Journal
MEDCHEMCOMM
Volume 2, Issue 10, Pages 977-981Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c1md00137j
Keywords
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Funding
- Cancer Therapeutics CRC under Australian Government
- NHMRC IRIISS [361646]
- Victorian State Government
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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.
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