A series of 1,3‐diaryl‐2‐propenones 2a–j and analogous 2‐benzylidene‐1,3‐indandiones 3a–j were evaluated against various neoplasms and normal cells. In general, greater cytotoxic potencies and selective toxicity to human malignant cells were observed by the compounds in series 2 rather than 3. In particular, 2i emerged as a lead molecule having an average CC50 figure of 8.6 µM and a selective index value of 18. Various physicochemical features of 2a–j were correlated with the cytotoxic potencies to neoplastic cell lines which provide guidelines for expansion of this series of compounds. The enone 2i induced internucleosomal DNA fragmentation and activated caspase‐3 in HL‐60 cells suggesting that one of the ways in which the cytotoxicity of the compounds in series 2 is mediated towards some of the cell lines used in this study is by apoptosis. Neurotoxicity in mice was generally lower in series 2 than 3a–j.

中文翻译：

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1,3-Diaryl-2-propenones 和 2-Benzylidene-1,3-indandiones：探索对肿瘤比正常细胞具有更大毒性的化合物

针对各种肿瘤和正常细胞评估了一系列 1,3-二芳基-2-丙烯酮 2a-j 和类似的 2-亚苄基-1,3-茚满二酮 3a-j。一般而言，通过系列 2 而非系列 3 中的化合物观察到更大的细胞毒性效力和对人类恶性细胞的选择性毒性。特别是，2i 以平均 CC50 值为 8.6 µM 和选择性指数值为 18 的先导分子出现。 2a-j 的各种理化特征与对肿瘤细胞系的细胞毒性效力相关，这为扩展这一系列化合物提供了指导。enone 2i 在 HL-60 细胞中诱导核小体间 DNA 断裂并激活 caspase-3，这表明系列 2 中化合物对本研究中使用的某些细胞系的细胞毒性的一种方式是通过细胞凋亡。