title: Design, synthesis and antiproliferative activity studies of novel 1,2,3-triazole-dithiocarbamate-urea hybrids.
abstract: A series of novel 1,2,3-triazole-dithiocarbamate-urea hybrids were designed, synthesized and their antiproliferative activities against four selected human cancer cell lines were evaluated. The results showed that a number of the hybrids exhibited potent activity in selected human cancer cell lines. Among them, compounds 27 and 34 showed broad spectrum anticancer activity with IC50 values ranging from 1.62 to 20.84 μM and 0.76 to 13.55 μM, respectively. Interestingly, compounds 27 and 34, being very potent against MGC-803 cells, exhibited no significant cytotoxicity against normal human embryonic kidney cells at up to 55 μM and 70 μM, respectively. Evidences of cell cycle arrest and apoptosis induction were obtained for the most effective compounds 27 and 34 by means of flow cytometry and microscopic techniques.
authors: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
authors: Ying-Chao
authors: YC
authors: Duan
authors: Yi-Chao
authors: YC
authors: Zheng
authors: Xiao-Chen
authors: XC
authors: Li
authors: Meng-Meng
authors: MM
authors: Wang
authors: Xian-Wei
authors: XW
authors: Ye
authors: Yuan-Yuan
authors: YY
authors: Guan
authors: Gai-Zhi
authors: GZ
authors: Liu
authors: Jia-Xin
authors: JX
authors: Zheng
authors: Hong-Min
authors: HM
authors: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013859:Thiocarbamates / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*; D014508:Urea / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D013859:Thiocarbamates; D014230:Triazoles; D014508:Urea