Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2669-73. doi: 10.1016/j.bmcl.2014.04.061.

Jianyang Chen ¹, Haixia Peng ¹, Jinxue He ², Xiajuan Huan ², Zehong Miao ³, Chunhao Yang ⁴

Affiliations

1 Department of Medicinal Chemistry, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China.
2 Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China.
3 Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China. Electronic address: zhmiao@simm.ac.cn.
4 Department of Medicinal Chemistry, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China. Electronic address: chyang@simm.ac.cn.

PMID: 24815508 DOI: 10.1016/j.bmcl.2014.04.061

Abstract

The isoquinolinone-based tricyclic compounds were designed and synthesized. Preliminary biological study of these compounds provided potent compounds 17a, 33b, 33c, 33d, and 33g with low nanomolar IC50s against PARP-1 Enzyme.

Keywords

Antitumor; Isoquinolinone-based tricycles; PARP-1 inhibitors.

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