Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors

Sleebs, B.E., Levit, A., Street, I.P., Falk, H., Hammonds, T., Wong, A.C., Charles, M.D., Olson, M.F. and Baell, J.B. (2011) Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors. MedChemComm, 2(10), p. 977. (doi: 10.1039/C1MD00137J)

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

• Item Type: Articles
• Status: Published
• Refereed: Yes
• Glasgow Author(s) Enlighten ID: Olson, Professor Michael
• Authors: Sleebs, B.E., Levit, A., Street, I.P., Falk, H., Hammonds, T., Wong, A.C., Charles, M.D., Olson, M.F., and Baell, J.B.
• College/School: College of Medical Veterinary and Life Sciences > School of Cancer Sciences
• Journal Name: MedChemComm
• ISSN: 2040-2503