title: Design, Synthesis and Antiproliferative Activity of Novel Benzothiazole Derivatives Conjugated with Semicarbazone Scaffold.
abstract: Two series of novel benzothiazole derivatives conjugated with semicarbazone scaffold were designed and synthesized through a structure-based molecular hybridization strategy. All the target compounds were evaluated for their cytotoxicity in vitro against three cancer cell lines (HT-29, MKN-45 and H460) by standard MTT assay. The pharmacological results indicated that seven compounds (17h-n) exhibited comparable or even better antiproliferative activity in comparison with reference drugs Sorafenib and PAC-1. Particularly, compound 17i displayed remarkable cytotoxicity against tested three cancer cell lines with IC50 values of 0.84, 0.06 and 0.52 µM, which were 4.3-, 36.6-, 4.2-folds more potent than Sorafenib and 1.2-, 13.7-, 6.9-times more active than PAC-1, respectively.
authors.forename: Guanglong
authors.initials: G
authors.lastname: Bao
authors.forename: Baoquan
authors.initials: B
authors.lastname: Du
authors.forename: Yuxiu
authors.initials: Y
authors.lastname: Ma
authors.forename: Meng
authors.initials: M
authors.lastname: Zhao
authors.forename: Ping
authors.initials: P
authors.lastname: Gong
authors.affiliation: School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China. zhaixin_syphu@126.com.
authors.forename: Xin
authors.initials: X
authors.lastname: Zhai
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006835:Hydrazones / Q000494:pharmacology; D015394:Molecular Structure; D009536:Niacinamide / Q000031:analogs & derivatives / Q000494:pharmacology; D010671:Phenylurea Compounds / Q000494:pharmacology; D010879:Piperazines / Q000494:pharmacology; D012664:Semicarbazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000077157:Sorafenib
chemical_list: C514579:(4-benzylpiperazin-1-yl)acetic acid (3-allyl-2-hydroxybenzylidene)hydrazine; C000621029:2-(5,7-dimethyl-2-oxoindolin-3-ylidene)-N-(6-((4-methylpiperidin-1-yl)methyl)benzo(d)thiazol-2-yl)hydrazinecarboxamide; D000970:Antineoplastic Agents; D052160:Benzothiazoles; D006835:Hydrazones; D010671:Phenylurea Compounds; D010879:Piperazines; D012664:Semicarbazones; D009536:Niacinamide; D000077157:Sorafenib