Design, synthesis and biological evaluation of novel carbamodithioates as anti-proliferative agents against human cancer cells
| Autor: | Rui Xie, Zhijun Wang, Pingwah Tang, Liu Xia, Qipeng Yuan |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Antineoplastic Agents Apoptosis HeLa Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Thiocarbamates Drug Discovery Tumor Cells Cultured Humans Cell Proliferation Pharmacology Dose-Response Relationship Drug Molecular Structure biology Chemistry Organic Chemistry General Medicine Anti proliferative biology.organism_classification Combinatorial chemistry 030104 developmental biology Design synthesis Drug Design 030220 oncology & carcinogenesis Cancer cell Drug Screening Assays Antitumor Human cancer Sulforaphane Protic solvent |
| Zdroj: | European Journal of Medicinal Chemistry. 157:1526-1540 |
| ISSN: | 0223-5234 |
| Popis: | A series of new carbamodithioates compounds has been successfully synthesized. All the carbamodithioate derivatives of SFE and SFA with benzenethiols (substituted or unsubstituted) exhibited, in general, higher percentages of inhibition than their parent compounds: SFE and SFA. A number of carbamodithioate derivatives with benzenethiols (substituted or unsubstituted) (1l, 1m, 1n, 1o, 1q, 1s, 2l, 2n, 2p, 2q, 2r and 2s) were investigated for in vitro anti-proliferative activities against five cancer cell lines: SMMC-7721, A549, A375, HCT 116 and Hela. The carbamodithioate compounds (1l, 1m, 1n, 1o, 1q and 1s) derived from SFE and the carbamodithioate compounds (2l, 2n, 2p, 2q, 2r and 2s) derived from SFA are more sensitive toward SMMC-7721and A549 cancer cells than toward other cancer cells in that their IC50 values are appreciably lower. Moreover, they exhibited stronger inhibitory activities than their parent compound SFE and SFE. Further investigation indicated that these carbamodithioate derivatives inhibited colony formation of SMMC-7721 and remarkably induced the G2/M or G0/G1 phase cell cycle arrest and apoptosis in SMMC-7721 cancer cells. More important, these carbamodithioate derivatives are stable in protic solvent media than their parent compounds. By virtue of the simplicity of the preparation of these carbamodithioate derivatives and their stability, compounds 1m and 2s could be the promising candidates for replacement for their parent SFE and SFA for cancer prevention agents. |
| Databáze: | OpenAIRE |
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