Department of Organic Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Arch Pharm (Weinheim). 2010 Jul;343(7):404-10. doi: 10.1002/ardp.200900150.
New derivatives of thiophenes 2, 12, iminoaminothieno[2,3-d]pyrimidines 3, 5, and 6, triazolothieno[2,3-d]pyrimidines 8-11, pyrazolo- and triazinothieno[2,3-d]pyrimidines 4, 7, respectively, have been prepared by different synthetic procedures. Structure elucidation of the newly synthesized compounds was carried out via elemental analyses and spectral data. The antitumor activity of compounds 2, 3, and 9-12 was evaluated against in-vitro cell lines (HEPG-2 and MCF-7). Compounds 2, 3, 10, 11, and 12 showed significant in-vitro cytotoxic activity against hepatocellular carcinoma (HEPG-2) compared to the reference drug Doxorubicin. Compound 2 showed significant in-vitro cytotoxic activity against breast cancer (MCF-7) cells compared to the reference drug Doxorubicin. The augmenting effect of gamma-radiation was assessed; here, compounds 2, 3, 10, and 11 showed the most potent in-vitro anticancer activity.
已通过不同的合成程序制备了噻吩、亚氨基氨基噻吩并[2,3-d]嘧啶、三唑并噻吩并[2,3-d]嘧啶、吡唑并噻吩并[2,3-d]嘧啶、吡嗪并噻吩并[2,3-d]嘧啶的新衍生物 2、12、3、5、6、8-11、4、7。通过元素分析和光谱数据对新合成的化合物的结构进行了阐明。对化合物 2、3 和 9-12 的抗肿瘤活性进行了评估，这些化合物针对的是体外细胞系（HEPG-2 和 MCF-7）。与参考药物阿霉素相比，化合物 2、3、10、11 和 12 对肝癌（HEPG-2）具有显著的体外细胞毒性。与参考药物阿霉素相比，化合物 2 对乳腺癌（MCF-7）细胞具有显著的体外细胞毒性。评估了伽马辐射的增强作用；在这里，化合物 2、3、10 和 11 显示出最强的体外抗癌活性。
