title: Design, synthesis and antiproliferative activity studies of novel dithiocarbamate-chalcone derivates.
abstract: A series of novel dithiocarbamate-chalcone derivates were designed, synthesized and evaluated for antiproliferative activity against three selected cancer cell lines (EC-109, SK-N-SH and MGC-803). Majority of the synthesized compounds exhibited moderate to potent activity against all the cancer cell lines assayed. Particularly, compounds II2 and II5 exhibited the excellent growth inhibition against SK-N-SH with IC50 values of 2.03μM and 2.46μM, respectively. Further mechanism studies revealed that compound II2 could obviously inhibit the proliferation of SK-N-SH cells by inducing apoptosis and arresting the cell cycle at G0/G1 phase.
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Dong-Jun
authors.initials: DJ
authors.lastname: Fu
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Sai-Yang
authors.initials: SY
authors.lastname: Zhang
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Ying-Chao
authors.initials: YC
authors.lastname: Liu
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Li
authors.initials: L
authors.lastname: Zhang
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Jun-Ju
authors.initials: JJ
authors.lastname: Liu
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Jian
authors.initials: J
authors.lastname: Song
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Ruo-Han
authors.initials: RH
authors.lastname: Zhao
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Feng
authors.initials: F
authors.lastname: Li
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Hui-Hui
authors.initials: HH
authors.lastname: Sun
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Hong-Min
authors.initials: HM
authors.lastname: Liu
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
authors.forename: Yan-Bing
authors.initials: YB
authors.lastname: Zhang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D053148:Caspase 3 / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002599:Chalcone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000633:toxicity; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects; D006801:Humans; D013329:Structure-Activity Relationship; D013859:Thiocarbamates / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D016159:Tumor Suppressor Protein p53 / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D013859:Thiocarbamates; D016159:Tumor Suppressor Protein p53; D002599:Chalcone; D053148:Caspase 3
keywords: Antiproliferative activity; Apoptosis; Chalcone; Dithiocarbamate