Carbonic anhydrase inhibition with a series of novel benzenesulfonamide-triazole conjugates

被引：27

作者：

El-Gazzar, Marwa G. ^{[1
]}

Nafie, Nessma H. ^{[1
]}

Nocentini, Alessio ^{[2
]}

Ghorab, Mostafa M. ^{[1
]}

Heiba, Helmi I. ^{[1
]}

Supuran, Claudiu T. ^{[2
]}

机构：

[1] EAEA, NCRRT, Dept Drug Radiat Res, POB 29, Cairo, Egypt

[2] Univ Florence, NEUROFARBA Dept, Pharmaceut & Nutraceut Sci Sect, Via Ugo Schiff 6, I-50019 Florence, Italy

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2018年 / 33卷 / 01期

关键词：

Carbonic anhydrase; benzenesulfonamide; 1,2,3-triazole; hCA IX; anti-proliferative; ISOZYME-II; RADIOSENSITIZING EVALUATION; SULFONAMIDE INHIBITION; HELICOBACTER-PYLORI; MOLECULAR DOCKING; DRUG DISCOVERY; IX; ANTICANCER; DESIGN; DERIVATIVES;

D O I：

10.1080/14756366.2018.1513927

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We report the synthesis and characterisation of a novel series of triazole benzenesulfonamide derivatives, which incorporate the general pharmacophore associated with carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The synthesised compounds were tested in vitro against four human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes, hCA I, hCA II, hCA IV and hCA IX. The obtained results showed that the tumour-associated hCA IX was the most sensitive to inhibition with the synthesised derivatives, with the triazolo-pyridine benzenesulfonamides 14, 16 and 17 being the most effective inhibitors. Some selected compounds were chosen for a single dose anti-proliferative activity testing against a panel of 57 human tumour cell lines and show some anti-proliferative activity ex vivo.

引用

页码：1565 / 1574

页数：10

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