Research Publications

Back

Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors


Sleebs, BE; Ganame, D; Levit, A; Street, IP; Gregg, A; Falk, H; Baell, JB
2011-10
MEDCHEMCOMM
Journal Article
2
10
982-986
7-Phenyl-4-aminobenzothieno[3,2-d]pyrimidines were previously reported to exhibit moderate LIMK1 inhibition. Further exploration of SAR around the 7-phenyl moiety has led to the development of a lead series with an increased potency for LIMK1. Evaluation of physicochemical and ADME properties, and off-target kinase screens has seen this novel series emerge as a promising platform for a set of tool compounds for evaluating LIMK as a therapeutic target.
ROYAL SOC CHEMISTRY
KINASES
10.1039/c1md00138h
Refer to copyright notice on published article.

Back
Creation Date 2011-10-01 12:00:00