Structure–activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors

…, CS Lai, DY Deng, C Sachidanandan, KD Bloch…

Index: Cuny, Gregory D.; Yu, Paul B.; Laha, Joydev K.; Xing, Xuechao; Liu, Ji-Feng; Lai, Carol S.; Deng, Donna Y.; Sachidanandan, Chetana; Bloch, Kenneth D.; Peterson, Randall T. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 15 p. 4388 - 4392

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Citation Number: 173

Abstract

A structure–activity relationship study of dorsomorphin, a previously identified inhibitor of SMAD 1/5/8 phosphorylation by bone morphogenetic protein (BMP) type 1 receptors ALK2, 3, and 6, revealed that increased inhibitory activity could be accomplished by replacing the pendent 4-pyridine ring with 4-quinoline. The activity contributions of various nitrogen atoms in the core pyrazolo [1, 5-a] pyrimidine ring were also examined by preparing and ...