Abstract

Seven benzophenone compounds were synthesized in one or two steps, then their antitumor activity was evaluated. The total yields ranged from 9% to 44%. Compounds 3c–5c exhibited obvious antitumor activity. Among them, compounds 3c and 4c exhibited excellent and broad-spectrum antitumor activity. Compound 3c exhibited much stronger inhibitory activities against fourteen cancer cells than cisplatin. In particular, compound 3c exhibited stronger cytotoxicity against hepatocarcinoma SMMC-7721 cells than Taxol, with a half maximal inhibitory concentration (IC₅₀) of approximately 0.111 μM. These results demonstrated that compounds 3c, 4c and 5c were very promising antitumor leads for further structural modification.

摘要

通过一个或两个步骤合成了七种二苯甲酮化合物，然后评估了它们的抗肿瘤活性。总产率为 9% 至 44%。化合物3c-5c表现出明显的抗肿瘤活性。其中化合物3c和4c表现出优异的广谱抗肿瘤活性。化合物3c对 14 种癌细胞的抑制活性比顺铂强得多。特别是，化合物3c对肝癌SMMC-7721细胞的细胞毒性比紫杉醇更强，半数最大抑制浓度(IC ₅₀ )约为0.111 μM。这些结果表明化合物3c、4c5c和5c是非常有前景的用于进一步结构修饰的抗肿瘤先导物。