Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases

被引：5

作者：

Donald, Alastair D. G. ^{[1
]}

Clark, Vanessa L. ^{[1
]}

Patel, Sanjay ^{[1
]}

Day, Francesca A. ^{[1
]}

Rowlands, Martin G. ^{[2
]}

Wibata, Judata ^{[2
]}

Stimson, Lindsay ^{[2
]}

Hardcastle, Anthea ^{[2
]}

Eccles, Sue A. ^{[2
]}

McNamara, Deborah ^{[1
]}

Needham, Lindsey A. ^{[1
]}

Raynaud, Florence I. ^{[2
]}

Aherne, Wynne ^{[2
]}

Moffat, David F. ^{[1
]}

机构：

[1] Chroma Therapeut, Abingdon OX14 4RY, Oxon, England

[2] Inst Canc Res, Canc Res UK Canc Therapeut Unit, Surrey SM2 5NG, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 22期

关键词：

HDAC; Cancer; Optimisation; PROMISE;

D O I：

10.1016/j.bmcl.2010.09.016

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibition of histone deacetylase activity represents a promising new modality in the treatment of a number of cancers. A novel HDAC series demonstrating inhibitory activity in cell proliferation assays is described. Optimisation based on the introduction of basic amine linkers to effect good drug distribution to tumour led to the identification of a compound with oral activity in a human colon cancer xenograft study associated with increased histone H3 acetylation in tumour tissue. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：6657 / 6660

页数：4

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