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Synthesis and Biological Evaluation of Novel Benzothiazole-2-thiol Derivatives as Potential Anticancer Agents.

Authors :
Xuan-Hong Shi
Zhao Wang
Yong Xia
Ting-Hong Ye
Mei Deng
You-Zhi Xu
Yu-Quan Wei
Luo-Ting Yu
Source :
Molecules; Apr2012, Vol. 17 Issue 4, p3933-3944, 12p
Publication Year :
2012

Abstract

A series of novel benzothiazole-2-thiol derivatives were synthesized and their structures determined by <superscript>1</superscript>H-NMR, <superscript>13</superscript>C-NMR and HRMS (ESI). The effects of all compounds on a panel of different types of human cancer cell lines were investigated. Among them, pyridinyl-2-amine linked benzothiazole-2-thiol compounds 7d, 7e, 7f and 7i exhibited potent and broad-spectrum inhibitory activities. Compound 7e displayed the most potent anticancer activity on SKRB-3 (IC<subscript>50</subscript> = 1.2 nM), SW620 (IC50 = 4.3 nM), A549 (IC<subscript>50</subscript> = 44 nM) and HepG2 (IC<subscript>50</subscript> = 48 nM) and was found to induce apoptosis in HepG2 cancer cells. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
14203049
Volume :
17
Issue :
4
Database :
Complementary Index
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
75144851
Full Text :
https://doi.org/10.3390/molecules17043933