Design and synthesis of novel 1,2,3-triazole-dithiocarbamate hybrids as potential anticancer agents

• Published in: European journal of medicinal chemistry Vol. 62; pp. 11 - 19
• Main Authors: Duan, Ying-Chao, Ma, Yong-Cheng, Zhang, En, Shi, Xiao-Jing, Wang, Meng-Meng, Ye, Xian-Wei, Liu, Hong-Min
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier 01.04.2013
• Subjects: Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Apoptosis - drug effects; Cell Cycle - drug effects; Cell Line, Tumor; Cell Proliferation - drug effects; Chemistry, Medicinal; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Humans; Life Sciences & Biomedicine; MCF-7 Cells; Molecular Structure; Pharmacology & Pharmacy; Science & Technology; Structure-Activity Relationship; Thiocarbamates - chemical synthesis; Thiocarbamates - chemistry; Thiocarbamates - pharmacology; Triazoles - chemical synthesis; Triazoles - chemistry; Triazoles - pharmacology; ANALOGS; ANTIFUNGAL ACTIVITY; Hybrid; Cell cycle arrest; ANTITUMOR-ACTIVITY; CANCER; 1,2,3-TRIAZOLES; BIOLOGICAL EVALUATION; Dithiocarbamate; HIV-1 PROTEASE; INHIBITORS; Anticancer; 1,2,3-triazole; DERIVATIVES; Apoptosis
• ISSN: 0223-5234; 1768-3254; 1768-3254
• DOI: 10.1016/j.ejmech.2012.12.046

A series of novel 1,2,3-triazole-dithiocarbamate hybrids were designed, synthesized and evaluated for anticancer activity against four selected human tumor cell lines (MGC-803, MCF-7, PC-3, EC-109). Majority of the synthesized compounds exhibited moderate to potent activity against MGC-803 and MCF-7. Among them, compounds 3a and 3c showed excellent broad spectrum anticancer activity with IC50 values ranging from 0.73 to 11.61 mu M and 0.49-12.45 mu M, respectively. Particularly, compound 3a was more potent than 5-fluorouracil against all tested human cancer cell lines. Flow cytometry analysis demonstrated that treatment of MGC-803 with 3c led to cell cycle arrest at G2/M phase accompanied by an increase in apoptotic cell death after 12 h. (C) 2013 Elsevier Masson SAS. All rights reserved.