Synthesis and biological evaluation of 2,3-diaryl isoquinolinone derivatives as anti-breast cancer agents targeting ERα and VEGFR-2

Bioorg Med Chem Lett. 2014 May 1;24(9):2129-33. doi: 10.1016/j.bmcl.2014.03.042.

Zhichao Tang ¹, Shaoxiong Niu ¹, Fei Liu ¹, Kejing Lao ¹, Jingshan Miao ², Jinzi Ji ², Xiang Wang ², Ming Yan ², Luyong Zhang ², Qidong You ¹, Hong Xiao ³, Hua Xiang ⁴

Affiliations

1 Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China.
2 New Drug Screening Center, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China.
3 Nanjing Brain Hospital Affiliated to Nanjing Medical University, 264 Guangzhou Road, Nanjing 210029, PR China. Electronic address: xiaohong63xx@163.com.
4 Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China. Electronic address: xianghua@cpu.edu.cn.

PMID: 24721727 DOI: 10.1016/j.bmcl.2014.03.042

Abstract

The Estrogen Receptor α is recognized as important pharmaceutical target for breast Cancer therapy, and vascular endothelial growth factor receptors (VEGFRs) play important roles in tumor angiogenesis including breast Cancer. A series of 2,3-diaryl isoquinolinone derivatives were designed and synthesized targeting both Estrogen Receptor α (ERα) and VEGFR-2. Bioactivity evaluation showed that compounds 7c, 7d and 7f exhibited significant anti-proliferative and anti-angiogenesis activities via ERα and VEGFR-2 dependent mechanisms.

Keywords

2,3-Diaryl isoquinolinone derivatives; Anti-breast cancer; ERα; Synthesis; VEGFR-2.

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