Synthesis and evaluation of functionalized indoles as antimycobacterial and anticancer agents

被引：0
作者：
Gökçe Cihan-Üstündağ
Gültaze Çapan
机构：
[1] Istanbul University,Department of Pharmaceutical Chemistry, Faculty of Pharmacy
来源：
Molecular Diversity | 2012年 / 16卷
关键词：
Indole; Spirothiazolidinone; Antimycobacterial activity; Antitumor activity;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A new series of 5-fluoro-N2-(cyclohexylidene)-3-phenyl-1H-indole-2-carbohydrazides (6a–6e) and their cyclization products 5-fluoro-N-(3-oxo-1-thia-4-azaspiro [4.5]dec-4-yl)-3-phenyl-1H-indole-2-carboxamides (7a–7e, 8a–8e) have been synthesized and evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using the Microplate Alamar Blue Assay (MABA). Compounds showed moderate to good inhibitory activity at 6.25 μg/mL. Among them, 7b, 7d, 8b, and 8d were the most potent analogs with an inhibition range of 91–95 %. Additionally, compounds 6a, 7a, 7e, 8a, and 8e were subjected to the National Cancer Institute’s (NCI) in vitro disease-oriented antitumor screening to be evaluated for antitumor activity. 8e, the most potent compound examined, displayed broad spectrum antiproliferative activity with particular selectivity against four leukemia cell lines (CCRF-CEM, HL-60 (TB), K-562, and RPMI-8226) with log10GI50 values between −5.68 and −6.09.
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页码：525 / 539
页数：14
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