Chemistry Department, Faculty of Science, Taif University, Al-Haweiah, P.O. Box 888, Taif 21974, Saudi Arabia.
On leave from Chemistry Department, Faculty of Science, Aswan University, Aswan, P.O. Box, Aswan 81528, Egypt.
Molecules. 2020 Apr 28;25(9):2051. doi: 10.3390/molecules25092051.
In search of unprecedented tri and/or tetrapod pharmacophoric conjugates, a series of 32 new 4-ethyl-1-benzo[][1,4]diazepin-2(3)-ones were synthesized and properly elucidated using MS, IR, NMR, and elemental analysis. investigation of 11 compounds of this series, using a panel of two human tumor cell lines namely; human breast adenocarcinoma (MCF-7), and human colorectal carcinoma (HCT-116), revealed promising cytotoxic activities. Among all synthesized compounds, analogue displayed maximum cytotoxicity with IC values of 16.19 ± 1.35 and 17.16 ± 1.54 μM against HCT-116 and MCF-7, respectively, compared to standard drug doxorubicin.
为了寻找前所未有的三或四元药效团共轭物，我们合成了一系列 32 种新型 4-乙基-1-苯并[][1,4]二氮杂卓-2(3)-酮，并通过 MS、IR、NMR 和元素分析进行了适当的阐明。对该系列中的 11 种化合物进行了研究，使用了两组人肿瘤细胞系，即人乳腺癌（MCF-7）和人结肠直肠癌细胞（HCT-116），显示出有希望的细胞毒性活性。在所合成的所有化合物中，类似物 表现出最大的细胞毒性，其对 HCT-116 和 MCF-7 的 IC 值分别为 16.19±1.35 和 17.16±1.54μM，与标准药物阿霉素相比。
