Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors
- Author(s)
- Sleebs, BE; Levit, A; Street, IP; Falk, H; Hammonds, T; Wong, AC; Charles, MD; Olson, MF; Baell, JB;
- Details
- Publication Year 2011-10,Volume 2,Issue #10,Page 977-981
- Journal Title
- MEDCHEMCOMM
- Publication Type
- Journal Article
- Abstract
- A high throughput chemical screening campaign has led to the identification of 3-aminobenzo[b]thiophene-2-carboxamides as LIMK I inhibitors. Evolution of bicyclic hits to the tricyclic 4-aminobenzothieno[3,2-d]pyrimidine, using a traditional medicinal chemistry SAR guided approach, resulted in a significant increase in potency. Further elaboration has seen the 7-phenyl-4-aminobenzothieno[3,2-d]pyrimidine emerge as a LIMK I inhibitor lead candidate.
- Publisher
- ROYAL SOC CHEMISTRY
- Keywords
- ACTIN DYNAMICS; KINASE
- Publisher's Version
- https://doi.org/10.1039/c1md00137j
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2011-10-01 12:00:00