ArticleRSC advances2021
Design, synthesis and mechanistic study of new benzenesulfonamide derivatives as anticancer and antimicrobial agents
Article in RSC advances, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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The trial behind it
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Who cites it
27 citing papers in PubMed, 75 citations in OpenAlex.
- Probing novel azole-sulfonamide urea/thiourea conjugates as multitarget inhibitors of AChE and hCAs (I and II): synthesis, in vitro, and in silico studies.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Article
- Dual-target carbonic anhydrase inhibitors in cancer therapy: progress, challenges, and opportunities.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- Characterization of beddomeilactone amide as bacterial DNA gyrase inhibitor: in vitro evaluation and computational insights.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Article
- Integral Lipophilicity Studies with in Silico ADMET Parameter Analysis of Novel Pseudothiohydantoin Derivatives.International journal of molecular sciences · 2026Article
- An overview on pharmaceutical applications of phosphodiesterase enzyme 5 (PDE5) inhibitors.Molecular diversity · 2025Review
- Synthesis, antiproliferative activity targeting lung cancer and in silico studies of hydroxypiperidine substituted thiosemicarbazones.Scientific reports · 2025Article
- Review
- Novel di-aryl chalcone derived pyrazole linked to methane sulfonyl pharmacophore as potent selective COX-2 inhibitors; design, synthesis, molecular modeling,Future medicinal chemistry · 2025Article
- Discovery of novel 4-trifluoromethyl-2-anilinoquinoline derivatives as potential anti-cancer agents targeting SGK1.Molecular diversity · 2025Article
- Design, synthesis and biological evaluation of thienopyridine derivatives as c-Met kinase inhibitors.Molecular diversity · 2025Article
- Discovery and optimization of 4-(imidazo[1,2-a]pyrimidin-3-yl)thiazol-2-amine derivatives as novel phosphodiesterase 4 inhibitors.Molecular diversity · 2025Article
- Design, Synthesis, and Antioxidant and Anti-Tyrosinase Activities of (Molecules (Basel, Switzerland) · 2025Article
- Exploring heterocyclic scaffolds in carbonic anhydrase inhibition: a decade of structural and therapeutic insights.RSC advances · 2024Review
- New antiproliferative 3-substituted oxindoles inhibiting EGFR/VEGFR-2 and tubulin polymerization.Molecular diversity · 2024Article
- Recent development of azole-sulfonamide hybrids with the anticancer potential.Future medicinal chemistry · 2024Review
- New 1,2,3-triazole/1,2,4-triazole hybrids linked to oxime moiety as nitric oxide donor selective COX-2, aromatase, B-RAFJournal of enzyme inhibition and medicinal chemistry · 2023Article
- New pyrazolyl-thiazolidinone/thiazole derivatives as celecoxib/dasatinib analogues with selective COX-2, HER-2 and EGFR inhibitory effects: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis, molecular modelling and ADME studies.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Novel thiazolone-benzenesulphonamide inhibitors of human and bacterial carbonic anhydrases.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Design, synthesis, docking, and anticancer evaluations of new thiazolo[3,2-Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Lipophilic Studies and In Silico ADME Profiling of Biologically Active 2-Aminothiazol-4(5International journal of molecular sciences · 2023Article
Corrections and comments
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Authors and funding
6 authors at 4 institutions in 7 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Changes in gene expression cause uncontrolled cell proliferation and consequently tumor hypoxia. The tumor cells shift their metabolism to anaerobic glycolysis with a significant modification in pH. Therefore, an over expression of carbonic anhydrase IX (CA IX) genes was detected in many solid tumors. Accordingly, selective inhibition of CA IX can be a useful target for discovering novel antiproliferative agents. The present study described the synthesis of new aryl thiazolone-benzenesulfonamides 4a-j as well as their carbonic anhydrase IX inhibitory effect. All the designed derivatives were evaluated for their anti-proliferative activity against triple-negative breast cancer cell line (as MDA-MB-231) and another breast cancer cell line (MCF-7) in addition to normal breast cell line MCF-10A. Compounds 4b-c, 4e, 4g-h showed significant inhibitory effect against both cancer cell lines at concentration ranges from 1.52-6.31 μM, with a high selectivity against breast cancer cell lines ranges from 5.5 to 17.5 times. Moreover, three sulfonamides derivatives 4e, 4g and 4h showed excellent enzyme inhibition against CA IX with IC
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Registered trials
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