Abstract
Method: A series of novel thiazole derivatives were synthesized in a good yield via reaction of 2-(1-(4-methyl-2-phenylthiazol-5-yl)ethylidene)hydrazine carbothioamide with hydrazonoyl halides. The reaction was performed in the presence of DABCO as an organocatalyst in short reaction times, easy workup, good to excellent yields. The structure of the newly synthesized products was elucidated via elemental analysis, spectral data and alternative routes whenever possible. Ten compounds were evaluated for their anti-cancer activity against the colon carcinoma cell line (HCT-116).
Results & Conclusion: The results revealed that most of the tested compounds showed high or moderate anti-cancer activity. The molecular docking of five novel thiazolyl-thiazole derivatives was performed by the Molecular Operating Environment (MOE) program.Keywords: Cytotoxic activity, hydrazonoyl halides, molecular docking, tautomerism, thiazoles, thiosemicarbazone.
Mini-Reviews in Medicinal Chemistry
Title:Green Synthesis and Molecular Docking of Thiazolyl-thiazole Derivatives as Potential Cytotoxic Agents
Volume: 17 Issue: 9
Author(s): Sobhi M. Gomha*, Mohamad R. Abdelaziz, Hassan M. Abdel-Aziz and Shaimaa A. Hassan
Affiliation:
- Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613,Egypt
Keywords: Cytotoxic activity, hydrazonoyl halides, molecular docking, tautomerism, thiazoles, thiosemicarbazone.
Abstract: Method: A series of novel thiazole derivatives were synthesized in a good yield via reaction of 2-(1-(4-methyl-2-phenylthiazol-5-yl)ethylidene)hydrazine carbothioamide with hydrazonoyl halides. The reaction was performed in the presence of DABCO as an organocatalyst in short reaction times, easy workup, good to excellent yields. The structure of the newly synthesized products was elucidated via elemental analysis, spectral data and alternative routes whenever possible. Ten compounds were evaluated for their anti-cancer activity against the colon carcinoma cell line (HCT-116).
Results & Conclusion: The results revealed that most of the tested compounds showed high or moderate anti-cancer activity. The molecular docking of five novel thiazolyl-thiazole derivatives was performed by the Molecular Operating Environment (MOE) program.Export Options
About this article
Cite this article as:
Gomha M. Sobhi*, Abdelaziz R. Mohamad, Abdel-Aziz M. Hassan and Hassan A. Shaimaa, Green Synthesis and Molecular Docking of Thiazolyl-thiazole Derivatives as Potential Cytotoxic Agents, Mini-Reviews in Medicinal Chemistry 2017; 17 (9) . https://dx.doi.org/10.2174/1389557516666161223154539
DOI https://dx.doi.org/10.2174/1389557516666161223154539 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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