123803-51-0Relevant articles and documents
Inhibition of invasion and capillary-like tube formation by retrohydroxamate-based MMP inhibitors
Choi, Seung-Su,Ji, Ae-Ri,Yu, Seung-Woo,Cho, Bong-Hwan,Park, Jung Dae,Park, Jun Hyoung,Lee, Hyun Soo,Ryu, Seong Eon,Kim, Dong Han,Kang, Jae-Hoon,Lee, Seung-Taek
experimental part, p. 2032 - 2038 (2012/01/14)
Matrix metalloproteinases (MMPs), a family of zinc-containing endopeptidases, participate in many normal processes such as embryonic development and wound repair, and in many pathological situations such as cancer, atherosclerosis, and arthritis. Peptidomimetic MMP inhibitors were designed and synthesized with Nformylhydroxylamine (retrohydroxamate) as a zinc-binding group and various side chains on the α, P1′, and P2′ positions. Using in vitro MMP assays with purified MMPs (MMP-1, MMP-2, MMP-3, MMP-9, and MMP-14) and fluorogenic peptide substrates, it was found that compounds 2d and 2g selectively inhibit gelatinases (MMP-2 and MMP-9) and interstitial collagenase (MMP-1). They also inhibited the chemo-invasion of fibrosarcoma HT-1080 cells and tube formation of human umbilical vascular endothelial cells in a dosedependent manner. Our results suggest that retrohydroxamate-based MMP inhibitors, especially compounds 2d and 2g, have the potential to be used as therapeutic drugs for cancer and other MMP-related diseases.
Design, asymmetric synthesis, and evaluation of pseudosymmetric sulfoximine inhibitors against HIV-1 protease
Lu, Ding,Sham, Yuk Yin,Vince, Robert
experimental part, p. 2037 - 2048 (2010/06/12)
The HIV-1 protease is a validated drug target for the design of antiretroviral drugs to combat AIDS. We previously established the sulfoximine functionality as a valid transition state mimetic (TSM) in the HIV-1 protease inhibitors (PI) design and have id
A practical method for the conversion of β-hydroxy carboxylic acids into the corresponding β-amino acids
Jin, Yonghao,Kim, Dong H.
, p. 1189 - 1190 (2007/10/03)
Optically active α- or β-substituted βamino acids were synthesized from the corresponding β-hydroxy acids in 4 steps in excellent yield. Stereochemistry was retained at the α-position and reversed at the β-position during the conversion.
N-substituted acylamino acid compounds, process for their production and their use
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, (2008/06/13)
The present invention provides an N-substituted acylamino acid compound of the formula: STR1 a process for their production and pharmaceutical uses, and intermediates useful for their production.
N-ACYLAMINO ACID DERIVATIVES AND THEIR PHARMACEUTICAL COMPOSITIONS
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, (2008/06/13)
An N-acylamino acid derivative of the formula: STR1 wherein the substituents are herein defined or a salt thereof, which is useful as hypotensive drugs.