- Carborane-Containing Matrix Metalloprotease (MMP) Ligands as Candidates for Boron Neutron-Capture Therapy (BNCT)
-
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
- Lutz, Marlon R.,Flieger, Sebastian,Colorina, Andre,Wozny, John,Hosmane, Narayan S.,Becker, Daniel P.
-
p. 1897 - 1908
(2020/09/01)
-
- CARBORANE HYDROXAMIC ACID MATRIX METALLOPROTEINASE INHIBITORS AND AGENTS FOR BORON NEUTRON CAPTURE THERAPY
-
Disclosed herein are novel carborane hydroxamic acid matrix metalloproteinase ("MMP") inhibitors and agents bearing borane-containing moieties and methods for their use in treating or preventing a disease, such as cancer and rheumatoid arthritis. In parti
- -
-
Paragraph 0066; 00118
(2020/01/24)
-
- Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl Sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease
-
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.
- 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)
-
- Synthesis and structure-activity relationships of β- and α-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy
-
α-Piperidine-β-sulfone hydroxamate derivatives were explored that are potent for matrix metalloproteinases (MMP)-2, -9, and -13 and are sparing of MMP-1. The investigation of the β-sulfones subsequently led to the discovery of hitherto unknown α-sulfone h
- Becker, Daniel P.,Villamil, Clara I.,Barta, Thomas E.,Bedell, Louis J.,Boehm, Terri L.,DeCrescenzo, Gary A.,Freskos, John N.,Getman, Daniel P.,Hockerman, Susan,Heintz, Robert,Howard, Susan Carol,Li, Madeleine H.,McDonald, Joseph J.,Carron, Chris P.,Funckes-Shippy, Chris L.,Mehta, Pramod P.,Munie, Grace E.,Swearingen, Craig A.
-
p. 6713 - 6730
(2007/10/03)
-