2. Academic Validation
  3. Synthesis, structure-activity relationships and preliminary antitumor evaluation of benzothiazole-2-thiol derivatives as novel apoptosis inducers

Synthesis, structure-activity relationships and preliminary antitumor evaluation of benzothiazole-2-thiol derivatives as novel apoptosis inducers

  • Bioorg Med Chem Lett. 2011 Feb 15;21(4):1097-101. doi: 10.1016/j.bmcl.2010.12.124.
Zhao Wang 1,  Xuan-Hong Shi,  Jia Wang,  Tian Zhou,  You-Zhi Xu,  Ting-Ting Huang,  Yan-Fang Li,  Ying-Lan Zhao,  Li Yang,  Sheng-Yong Yang,  Luo-Ting Yu,  Yu-Quan Wei
Affiliations

Affiliation

  • 1 State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Sichuan 610041, China.
PMID: 21262571 DOI: 10.1016/j.bmcl.2010.12.124
Abstract

A series of novel benzothiazole-2-thiol derivatives were synthesized, and their anti-proliferative activities on HepG2 and MCF-7 cells were investigated. Most compounds had inhibitory effects on cell growth, and some of them were more effective than cisplatin. Compounds 6m and 6t displayed good inhibitory activities against a panel of different types of human Cancer cell lines, with IC(50) values in the low micromolar range. Further biological evaluation indicated that 6m induced Apoptosis in HepG2 Cancer cells. Structure-activity relationships were also proposed.

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