RSC Advances
Drug discovery articles published in the last
6 months
Aminoguanidine-based bioactive proligand as AIEE probe for anticancer and anticovid studies
An anticancer proligand, with AIEE features, demonstrates exceptional binding efficiencies with DNA and SARS-CoV-2 and offers as a promising bioprobe.
RSC Adv., 2024,14, 13654-13668
https://doi.org/10.1039/D4RA00554F
Nanoparticles incorporated hydrogels for delivery of antimicrobial agents: developments and trends
Nanoparticle-hydrogel systems are versatile biomaterials that possess numerous advantages for biomedical applications. This review focuses on the application of the nanoparticle-hydrogels system for the delivery of antimicrobial agents.
RSC Adv., 2024,14, 13535-13564
https://doi.org/10.1039/D4RA00631C
Advancements in application of chitosan and cyclodextrins in biomedicine and pharmaceutics: recent progress and future trends
The global community is faced with numerous health concerns such as cancer, cardiovascular and neurological diseases, diabetes, joint pain, osteoporosis, among others.
RSC Adv., 2024,14, 13384-13412
https://doi.org/10.1039/D4RA01370K
Inhibition of survivin by 2′-O-methyl phosphorothioate-modified steric-blocking antisense oligonucleotides
We have designed and screened seven fully 2′-O-methyl phosphorothioate-modified steric-blocking ASOs for specific inhibition of BIRC5 expression. As a result, ASO-7 was identified as the lead sequence.
RSC Adv., 2024,14, 13336-13341
https://doi.org/10.1039/D4RA01925C
Synthesis of novel phthalazine-based derivatives with potent cytotoxicity against HCT-116 cells through apoptosis and VEGFR2 inhibition
A novel phthalazine derivative exhibited potent cytotoxicity against HCT-116 cells as VEGFR2 inhibitor and apoptosis cell death.
RSC Adv., 2024,14, 13027-13043
https://doi.org/10.1039/D4RA02103G
Mono and di ortho-C–H acetoxylation of 2-aryloxyquinoline-3-carbaldehydes
A novel protocol for introducing an acetoxy functional group selectively on the ortho aryl sp2 carbon of 2-aryloxyquinoline-3-carbaldehydes in good yields with good functional group tolerance using a palladium catalyst was developed for the first time.
RSC Adv., 2024,14, 13306-13310
https://doi.org/10.1039/D4RA01289E
Quinazolines and thiazolidine-2,4-dions as SARS-CoV-2 inhibitors: repurposing, in silico molecular docking and dynamics simulation
This paper presents an extensive analysis of COVID-19 with a specific focus on VEGFR-2 inhibitors as potential treatments.
RSC Adv., 2024,14, 13237-13250
https://doi.org/10.1039/D4RA02029D
Exploring the synthetic potential of epoxide ring opening reactions toward the synthesis of alkaloids and terpenoids: a review
Epoxides are oxygen containing three-membered heterocycles which can undergo ring opening reactions. These reactions have been significantly employed in the synthesis of alkaloids and terpenoids-based natural products.
RSC Adv., 2024,14, 13100-13128
https://doi.org/10.1039/D4RA01834F
The conjugates of 5′-deoxy-5-fluorocytidine and hydroxycinnamic acids – synthesis, anti-pancreatic cancer activity and molecular docking studies
New conjugates 1–6 containing 5-dFCR and selected hydroxycinnamic acids were synthesized and tested in vitro against pancreatic cancer (PDAC) lines. The ADME properties and molecular docking to CES2 or human albumin were discussed.
RSC Adv., 2024,14, 13129-13141
https://doi.org/10.1039/D4RA01683A
ProteoMutaMetrics: machine learning approaches for solute carrier family 6 mutation pathogenicity prediction
Predict SLC6 mutation clinical pathogenicity by calculating the amino acid descriptors in different ranges with rationalization analysis of the prediction.
RSC Adv., 2024,14, 13083-13094
https://doi.org/10.1039/D4RA00748D
Construction of glutathione-responsive paclitaxel prodrug nanoparticles for image-guided targeted delivery and breast cancer therapy
HA-coated redox sensitive visualized nano-prodrug HA/TPE-CS-SS-PTX were exploited in order to highly efficient treatment of cancer and real-time monitoring of drug localization.
RSC Adv., 2024,14, 12796-12806
https://doi.org/10.1039/D4RA00610K
Current status of controlled onco-therapies based on metal organic frameworks
Most MOFs for controllable cancer treatment act as drug delivery vehicle and/or anti-cancer agent. Molecules with anti-cancer roles such as chemotherapies, gases, peptides or nucleic acids can be loaded into MOFs that decompose in cancer cells or in the TME to release its cargoes.
RSC Adv., 2024,14, 12817-12828
https://doi.org/10.1039/D4RA00375F
Design, synthesis and antiproliferative evaluation of tetrahydro-β-carboline histone deacetylase inhibitors bearing an aliphatic chain linker
The use of histone deacetylase inhibitors (HDACis) is an effective approach for cancer treatment.
