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

Bozdag, Murat and Alafeefy, Ahmed Mahmoud and Altamimi, Abdul Malik and Vullo, Daniela and Carta, Fabrizio and Supuran,, Claudiu T. (2017) Coumarins and other fused bicyclic heterocycles with selective tumor-associated carbonic anhydrase isoforms inhibitory activity. Bioorganic and Medicinal Chemistry, 25 (2). pp. 677-683. ISSN 0968-0896 E-ISSN 1464-3391

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Abstract

Herein we report for the first time a series of 2-benzamido-N-(2-oxo-4-(methyl/trifluoromethyl)-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 KIs of 10.9 and 6.7 nM

Item Type:	Article (Journal)
Additional Information:	7668/56574
Uncontrolled Keywords:	Carbonic anhydrase inhibitors (CAIs); Quinazolines; Coumarins; 2H-Benzo[e][1,2,4]thiadiazine 1,1-dioxides; Hypoxic tumors
Subjects:	Q Science > Q Science (General) R Medicine > RC Internal medicine R Medicine > RM Therapeutics. Pharmacology
Kulliyyahs/Centres/Divisions/Institutes (Can select more than one option. Press CONTROL button):	Kulliyyah of Science Kulliyyah of Science > Department of Chemistry
Depositing User:	Engku Norulizati Engku Aziz
Date Deposited:	08 Jun 2017 13:50
Last Modified:	13 Mar 2018 09:18
URI:	http://irep.iium.edu.my/id/eprint/56574

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