title: Synthesis and biological evaluation of novel benzothiazole-2-thiol derivatives as potential anticancer agents.
abstract: A series of novel benzothiazole-2-thiol derivatives were synthesized and their structures determined by 1H-NMR, 13C-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(50) = 1.2 nM), SW620 (IC(50) = 4.3 nM), A549 (IC(50) = 44 nM) and HepG2 (IC(50) = 48 nM) and was found to induce apoptosis in HepG2 cancer cells.
authors.affiliation: State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
authors.forename: Xuan-Hong
authors.initials: XH
authors.lastname: Shi
authors.forename: Zhao
authors.initials: Z
authors.lastname: Wang
authors.forename: Yong
authors.initials: Y
authors.lastname: Xia
authors.forename: Ting-Hong
authors.initials: TH
authors.lastname: Ye
authors.forename: Mei
authors.initials: M
authors.lastname: Deng
authors.forename: You-Zhi
authors.initials: YZ
authors.lastname: Xu
authors.forename: Yu-Quan
authors.initials: YQ
authors.lastname: Wei
authors.forename: Luo-Ting
authors.initials: LT
authors.lastname: Yu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D052160:Benzothiazoles