213013-98-0Relevant academic research and scientific papers
Structure-based design of TACE selective inhibitors: Manipulations in the S1′-S3′ pocket
Huang, Adrian,Joseph-McCarthy, Diane,Lovering, Frank,Sun, Linhong,Wang, Weiheng,Xu, Weixin,Zhu, Yi,Cui, Junqing,Zhang, Yuhua,Levin, Jeremy I.
, p. 6170 - 6181 (2008/03/27)
A series of β-sulfonyl hydroxamate TACE inhibitors, bearing a butynylamino or a butynyloxy P1′ group, was designed and synthesized. Of the compounds investigated, 22 has excellent potency against isolated TACE enzyme, shows good selectivity over MMP-2 and
Identification of potent and selective TACE inhibitors via the S1 pocket
Condon, Jeffrey S.,Joseph-McCarthy, Diane,Levin, Jeremy I.,Lombart, Henry-Georges,Lovering, Frank E.,Sun, Linhong,Wang, Weiheng,Xu, Weixin,Zhang, Yuhua
, p. 34 - 39 (2007/10/03)
By focusing on the P1 portion of the piperidine β-sulfone ligands we identified a motif that induces selectivity and resulted in a series of TACE inhibitors that demonstrated excellent in vitro potency against isolated TACE enzyme and excellent selectivity over MMPs 1, 2, 9, 13, and 14.
Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors
Lombart, Henry-Georges,Feyfant, Eric,Joseph-McCarthy, Diane,Huang, Adrian,Lovering, Frank,Sun, LinHong,Zhu, Yi,Zeng, Congmei,Zhang, Yuhua,Levin, Jeremy
, p. 4333 - 4337 (2008/02/11)
Structure-based methods were used to design β-sulfone 3,3-piperidine hydroxamates as TACE inhibitors with the aim of improving selectivity for TACE versus MMP-13. Several compounds in this series were synthesized and evaluated in enzymatic and cell-based
Design and synthesis of butynyloxyphenyl β-sulfone piperidine hydroxamates as TACE inhibitors
Park, Kaapjoo,Aplasca, Alexis,Du, Mila T.,Sun, LinHong,Zhu, Yi,Zhang, Yuhua,Levin, Jeremy I.
, p. 3927 - 3931 (2007/10/03)
A series of butynyloxyphenyl β-sulfone piperidine hydroxamate TACE inhibitors was designed and synthesized. The resulting structure-activity relationship and MMP selectivity of the series were examined. Of the compounds investigated, 17s has excellent in
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
ALKYNYL CONTAINING HYDROXAMIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MATRIX METALLOPROTEINASE (MMP) INHIBITORS / TNF-ALPHA CONVERTING ENZYME (TACE) INHIBITORS
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Page/Page column 41, (2010/02/14)
Compounds of the formula:useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring
Ueno, Hiroshi,Yokota, Katsuyuki,Hoshi, Jun-Ichi,Yasue, Katsutaka,Hayashi, Mikio,Hase, Yasunori,Uchida, Itsuo,Aisaka, Kazuo,Katoh, Susumu,Cho, Hidetsura
, p. 3586 - 3604 (2007/10/03)
A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine
Amidine compounds
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, (2008/06/13)
A compound of the formula [I] wherein R1, R2and R3are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. The compound of the presen
Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase/tace inhibitors
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, (2008/06/13)
Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
