一些新型四氢苯并[4,5]噻吩并[2,3-d]嘧啶衍生物的合成、抗肿瘤和抗菌活性。
Synthesis, antitumor and antibacterial activities of some novel tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine derivatives.
机构信息
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, El-Kasr El Aini Street, 11562 Cairo, Egypt.
出版信息
Eur J Med Chem. 2013 Jul;65:195-204. doi: 10.1016/j.ejmech.2013.04.055. Epub 2013 May 3.
Two series of new tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidines namely 2,3-disubstituted derivatives 3a-z and 2,4-disubstituted ones 6a-c were prepared and tested for their antitumor and antibacterial activities. The structures of the prepared compounds were confirmed by spectral and elemental analyses. Compound 3z exhibited the highest antitumor activity against breast MCF-7 with IC50 = 0.19 μM compared to Doxorubicin (IC50 = 5.46 μM), while 3r was the most active one against liver HEPG-2 cancer cell line with IC50 = 1.29 μM as regard to Doxorubicin (IC50 = 7.36 μM). Concerning the antibacterial activity, compounds 3m and 3z exerted remarkable activity against the tested bacterial species compared to Ampicillin, whereas compound 6c showed good activity against only Gram positive species.
我们合成了两类新的四氢苯并[4,5]噻吩并[2,3-d]嘧啶类化合物，分别是 2,3-二取代衍生物 3a-z 和 2,4-二取代衍生物 6a-c，并对它们的抗肿瘤和抗菌活性进行了测试。通过光谱和元素分析确认了所合成化合物的结构。化合物 3z 在针对 MCF-7 乳腺癌细胞的实验中表现出最强的抗肿瘤活性，IC50 值为 0.19 μM，而对照品多柔比星（Doxorubicin）的 IC50 值为 5.46 μM；化合物 3r 对 HEPG-2 肝癌细胞系的活性最强，IC50 值为 1.29 μM，而对照品多柔比星（Doxorubicin）的 IC50 值为 7.36 μM。在抗菌活性方面，化合物 3m 和 3z 对测试的细菌种类表现出显著的活性，优于氨苄西林（Ampicillin），而化合物 6c 仅对革兰氏阳性菌表现出良好的活性。
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