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. 2018 Mar 1;28(5):847-852. doi: 10.1016/j.bmcl.2018.02.008.
Xin He  1 ,  Xin-Yang Li  1 ,  Jing-Wei Liang  1 ,  Chong Cao  1 ,  Shuai Li  1 ,  Ting-Jian Zhang  1 ,  Fan-Hao Meng  2
Affiliations
  • 1. Department of Medicinal Chemistry, School of Pharmacy, China Medical University, No. 77 Puhe Road, Shenbei District, Shenyang 110122, China.
  • 2. Department of Medicinal Chemistry, School of Pharmacy, China Medical University, No. 77 Puhe Road, Shenbei District, Shenyang 110122, China. Electronic address: [email protected].
PMID: 29456106 DOI: 10.1016/j.bmcl.2018.02.008
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.

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