Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors
- Author(s)
- Sleebs, BE; Ganame, D; Levit, A; Street, IP; Gregg, A; Falk, H; Baell, JB;
- Details
- Publication Year 2011-10,Volume 2,Issue #10,Page 982-986
- Journal Title
- MEDCHEMCOMM
- Publication Type
- Journal Article
- Abstract
- 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.
- Publisher
- ROYAL SOC CHEMISTRY
- Keywords
- KINASES
- Publisher's Version
- https://doi.org/10.1039/c1md00138h
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2011-10-01 12:00:00