The discovery of novel N-(2-pyrimidinylamino) benzamide derivatives as potent hedgehog signaling pathway inhibitors

Minhang Xin; Jun Wen; Feng Tang; Chongxing Tu; Han Shen; Xinge Zhao

doi:10.1016/j.bmcl.2013.10.022

The discovery of novel N-(2-pyrimidinylamino) benzamide derivatives as potent hedgehog signaling pathway inhibitors

Minhang Xin
, Jun Wen
, Feng Tang
, Chongxing Tu
, Han Shen
, Xinge Zhao

Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research

科研成果: 期刊稿件 › 文章 › 同行评审

31 引用（Scopus）

摘要

Hedgehog signaling pathway inhibitors are emerging as new therapeutic intervention against cancer. A novel series of N-(2-pyrimidinylamino) benzamide derivatives as hedgehog signaling pathway inhibitors were designed and synthesized. Most compounds presented significant inhibitory effect on hedgehog signaling pathway, among which 21 compounds exhibited more potent than vismodegib. Furthermore, compound 6a showed moderate pharmacokinetic properties in vivo, representing a promising lead compound for further exploration.

源语言	英语
页（从-至）	6777-6783
页数	7
期刊	Bioorganic and Medicinal Chemistry Letters
卷	23
期	24
DOI	https://doi.org/10.1016/j.bmcl.2013.10.022
出版状态	已出版 - 15 12月 2013
已对外发布	是

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title = "The discovery of novel N-(2-pyrimidinylamino) benzamide derivatives as potent hedgehog signaling pathway inhibitors",

abstract = "Hedgehog signaling pathway inhibitors are emerging as new therapeutic intervention against cancer. A novel series of N-(2-pyrimidinylamino) benzamide derivatives as hedgehog signaling pathway inhibitors were designed and synthesized. Most compounds presented significant inhibitory effect on hedgehog signaling pathway, among which 21 compounds exhibited more potent than vismodegib. Furthermore, compound 6a showed moderate pharmacokinetic properties in vivo, representing a promising lead compound for further exploration.",

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author = "Minhang Xin and Jun Wen and Feng Tang and Chongxing Tu and Han Shen and Xinge Zhao",

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AU - Xin, Minhang

AU - Wen, Jun

AU - Tang, Feng

AU - Tu, Chongxing

AU - Shen, Han

AU - Zhao, Xinge

PY - 2013/12/15

Y1 - 2013/12/15

N2 - Hedgehog signaling pathway inhibitors are emerging as new therapeutic intervention against cancer. A novel series of N-(2-pyrimidinylamino) benzamide derivatives as hedgehog signaling pathway inhibitors were designed and synthesized. Most compounds presented significant inhibitory effect on hedgehog signaling pathway, among which 21 compounds exhibited more potent than vismodegib. Furthermore, compound 6a showed moderate pharmacokinetic properties in vivo, representing a promising lead compound for further exploration.

AB - Hedgehog signaling pathway inhibitors are emerging as new therapeutic intervention against cancer. A novel series of N-(2-pyrimidinylamino) benzamide derivatives as hedgehog signaling pathway inhibitors were designed and synthesized. Most compounds presented significant inhibitory effect on hedgehog signaling pathway, among which 21 compounds exhibited more potent than vismodegib. Furthermore, compound 6a showed moderate pharmacokinetic properties in vivo, representing a promising lead compound for further exploration.

KW - Hedgehog signaling

KW - Hedgehog signaling pathway inhibitors

KW - Lead compound

KW - Synthesize

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 24

ER -

The discovery of novel N-(2-pyrimidinylamino) benzamide derivatives as potent hedgehog signaling pathway inhibitors

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