Journal article
Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors
BE Sleebs, A Levit, IP Street, H Falk, T Hammonds, AC Wong, MD Charles, MF Olson, JB Baell
Medchemcomm | ROYAL SOC CHEMISTRY | Published : 2011
DOI: 10.1039/c1md00137j
Abstract
A high throughput chemical screening campaign has led to the identification of 3-aminobenzo[b]thiophene-2-carboxamides as LIMK1 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 LIMK1 inhibitor lead candidate. © The Royal Society of Chemistry 2011.
Grants
Awarded by NHMRC IRIISS
Funding Acknowledgements
The authors acknowledge the financial support of the Cancer Therapeutics CRC, established and supported under the Australian Government's Cooperative Research Centres Program; NHMRC IRIISS grant number 361646 and Victorian State Government OIS grant.