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Memphis, TN, United States

Mayasundari A.,Medicinal Chemistry Center | Fujii N.,Medicinal Chemistry Center
Tetrahedron Letters | Year: 2010

A concise synthesis of 4,6-disubstituted pyrrolo[2,3-d]pyrimidines is described. The key step involves the formation of an ether or thioether linkage along with concurrent ring closure in one-pot to yield the desired product in only two steps from a common intermediate. The reaction is chemoselective to incorporate phenol, thiophenol, and thiol. This method enabled efficient production of TWS119, a glycogen synthase kinase-3β inhibitor. © 2010 Elsevier Ltd. All rights reserved. Source


Actis M.,Medicinal Chemistry Center | Actis M.,St Jude Childrens Research Hospital | Connelly M.C.,St Jude Childrens Research Hospital | Mayasundari A.,Medicinal Chemistry Center | And 4 more authors.
Biopolymers | Year: 2011

We have previously reported ketoprofen amide compounds as inhibitors of GLI1-mediated transcription, an essential down-stream element of the Hedgehog (Hh) pathway. These compounds inhibited Gli-luciferase reporter in C3H10T1/2 cells that were exogenously transfected with GLI1 and in Rh30 cells that endogenously overexpress GLI1. Here we have designed new derivatives of these compounds aiming to explore the structure-activation relationship (SAR). By replacing the ketone carbonyl group of the ketoprofen moiety with an ether, amide, sulfonamide, or sulfone, we found several new compounds that are equipotent to the ketoprofen amide compounds. Among them, sulfone 30 inhibited Gli-luciferase reporter in C3H10T1/2 cells that were exogenously transfected with GLI1 and in Rh30 cells that endogenously overexpress GLI1. © 2010 Wiley Periodicals, Inc. Biopolymers 95: 24-30, 2011. Source

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