Coumarins and other fused bicyclic heterocycles with selective tumor-associated carbonic anhydrase isoforms inhibitory activity

被引：37

作者：

Bozdag, Murat ^{[1
]}

Alafeefy, Ahmed Mahmoud ^{[2
]}

Altamimi, Abdul Malik ^{[3
]}

Vullo, Daniela ^{[1
]}

Carta, Fabrizio ^{[4
]}

Supuran, Claudiu T. ^{[4
]}

机构：

[1] Univ Florence, Dipartimento Chim, Lab Chim Bioinorgan, Rm 188,Via Lastruccia 3, I-50019 Florence, Italy

[2] Int Islamic Univ, Kulliyyah Sci, Dept Chem, Kuantan, Malaysia

[3] Prince Sattam Bin Abdulaziz Univ, Coll Pharm, Pharmaceut Chem Dept, Al Kharj, Saudi Arabia

[4] Univ Florence, Dipartimento Neurofarba, Sez Sci Farmaceut, Polo Sci, Via U Schiff 6, I-50019 Florence, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2017年 / 25卷 / 02期

关键词：

Carbonic anhydrase inhibitors (CFOs); Quinazolines; Coumarins; 2H-Benzo[e][1,2,4]thiadiazine 1,1-dioxides; Hypoxic tumors; IN-VIVO; THERAPEUTIC APPLICATIONS; ANTIGLAUCOMA ACTION; PHENOLIC-COMPOUNDS; XII INHIBITORS; VB INHIBITORS; ISOZYME-II; IX; DERIVATIVES; ACTIVATORS;

D O I：

10.1016/j.bmc.2016.11.039

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：

Herein we report for the first time a series of 2-benzamido-N-(2-oxo-4-(methylitrifluoromethyl)-2H-chromen-7-yl) benzamide 3a-f and substituted quinazolin-4(3H)-ones and 2H-benzo[e][1,2,4]thiadiazin-3(4H)-one 1,1-dioxides (5, 6, 8 and 10a-c) as selective inhibitors of the tumor associated hCA IX and XII isoforms. Among the compounds reported the trifluoromethyl derivative 3d resulted the most potent against these CA isoforms with K(I)s of 10.9 and 6.7 nM. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：677 / 683

页数：7

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