226396-64-1Relevant articles and documents
Carborane-Containing Matrix Metalloprotease (MMP) Ligands as Candidates for Boron Neutron-Capture Therapy (BNCT)
Lutz, Marlon R.,Flieger, Sebastian,Colorina, Andre,Wozny, John,Hosmane, Narayan S.,Becker, Daniel P.
, p. 1897 - 1908 (2020/09/01)
Based on the previously reported potent and selective sulfone hydroxamate inhibitors SC-76276, SC-78080 (SD-2590), and SC-77964, potent MMP inhibitors have been designed and synthesized to append a boron-rich carborane cluster by employing click chemistry
Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl Sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease
Becker, Daniel P.,Barta, Thomas E.,Bedell, Louis J.,Boehm, Terri L.,Bond, Brian R.,Carroll, Jeffery,Carron, Chris P.,Decrescenzo, Gary A.,Easton, Alan M.,Freskos, John N.,Funckes-Shippy, Chris L.,Heron, Marcia,Hockerman, Susan,Howard, Carol Pearcy,Kiefer, James R.,Li, Madeleine H.,Mathis, Karl J.,McDonald, Joseph J.,Mehta, Pramod P.,Munie, Grace E.,Sunyer, Teresa,Swearingen, Craig A.,Villamil, Clara I.,Welsch, Dean,Williams, Jennifer M.,Yu, Ying,Yao, Jun
experimental part, p. 6653 - 6680 (2010/11/18)
α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMPs-2,-9, and-13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the bovine cartilage degradation ex vivo explant system. α-Piperidine 19v (SC-78080/SD-2590) was selected for development toward the initial indication of cancer, while α-piperidine and α-tetrahydropyranyl hydroxamates 19w (SC-77964) and 9i (SC-77774), respectively, were identified as backup compounds.