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

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...

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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
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Abstract	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.
AbstractList	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 μM and 0.49-12.45 μM, 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.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 μM and 0.49-12.45 μM, 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. 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. 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 μM and 0.49-12.45 μM, 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.
Author	Zhang, En Liu, Hong-Min Ye, Xian-Wei Duan, Ying-Chao Shi, Xiao-Jing Ma, Yong-Cheng Wang, Meng-Meng
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BackLink	https://www.ncbi.nlm.nih.gov/pubmed/23353743$$D View this record in MEDLINE/PubMed
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Keywords	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
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PublicationTitle	European journal of medicinal chemistry
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Snippet	A series of novel 1,2,3-triazole-dithiocarbamate hybrids were designed, synthesized and evaluated for anticancer activity against four selected human tumor...
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SubjectTerms	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
Title	Design and synthesis of novel 1,2,3-triazole-dithiocarbamate hybrids as potential anticancer agents
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