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Small molecules that allosterically inhibit p21-activated kinase activity by binding to the regulatory p21-binding domain
p21-activated kinases (PAKs) are key regulators of actin dynamics, cell proliferation and cell survival. Deregulation of PAK activity contributes to the pathogenesis of various human diseases,Expand
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Identification of osteogenic purmorphamine derivatives.
During embryonic and cancer development, the Hedgehog family of proteins, including Sonic Hedgehog, play an important role by relieving the inhibition of Smo by Ptc, thus activating the Smo signalingExpand
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PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IκB kinase β (IKK-β)
Abstract Ertiprotafib was developed as an inhibitor of PTP1B for the treatment of type 2 diabetes. It normalized the plasma glucose and insulin levels in diabetic animal models, and progressed to aExpand
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Discovery of a novel protein tyrosine phosphatase-1B inhibitor, KR61639: potential development as an antihyperglycemic agent.
Protein tyrosine phosphatase-1B (PTP-1B), a negative regulator of insulin signaling, may be an attractive therapeutic target for type 2 diabetes mellitus. High throughput screening (HTS) for PTP-1BExpand
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Palladium-catalyzed functionalization of 5- and 7-azaindoles
Abstract Palladium-catalyzed functionalization at the 2-position of various 5- and 7-azaindoles was performed by Suzuki, Heck, and Stille reactions. The 2-substituted azaindoles were obtained with 5%Expand
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Synthesis of 1,2,3-trisubstituted pyrrolo[3,2-c]quinolines via palladium-catalyzed heteroannulation with internal alkynes
Abstract Various 1,2,3-trisubstituted pyrrolo[3,2- c ]quinolines were synthesized by palladium-catalyzed heteroannulation of 4-amino-3-iodoquinoline derivatives and internal alkynes. TheExpand
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Xanthene Derivatives Increase Glucose Utilization through Activation of LKB1-Dependent AMP-Activated Protein Kinase
5′ AMP-activated protein kinase (AMPK) is a highly conserved serine-threonine kinase that regulates energy expenditure by activating catabolic metabolism and suppressing anabolic pathways to increaseExpand
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Scandium(III) triflate–TMSCl promoted cyclization of aziridin-1-yl oximes to 5,6-dihydro-4H-[1,2,4]oxadiazines
Abstract A convenient and facile one-pot synthesis of 5,6-dihydro-4 H -[1,2,4]oxadiazine is described. Treatment of aziridin-1-yl-oximes with Scandium(III) triflate readily afforded 5,6-dihydro-4 HExpand
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Protein Tyrosine Phosphatase 1B Inhibitors: Heterocyclic Carboxylic Acids
Several series of compounds (benzoic acids, pyrazolecarboxylic acids, phenoxyacetic acids, and quinolinoxyacetic acids) were prepared and evaluated for their inhibitory activity against PTP-1B.Expand
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Regio- and stereoselective ring opening of vinyl epoxides with MgBr2
Abstract The regio- and stereoselective ring opening of vinyl epoxides has been achieved by the use of Lewis acid, MgBr 2 , affording bromohydrins in excellent yield, which are readily transformed toExpand
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