Gomha Sobhi M, Abdelaziz Mohamad R, Abdel-Aziz Hassan M, Hassan Shaimaa A
Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, MIU University, Egypt.
Mini Rev Med Chem. 2017;17(9):805-815. doi: 10.2174/1389557516666161223154539.
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.
通过2-(1-(4-甲基-2-苯基噻唑-5-基)亚乙基)肼基硫代酰胺与卤代肼叉反应，以良好的产率合成了一系列新型噻唑衍生物。该反应在DABCO作为有机催化剂的存在下进行，反应时间短，后处理容易，产率良好至优异。新合成产物的结构尽可能通过元素分析、光谱数据和替代路线进行阐明。对十种化合物针对结肠癌细胞系（HCT-116）的抗癌活性进行了评估。
结果表明，大多数测试化合物显示出高或中等抗癌活性。通过分子操作环境（MOE）程序对五种新型噻唑基-噻唑衍生物进行了分子对接。
