Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369154 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
A structure–activity relationship of the 3- and 6-positions of the pyrazolo[1,5-a]pyrimidine scaffold of the known BMP inhibitors dorsomorphin, 1, LDN-193189, 2, and DMH1, 3, led to the identification of a potent and selective compound for ALK2 versus ALK3. The potency contributions of several 3-position substituents were evaluated with subtle structural changes leading to significant changes in potency. From these studies, a novel 5-quinoline molecule was identified and designated an MLPCN probe molecule, ML347, which shows >300-fold selectivity for ALK2 and presents the community with a selective molecular probe for further biological evaluation.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Darren W. Engers, Audrey Y. Frist, Craig W. Lindsley, Charles C. Hong, Corey R. Hopkins,