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

Bioorg Med Chem Lett

Department of Medicinal Chemistry, School of Pharmacy, China Medical University, No. 77 Puhe Road, Shenbei District, Shenyang 110122, China. Electronic address:

Published: March 2018

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.

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http://dx.doi.org/10.1016/j.bmcl.2018.02.008DOI Listing

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