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Discovery and optimization of novel dual dithiocarbamates as potent anticancer agents
Li R.-D.; Wang H.-L.; Li Y.-B.; Wang Z.-Q.; Wang X.; Wang Y.-T.; Ge Z.-M.; Li R.-T.
Source PublicationEuropean Journal of Medicinal Chemistry

A series of dual dithiocarbamates were synthesized and evaluated for their in-vitro anticancer activities on human non-small cell lung cancer cell line H460. Nine compounds exhibited significant antiproliferative activities with IC50 less than 1 μM. Among them, compound 14m showed the highest inhibitory activity against H460 cell and inhibited the growth of nine types of tumor cells with IC50 values less than 1 μM. It also achieved IC50 of 54 nM and 23 nM against HepG2 and MCF-7 cell lines, respectively. Preliminary structure-activity relationship study indicated that: a) when the methyl group (region A) is substituted with benzene rings, ortho substitution on the benzene ring is favored for activity; b) substitution with heterocyclic structures at region A exhibited greater impact on the anti-tumor activity of compounds, in which pyridine ring, thiazole ring, coumarin and benzo[b]thiophene are favored and quinoline ring is the most favored; c) substitution with different amines (region B) also showed marked effect on the activity of compounds and dimethylamine and morpholine are preferred to other tested amines. © 2015 Elsevier Masson SAS. All rights reserved.

KeywordAnti-tumor Activity Dual Dithiocarbamate Structureeactivity Relationship Synthesis
URLView the original
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000351646100039
The Source to ArticleScopus
被引频次[WOS]:28   [WOS记录]     [WOS相关记录]
Document TypeJournal article
专题Institute of Chinese Medical Sciences
Affiliation1.State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China
2.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau999078, Macau
GB/T 7714
Li R.-D.,Wang H.-L.,Li Y.-B.,et al. Discovery and optimization of novel dual dithiocarbamates as potent anticancer agents[J]. European Journal of Medicinal Chemistry,2015,93:381.
APA Li R.-D..,Wang H.-L..,Li Y.-B..,Wang Z.-Q..,Wang X..,...&Li R.-T..(2015).Discovery and optimization of novel dual dithiocarbamates as potent anticancer agents.European Journal of Medicinal Chemistry,93,381.
MLA Li R.-D.,et al."Discovery and optimization of novel dual dithiocarbamates as potent anticancer agents".European Journal of Medicinal Chemistry 93(2015):381.
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