RSC Adv., 2024,14, 12762-12771
https://doi.org/10.1039/D4RA01672F
In vitro and in silico docking and molecular dynamic of antimicrobial activities, alpha-glucosidase, and anti-inflammatory activity of compounds from the aerial parts of Mussaenda saigonensis
Twelve compounds were isolated from Mussaenda saigonensis aerial parts through phytochemical analysis and the genus Mussaenda is the first place where the compounds 4–6 and 11–12 have been found.
RSC Adv., 2024,14, 12081-12095
https://doi.org/10.1039/D4RA01865F
Label-free detection of Aβ-42: a liquid crystal droplet approach for Alzheimer's disease diagnosis
This study introduces a biosensor based on liquid crystals (LC) designed to detect the Aβ-42 biomarker, commonly associated with Alzheimer's disease.
RSC Adv., 2024,14, 12107-12118
https://doi.org/10.1039/D4RA00615A
Skin emitted volatiles analysis for noninvasive diagnosis: the current advances in sample preparation techniques for biomedical application
Analytical technique for monitoring skin-emitted metabolites to diagnose diseases.
RSC Adv., 2024,14, 12009-12020
https://doi.org/10.1039/D4RA01579G
Activity against Mycobacterium tuberculosis of a new class of spirooxindolopyrrolidine embedded chromanone hybrid heterocycles
Spirooxindolopyrrolidines were synthesized in quantitative yield through cycloaddition strategy. Compounds exhibited significant anti-tubercular activity and molecular docking studies of the compound is well correlates with in vitro findings.
RSC Adv., 2024,14, 11604-11613
https://doi.org/10.1039/D4RA01501K
pH-responsive niosome-based nanocarriers of antineoplastic agents
Modified niosomes possessing pH-responsive properties were developed for delivery of antineoplastic agents.
RSC Adv., 2024,14, 11124-11140
https://doi.org/10.1039/D4RA01334D
Immunomodulatory zymosan/ι-carrageenan/ agarose hydrogel for targeting M2 to M1 macrophages (antitumoral)
Zymosan/ι-carrageenan/agarose hydrogel (antitumor) as tumor targeting (M2 to M1 genes) and wound healing material.
RSC Adv., 2024,14, 11694-11705
https://doi.org/10.1039/D3RA06978H
Design, synthesis and cytotoxic activity of molecular hybrids based on quinolin-8-yloxy and cinnamide hybrids and their apoptosis inducing property
A sequence of novel quinoline-8-yloxy and cinnamide hybrids has been synthesized and evaluated for in vitro cytotoxicity against HepG2 liver cancer cells.
RSC Adv., 2024,14, 11443-11451
https://doi.org/10.1039/D4RA01911C
Anticancer potential of novel symmetrical and asymmetrical dihydropyridines against breast cancer via EGFR inhibition: molecular design, synthesis, analysis and screening
Our study introduces novel symmetrical and asymmetrical dihydropyridines as breast cancer inhibitors, showing cytotoxicity against MCF-7 cells and EGFR kinase inhibition. Molecular docking and dynamics validate superior binding to Lapatinib.
RSC Adv., 2024,14, 11368-11387
https://doi.org/10.1039/D4RA01424C
Synthesis of novel bioactive pyrido[2,3-d]pyrimidine derivatives with potent cytotoxicity through apoptosis as PIM-1 kinase inhibitors
Novel bioactive pyrido[2,3-d]pyrimidine derivatives with potent apoptotic inducers as PIM-1 kinase inhibitors.
RSC Adv., 2024,14, 11098-11111
https://doi.org/10.1039/D4RA00902A
Review on anti-alzheimer drug development: approaches, challenges and perspectives
Alzheimer has many crucial factors that should be considered in order to get better results from clinical trials. Benzimidazole and its isosteres represent significant scaffolds for designing potential multi-target anti-alzheimer molecules.
RSC Adv., 2024,14, 11057-11088
https://doi.org/10.1039/D3RA08333K
Synthesis of hydrazone-based polyhydroquinoline derivatives – antibacterial activities, α-glucosidase inhibitory capability, and DFT study
Hydrazone-based polyhydroquinoline derivatives are synthesized and characterized through modern spectroscopic techniques, compounds showed high potency and inhibitory activity. Molecular docking and DFT analyses were performed to predict structure activity relationship, electronic properties etc.
RSC Adv., 2024,14, 10978-10994
https://doi.org/10.1039/D4RA00045E
Computational studies and synthesis of 131iodine-labeled nocardiotide A analogs as a peptide-based theragnostic radiopharmaceutical ligand for cancer targeting SSTR2
The cWIWLYA peptide shows high labeling efficiency with I-131 (>90%). Its 131I2-complex has high stability at room temperature as well as in plasma.
RSC Adv., 2024,14, 10962-10968
https://doi.org/10.1039/D4RA00684D
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