00132G, Research Article

V. Rukyanaik, Samata Pradhan, Chandraiah Godugu, Srinu Tothadi, Kadiyam Rama Krishna, Ravinder Pawar, Srinivas Basavoju
The design of new molecules from known structural motifs via [3 + 2] cycloaddition is a widely used strategy in modern drug discovery.
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Design, synthesis, and biological evaluation of novel SN38–sulfonamide conjugates as Topo I/CA IX dual inhibitors inducing ferroptosis in colorectal cancer

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00290K, Research Article

Xinyu Zhao, Anna Ye, Yujie Wang, Yeying Qiu, Shiyan Liu, Liyu Wei, Feng Qin, Ye Zhang, Rizhen Huang
A series of novel SN38–sulfonamide conjugates were designed and synthesized as carbonic anhydrase IX (CA IX) and topoisomerase I (Topo I) dual inhibitors for colorectal cancer therapy.
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From scaffold to selectivity-medicinal insights of PRMT1 and PRMT4 inhibitors for epigenetic cancer therapy

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00286B, Review Article

Kanchan Pal, Shivani Kasana, Balak Das Kurmi, Preeti Patel
SAR and docking analysis indicate important structural determinants and binding interactions that promote Selective and Dual PRMT1 and PRMT4 inhibition, making them potentially useful as epigenetic targets in various cancer treatments.
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Structure-activity relationship for calanthoside, a potential hairgrowth stimulant with an indole 2-S-,3-O-bis-glucoside structure. Part 1: Role of two glucoside moieties in promoting HFDPC proliferation

RSC Med. Chem., 2026, Accepted Manuscript
DOI: 10.1039/D6MD00273K, Research Article

Open Access

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.

Riko Suzuki, Katsuki Takashima, Yoshiaki Mannse, Haruto Nishikawa, Mina Ashidate, Shinsuke Marumoto, Fumihiro Ishikawa, Toshio Morikawa, Genzoh Tanabe
The development of new and effective drugs for treating androgenetic alopecia (AGA) remains challenging. Minoxidil and finasteride, two drugs currently used to treat AGA, were originally developed for treating hypertension...
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Addressing multidrug-resistant bacterial infections with iridium-based theragnostic agents

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00120C, Research Article

Rama Karn, Mahesmita Sahoo, Sayantani Biswas, Suravi Chauhan, Ajay Kumar Nag, Soham Basu, Srikanta Patra, Debasis Manna
An amphiphilic iridium(III) complex self-assembles into cationic nanoaggregates that disrupt bacterial membranes and facilitate selective fluorescence imaging, providing a promising theragnostic platform to combat antimicrobial resistance.
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Histone deacetylase-based dual inhibitors: research progress focusing on non-small cell lung cancer therapy

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D6MD00063K, Review Article

Zihao Liu, Zhiguang Yang
HDAC dual-target inhibitors integrate epigenetic modulation with complementary pathway blockade, achieving synergistic antitumor effects in NSCLC by enhancing efficacy, overcoming drug resistance, and reducing toxicity.
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Sulfone and sulfoxide-containing pharmaceuticals: targets, pharmacological properties and SAR studies

RSC Med. Chem., 2026, Advance Article
DOI: 10.1039/D5MD01089F, Review Article

Yiran Zhou, Jinqu Li, Yiou Mei, Yuzhu Chen, Fengxia Sun, Yunfei Du
Numerous sulfone/sulfoxide-containing drugs are FDA-approved for clinical use, and these moieties remain of great interest. This review overviews these agents, focusing on their targets, activities, and SAR studies.
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