Synthesis and evaluation of 4-(2-pyrimidinylamino) benzamides inhibitors of hedgehog signaling pathway

Minhang Xin; Jun Wen; Feng Tang; Chongxing Tu; Wei Huang; Han Shen; Xinge Zhao; Lingfei Cheng; Mengyu Wang; Liandi Zhang

doi:10.1016/j.bmcl.2013.12.050

Synthesis and evaluation of 4-(2-pyrimidinylamino) benzamides inhibitors of hedgehog signaling pathway

Minhang Xin
, Jun Wen
, Feng Tang
, Chongxing Tu
, Wei Huang
, Han Shen
, Xinge Zhao
, Lingfei Cheng
, Mengyu Wang
, Liandi Zhang

医学部

Jiangsu Simcere Pharmaceutical Co. Ltd

科研成果: 期刊稿件 › 文章 › 同行评审

20 引用（Scopus）

摘要

A novel series of hedgehog signaling pathway inhibitors has been designed based on the 4-(2-pyrimidinylamino) benzamides scaffold. The synthesis and SAR of these compounds are described. Optimization leads to the identification of compound 3c, a potent and orally available agent with improved physicochemical and pharmacokinetic properties.

源语言	英语
页（从-至）	983-988
页数	6
期刊	Bioorganic and Medicinal Chemistry Letters
卷	24
期	3
DOI	https://doi.org/10.1016/j.bmcl.2013.12.050
出版状态	已出版 - 1 2月 2014

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10.1016/j.bmcl.2013.12.050

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abstract = "A novel series of hedgehog signaling pathway inhibitors has been designed based on the 4-(2-pyrimidinylamino) benzamides scaffold. The synthesis and SAR of these compounds are described. Optimization leads to the identification of compound 3c, a potent and orally available agent with improved physicochemical and pharmacokinetic properties.",

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AU - Xin, Minhang

AU - Wen, Jun

AU - Tang, Feng

AU - Tu, Chongxing

AU - Huang, Wei

AU - Shen, Han

AU - Zhao, Xinge

AU - Cheng, Lingfei

AU - Wang, Mengyu

AU - Zhang, Liandi

PY - 2014/2/1

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N2 - A novel series of hedgehog signaling pathway inhibitors has been designed based on the 4-(2-pyrimidinylamino) benzamides scaffold. The synthesis and SAR of these compounds are described. Optimization leads to the identification of compound 3c, a potent and orally available agent with improved physicochemical and pharmacokinetic properties.

AB - A novel series of hedgehog signaling pathway inhibitors has been designed based on the 4-(2-pyrimidinylamino) benzamides scaffold. The synthesis and SAR of these compounds are described. Optimization leads to the identification of compound 3c, a potent and orally available agent with improved physicochemical and pharmacokinetic properties.

KW - Hedgehog signaling pathway

KW - Inhibitors

KW - Pharmacokinetic properties

KW - SAR

UR - https://www.scopus.com/pages/publications/84893650738

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DO - 10.1016/j.bmcl.2013.12.050

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ER -

Synthesis and evaluation of 4-(2-pyrimidinylamino) benzamides inhibitors of hedgehog signaling pathway

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