Journal of medicinal and pharmaceutical chemistry 2014-03-27

Cathepsin C inhibitors: property optimization and identification of a clinical candidate.

Mark Furber, Anna-Karin Tiden, Philip Gardiner, Antonio Mete, Rhonan Ford, Ian Millichip, Linda Stein, Andrew Mather, Elizabeth Kinchin, Christopher Luckhurst, Simon Barber, Peter Cage, Hitesh Sanganee, Rupert Austin, Kamaldeep Chohan, Raj Beri, Bob Thong, Alan Wallace, Victor Oreffo, Ray Hutchinson, Steve Harper, Judit Debreczeni, Jason Breed, Lisa Wissler, Karl Edman

Index: J. Med. Chem. 57(6) , 2357-67, (2014)

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Abstract

A lead generation and optimization program delivered the highly selective and potent CatC inhibitor 10 as an in vivo tool compound and potential development candidate. Structural studies were undertaken to generate SAR understanding.