Literature DB >> 29456106

Design, synthesis and anticancer activities evaluation of novel 5H-dibenzo[b,e]azepine-6,11-dione derivatives containing 1,3,4-oxadiazole units.

Xin He1, Xin-Yang Li1, Jing-Wei Liang1, Chong Cao1, Shuai Li1, Ting-Jian Zhang1, Fan-Hao Meng2.   

Abstract

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.
Copyright © 2018 Elsevier Ltd. All rights reserved.

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Keywords:  5H-dibenzo[b,e]azepine-6,11-dione; Anticancer; PARP-1 inhibitors

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Year:  2018        PMID: 29456106     DOI: 10.1016/j.bmcl.2018.02.008

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Development of a novel thymidylate synthase (TS) inhibitor capable of up-regulating P53 expression and inhibiting angiogenesis in NSCLC.

Authors:  Xin-Yang Li; De-Pu Wang; Guo-Qing Lu; Kai-Li Liu; Ting-Jian Zhang; Shuai Li; Kamara Mohamed O; Wen-Han Xue; Xin-Hua Qian; Fan-Hao Meng
Journal:  J Adv Res       Date:  2020-07-25       Impact factor: 10.479

2.  Synthesis and biological evaluation of 3-(1,3,4-oxadiazol-2-yl)-1,8-naphthyridin-4(1H)-ones as cisplatin sensitizers.

Authors:  Xueyan Hou; Hao Luo; Mengqi Zhang; Guoyi Yan; Chunlan Pu; Suke Lan; Rui Li
Journal:  Medchemcomm       Date:  2018-09-25       Impact factor: 3.597

  2 in total

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