Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors

Bioorg Med Chem Lett. 2019 Jul 1;29(13):1605-1608. doi: 10.1016/j.bmcl.2019.04.047.

Aixin Geng ¹, Hao Cui ¹, Liyuan Zhang ¹, Xin Chen ², Hongmei Li ¹, Tao Lu ³, Yong Zhu ⁴

Affiliations

1 Department of Organic Chemistry, School of Science, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China.
2 Department of Organic Chemistry, School of Science, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China; Shanxi Key Laboratory of Natural Products & Chemical Biology, College of Science, Northwest A&F University, Yangling 712100, China.
3 Laboratory of Molecular Design and Drug Discovery, School of Science, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China; State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China. Electronic address: lutao@cpu.edu.cn.
4 Department of Organic Chemistry, School of Science, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China. Electronic address: zhuyong@cpu.edu.cn.

PMID: 31053508 DOI: 10.1016/j.bmcl.2019.04.047

Abstract

Histone deacetylase (HDAC) inhibitors as an important epigenetic therapeutic strategy affect signaling networks and act synergistically with kinase inhibitors for the treatment of Cancer. Herein we presented a series of novel phenoxybenzamide analogues with inhibition of Raf and HDAC. Among them, compound 10e showed potent antiproliferative activities against Hepg2 and MDA-MB-468 in cellular assays. This work may lay the foundation for developing novel dual Raf/HDAC inhibitors as potential Anticancer therapeutics.

Keywords

Antiproliferative activity; Dual inhibitor; HDAC; Phenoxybenzamide; Raf.

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