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Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.

Abstract：

:We report the discovery of the pyrimido-diazepine scaffolds as novel adenine mimics. Structure-based design led to the discovery of analogs with potent inhibitory activity against receptor tyrosine kinases, such as KDR, Flt3 and c-Kit. Compound 14 exhibited low nanomolar KDR enzymatic and cellular potencies (IC(50)=9 and 52 nM, respectively).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gracias V,Ji Z,Akritopoulou-Zanze I,Abad-Zapatero C,Huth JR,Song D,Hajduk PJ,Johnson EF,Glaser KB,Marcotte PA,Pease L,Soni NB,Stewart KD,Davidsen SK,Michaelides MR,Djuric SW

doi

10.1016/j.bmcl.2008.03.021

subject

Has Abstract

pub_date

2008-04-15 00:00:00

pages

2691-5

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)00296-5

journal_volume

18

pub_type

杂志文章

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