DNA依赖性蛋白激酶（DNA-PK）的8-二芳基色原酮-4-酮抑制剂。

8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).

作者信息

Desage-El Murr Marine, Cano Celine, Golding Bernard T, Hardcastle Ian R, Hummersome Marc, Frigerio Mark, Curtin Nicola J, Menear Keith, Richardson Caroline, Smith Graeme C M, Griffin Roger J

机构信息

Northern Institute for Cancer Research, School of Natural Sciences-Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne NE1 7RU, UK.

出版信息

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4885-90. doi: 10.1016/j.bmcl.2008.07.066. Epub 2008 Jul 20.

DOI:10.1016/j.bmcl.2008.07.066

PMID:18678488

Abstract

The synthesis and biological evaluation of libraries of 8-biarylchromen-4-ones enabled the elucidation of structure-activity relationships for inhibition of the DNA-dependent protein kinase (DNA-PK), with 8-(3-(thiophen-2-yl)phenyl)chromen-4-one and 8-(3-(thiophen-3-yl)phenyl)chromen-4-one being especially potent inhibitors.

摘要

8-联芳基色原酮库的合成及生物学评价有助于阐明抑制DNA依赖性蛋白激酶（DNA-PK）的构效关系，其中8-(3-(噻吩-2-基)苯基)色原酮-4-酮和8-(3-(噻吩-3-基)苯基)色原酮-4-酮是特别有效的抑制剂。