RSC Advances  

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Drug discovery articles published in the last 6 months

189 items - Showing page 1 of 8
Open Access Paper

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.

Graphical abstract: Aminoguanidine-based bioactive proligand as AIEE probe for anticancer and anticovid studies
Open Access Review Article

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.

Graphical abstract: Nanoparticles incorporated hydrogels for delivery of antimicrobial agents: developments and trends
Open Access Review Article

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.

Graphical abstract: Advancements in application of chitosan and cyclodextrins in biomedicine and pharmaceutics: recent progress and future trends
Open Access Paper

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.

Graphical abstract: Inhibition of survivin by 2′-O-methyl phosphorothioate-modified steric-blocking antisense oligonucleotides
Open Access Paper

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.

Graphical abstract: Synthesis of novel phthalazine-based derivatives with potent cytotoxicity against HCT-116 cells through apoptosis and VEGFR2 inhibition
Open Access Paper

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.

Graphical abstract: Mono and di ortho-C–H acetoxylation of 2-aryloxyquinoline-3-carbaldehydes
Open Access Paper

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.

Graphical abstract: Quinazolines and thiazolidine-2,4-dions as SARS-CoV-2 inhibitors: repurposing, in silico molecular docking and dynamics simulation
Open Access Review Article

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.

Graphical abstract: Exploring the synthetic potential of epoxide ring opening reactions toward the synthesis of alkaloids and terpenoids: a review
Open Access Paper

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.

Graphical abstract: The conjugates of 5′-deoxy-5-fluorocytidine and hydroxycinnamic acids – synthesis, anti-pancreatic cancer activity and molecular docking studies
Open Access Paper

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.

Graphical abstract: ProteoMutaMetrics: machine learning approaches for solute carrier family 6 mutation pathogenicity prediction
Open Access Paper

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.

Graphical abstract: Construction of glutathione-responsive paclitaxel prodrug nanoparticles for image-guided targeted delivery and breast cancer therapy
Open Access Review Article

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.

Graphical abstract: Current status of controlled onco-therapies based on metal organic frameworks
Open Access Paper

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.

Graphical abstract: Design, synthesis and antiproliferative evaluation of tetrahydro-β-carboline histone deacetylase inhibitors bearing an aliphatic chain linker
Open Access Paper

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.

Graphical abstract: 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
Open Access Paper

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.

Graphical abstract: Label-free detection of Aβ-42: a liquid crystal droplet approach for Alzheimer's disease diagnosis
Open Access Review Article

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.

Graphical abstract: Skin emitted volatiles analysis for noninvasive diagnosis: the current advances in sample preparation techniques for biomedical application
Open Access Paper

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.

Graphical abstract: Activity against Mycobacterium tuberculosis of a new class of spirooxindolopyrrolidine embedded chromanone hybrid heterocycles
Open Access Paper

pH-responsive niosome-based nanocarriers of antineoplastic agents

Modified niosomes possessing pH-responsive properties were developed for delivery of antineoplastic agents.

Graphical abstract: pH-responsive niosome-based nanocarriers of antineoplastic agents
Open Access Paper

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.

Graphical abstract: Immunomodulatory zymosan/ι-carrageenan/ agarose hydrogel for targeting M2 to M1 macrophages (antitumoral)
Open Access Paper

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.

Graphical abstract: Design, synthesis and cytotoxic activity of molecular hybrids based on quinolin-8-yloxy and cinnamide hybrids and their apoptosis inducing property
Open Access Paper

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.

Graphical abstract: Anticancer potential of novel symmetrical and asymmetrical dihydropyridines against breast cancer via EGFR inhibition: molecular design, synthesis, analysis and screening
Open Access Paper

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.

Graphical abstract: Synthesis of novel bioactive pyrido[2,3-d]pyrimidine derivatives with potent cytotoxicity through apoptosis as PIM-1 kinase inhibitors
Open Access Review Article

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.

Graphical abstract: Review on anti-alzheimer drug development: approaches, challenges and perspectives
Open Access Paper

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.

Graphical abstract: Synthesis of hydrazone-based polyhydroquinoline derivatives – antibacterial activities, α-glucosidase inhibitory capability, and DFT study
Open Access Paper

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.

Graphical abstract: Computational studies and synthesis of 131iodine-labeled nocardiotide A analogs as a peptide-based theragnostic radiopharmaceutical ligand for cancer targeting SSTR2
189 items - Showing page 1 of 8

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