146621-94-5Relevant articles and documents
Pro-Soft Val-boroPro: A strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases
Poplawski, Sarah E.,Lai, Jack H.,Sanford, David G.,Sudmeier, James L.,Wu, Wengen,Bachovchin, William W.
, p. 2022 - 2028 (2011)
Val-boroPro, 1, is a potent, but relatively nonspecific inhibitor of the prolyl peptidases. It has antihyperglycemic activity from inhibition of DPPIV but also striking anticancer activity and a toxicity for which the mechanisms are unknown. 1 cyclizes at
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position
Tucker, Thomas J.,Brady, Stephen F.,Lumma, William C.,Lewis, S. Dale,Gardell, Stephen J.,Naylor-Olsen, Adel M.,Yan, Youwei,Sisko, Jack T.,Stauffer, Kenneth J.,Lucas, Bobby J.,Lynch, Joseph J.,Cook, Jacquelynn J.,Stranieri, Maria T.,Holahan, Marie A.,Lyle, Elizabeth A.,Baskin, Elizabeth P.,Chen, I.-Wu,Dancheck, Kimberly B.,Krueger, Julie A.,Cooper, Carolyn M.,Vacca, Joseph P.
, p. 3210 - 3219 (2007/10/03)
As part of an ongoing effort to prepare therapeutically useful orally active thrombin inhibitors, we have synthesized a series of compounds that utilize nonbasic groups in the P1 position. The work is based on our previously reported lead structure, compo