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Design, synthesis and anticancer activities evaluation of novel 5H-dibenzo[b,e]azepine-6,11-dione derivatives containing 1,3,4-oxadiazole units
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-02-08 , DOI: 10.1016/j.bmcl.2018.02.008
Xin He , Xin-yang Li , Jing-wei Liang , Chong Cao , Shuai Li , Ting-jian Zhang , Fan-hao Meng

Rucaparib and PJ34 were used as the structural model for the design of novel 5H-dibenzo[b,e]azepine-6,11-dione derivatives containing 1,3,4-oxadiazole units. And target compounds were successfully synthesized through a 3-step synthetic strategy. All target compounds were screened for their anti-proliferative effects against OVCAR-3 cell line. Preliminary biological study of these compounds provided potent compounds d21 and d22 with better activities than Rucaparib.



中文翻译:

新型含1,3,4-恶二唑单元的5 H-二苯并[ be ]氮杂6,11-二酮衍生物的设计,合成和抗癌活性评估

Rucaparib和PJ34被用作结构模型,用于设计含有1,3,4-恶二唑单元的新型5 H-二苯并[ be ]氮杂6,11-二酮衍生物。通过三步合成策略成功合成了目标化合物。筛选所有目标化合物针对OVCAR-3细胞系的抗增殖作用。对这些化合物的初步生物学研究提供了比rucaparib更好的活性化合物d21d22

更新日期:2018-02-08
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