226396-64-1Relevant academic research and scientific papers
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
CARBORANE HYDROXAMIC ACID MATRIX METALLOPROTEINASE INHIBITORS AND AGENTS FOR BORON NEUTRON CAPTURE THERAPY
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Paragraph 0066; 00118, (2020/01/24)
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
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.
Synthesis and structure-activity relationships of β- and α-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy
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)
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
