Synthesis and Cytotoxicity of Some Thieno[2,3-d]pyrimidine Derivatives

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• 作者：Abdelreheem A. Saddik ; Adel M. Kamal El-Dean ; Gamal H. El-Sokary ; Khairy M. Hassan ; Mohamed S. Abbady ; Ismail A. Ismail and Saber H. Saber
• 刊名：Journal of the Chinese Chemical Society
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：64
• 期：1
• 页码：87-93
• 全文大小：332K
• ISSN：2192-6549

文摘

A series of compounds 5-amino-2-ethylmercapto-4-phenyl-6-subistitutedthieno[2,3-d]pyrimidines (8a–d), 4-chloro-7-ethylmercapto-9-phenylpyrimido[5′,4′:4,5]thieno[3,2-d]triazine (9), and 2-ethylmercapto-8-oxo-4-phenyl-7-(4-chlorophenyl)pyrimido [4′,5′:4,5]thieno[2,3-d]pyrimidine (10) were synthesized and their structures were confirmed by ¹H NMR, ¹³C NMR, and MS. All compounds were evaluated for their IC₅₀ values against three cancer cell lines (MCF-7, HUH-7 and BHK) and WISH cells. The IC₅₀ of compound (8d) was calculated for each cell line. Interestingly, the IC₅₀ for the normal human amnion WISH cell line was much higher (723 µg/mL) than those found for the tumor cell lines BHK (17 µg/mL), HUH-7 (5.8 µg/mL), and MCF-7 (8.3 µg/mL). The proliferation inhibition of normal (WISH) and tumor (BHK, HUH-7, and MCF-7) cells by compound (8d) was investigated using MTT assay, and the IC₅₀ was calculated after 48 h of treatment for each cell line.