Design, synthesis, cytotoxic evaluation and molecular docking of novel 1, 3, 4-thiadiazole sulfonamides with azene and coumarin moieties as carbonic anhydrase inhibitors DOI Creative Commons
Samir Bondock,

Tallah Albarqi,

Tamer Nasr

et al.

Arabian Journal of Chemistry, Journal Year: 2023, Volume and Issue: 16(8), P. 104956 - 104956

Published: May 3, 2023

New thiadiazole sulfonamide derivatives were designed as human carbonic anhydrase inhibitors (hCAIs) to develop robust and novel anticancer agents. Tail modification approach was considered in designing the target compounds which synthesized following two-step procedure starting from 5-acetyl-3-N-(4-sulfamoylphenyl)-2-imino-1,3,4-thiadiazoline. Cytotoxic evaluation revealed potent diazene derivative 2 with IC50 1.18 μM, 5.28 μM 7.15 against MCF-7, Caco2 HepG-2, respectively. Moreover, dihydroxyphenyl triazene 5 demonstrated 3.03 5.66 12.50 Caco2, HepG-2 Similarly, carbohydrazide coumarin 18 showed of 2.00 12.30 HepG2, Molecular docking using hCAIX hCAXII adopted explain achieved cytotoxicity on molecular level their silico ADME evaluation.

Language: Английский

Unveiling sultam in drug discovery: spotlight on the underexplored scaffold DOI
Yie Kie Chong,

Yee Swen Ong,

Keng Yoon Yeong

et al.

RSC Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 15(6), P. 1798 - 1827

Published: Jan. 1, 2024

Decades ago, the application of cyclic sulfonamide (sultam) and its derivatives primarily focused on their antibacterial properties. However, recent years have seen a shift in research attention towards exploring potential as anticancer, anti-inflammatory, antidiabetic, antiviral agents. Despite this broadening scope, only few sultam drugs made it to commercial market, much sultams remains discovery phase. This class compounds holds significant promise pertinent pharmaceutical research. Due sultam's relevance growing importance drug discovery, review paper aims consolidate examine biological activities ranging from 4 8-membered ring structures.

Language: Английский

Citations

6
A comparative study of diaryl urea molecules with and without sulfonamide group on Carbonic anhydrase IX and XII inhibition and its consequence on breast cancer cells DOI
Joy Debnath,

Dhananjaya Keshamasetthy,

Jacob Combs

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 145, P. 107192 - 107192

Published: Feb. 10, 2024

Language: Английский

Citations

5
Interactions of novel 1,3-diaryltriazene-sulfamethazines with carbonic anhydrases: Kinetic studies and in silico simulations DOI
Nebih Lolak, Cüneyt Türkeş, Süleyman Akocak

et al.

Archives of Biochemistry and Biophysics, Journal Year: 2024, Volume and Issue: 761, P. 110181 - 110181

Published: Oct. 11, 2024

Language: Английский

Citations

5
CRISPRi/a screens in human iPSC-cardiomyocytes identify glycolytic activation as a druggable target for doxorubicin-induced cardiotoxicity DOI
Chunying Liu, Mengcheng Shen, Yanxia Liu

et al.

Cell stem cell, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 1, 2024

Language: Английский

Citations

5
Design, synthesis, cytotoxic evaluation and molecular docking of novel 1, 3, 4-thiadiazole sulfonamides with azene and coumarin moieties as carbonic anhydrase inhibitors DOI Creative Commons
Samir Bondock,

Tallah Albarqi,

Tamer Nasr

et al.

Arabian Journal of Chemistry, Journal Year: 2023, Volume and Issue: 16(8), P. 104956 - 104956

Published: May 3, 2023

New thiadiazole sulfonamide derivatives were designed as human carbonic anhydrase inhibitors (hCAIs) to develop robust and novel anticancer agents. Tail modification approach was considered in designing the target compounds which synthesized following two-step procedure starting from 5-acetyl-3-N-(4-sulfamoylphenyl)-2-imino-1,3,4-thiadiazoline. Cytotoxic evaluation revealed potent diazene derivative 2 with IC50 1.18 μM, 5.28 μM 7.15 against MCF-7, Caco2 HepG-2, respectively. Moreover, dihydroxyphenyl triazene 5 demonstrated 3.03 5.66 12.50 Caco2, HepG-2 Similarly, carbohydrazide coumarin 18 showed of 2.00 12.30 HepG2, Molecular docking using hCAIX hCAXII adopted explain achieved cytotoxicity on molecular level their silico ADME evaluation.

Language: Английский

Citations

13