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巯基三唑并苯并噻二嗪连接的氨基苯并噻唑作为潜在抗癌剂的合成及生物学评价

Synthesis and biological evaluation of mercapto triazolo-benzothiadiazine linked aminobenzothiazoles as potential anticancer agents.

作者信息

Kamal Ahmed, Khan Mohammed Naseer A, Srikanth Yellamelli V V, Rajesh Shetti V C R N C

出版信息

Chem Biol Drug Des. 2009 Jun;73(6):687-93. doi: 10.1111/j.1747-0285.2009.00815.x.

DOI:10.1111/j.1747-0285.2009.00815.x
PMID:19635062
Abstract

The synthesis of a series of 10-substituted 5,5-dioxo-5,10-dihydro[1,2,4]triazolo[4,3-b][1,2,4]benzothiadiazine coupled with sulfanylacetamido benzothiazole pharmacophores (5a-g) is described. All the synthesized compounds have been evaluated for their anticancer activity. Most of the compounds showed significant growth inhibitory activity against selected human tumor cell lines. Interestinlgy, one of the synthesized compounds 5d, exhibited GI(50) values of 1.4 and 2.1 microM against RPMI-8226 (leukemia) and HOP-62 (lungs) cell lines, respectively.

摘要

描述了一系列10-取代的5,5-二氧代-5,10-二氢[1,2,4]三唑并[4,3-b][1,2,4]苯并噻二嗪与硫代乙酰氨基苯并噻唑药效基团（5a - g）的合成。对所有合成的化合物进行了抗癌活性评估。大多数化合物对选定的人类肿瘤细胞系显示出显著的生长抑制活性。有趣的是，合成化合物之一5d对RPMI - 8226（白血病）和HOP - 62（肺癌）细胞系的GI(50)值分别为1.4和2.1 microM。

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