Matrix metallo-proteinase (MMP-2) organoboronate inhibitors

Hijazi Abu Ali; Ronny Berkovitz; Reuven Reich; Morris Srebnik

doi:10.1002/ardp.200300827

Matrix metallo-proteinase (MMP-2) organoboronate inhibitors

Hijazi Abu Ali
, Ronny Berkovitz
, Reuven Reich
, Morris Srebnik^*

^*Corresponding author for this work

School of Pharmacy

Research output: Contribution to journal › Article › peer-review

10 Scopus citations

Abstract

Novel organoboronate derivatives consisting of BB, BC(R₁R ₂)B, BCCB, CBC, RBC=CBB, and RBC=CBP structures were synthesized and have been investigated in vitro as MMP-2 inhibitors. We discovered that most of the boronate derivatives (those not containing phosphorus) showed significant activity against MMP-2. The trisboronate 14 proved to be a potent MMP-2 inhibitor at 5 and 10 μMU. Structure-activity relationships (SARs) data for the compounds were investigated and are discussed.

Original language	English
Pages (from-to)	183-187
Number of pages	5
Journal	Archiv der Pharmazie
Volume	337
Issue number	4
DOIs	https://doi.org/10.1002/ardp.200300827
State	Published - Apr 2004

Keywords

Basement membrane invasion
Gelatinase
Matrix Metallo-proteinase
Organoboronates
Structure-activity relationships

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10.1002/ardp.200300827

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title = "Matrix metallo-proteinase (MMP-2) organoboronate inhibitors",

abstract = "Novel organoboronate derivatives consisting of BB, BC(R1R 2)B, BCCB, CBC, RBC=CBB, and RBC=CBP structures were synthesized and have been investigated in vitro as MMP-2 inhibitors. We discovered that most of the boronate derivatives (those not containing phosphorus) showed significant activity against MMP-2. The trisboronate 14 proved to be a potent MMP-2 inhibitor at 5 and 10 μMU. Structure-activity relationships (SARs) data for the compounds were investigated and are discussed.",

keywords = "Basement membrane invasion, Gelatinase, Matrix Metallo-proteinase, Organoboronates, Structure-activity relationships",

author = "Ali, \{Hijazi Abu\} and Ronny Berkovitz and Reuven Reich and Morris Srebnik",

year = "2004",

month = apr,

doi = "10.1002/ardp.200300827",

language = "אנגלית",

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AU - Ali, Hijazi Abu

AU - Berkovitz, Ronny

AU - Reich, Reuven

AU - Srebnik, Morris

PY - 2004/4

Y1 - 2004/4

N2 - Novel organoboronate derivatives consisting of BB, BC(R1R 2)B, BCCB, CBC, RBC=CBB, and RBC=CBP structures were synthesized and have been investigated in vitro as MMP-2 inhibitors. We discovered that most of the boronate derivatives (those not containing phosphorus) showed significant activity against MMP-2. The trisboronate 14 proved to be a potent MMP-2 inhibitor at 5 and 10 μMU. Structure-activity relationships (SARs) data for the compounds were investigated and are discussed.

AB - Novel organoboronate derivatives consisting of BB, BC(R1R 2)B, BCCB, CBC, RBC=CBB, and RBC=CBP structures were synthesized and have been investigated in vitro as MMP-2 inhibitors. We discovered that most of the boronate derivatives (those not containing phosphorus) showed significant activity against MMP-2. The trisboronate 14 proved to be a potent MMP-2 inhibitor at 5 and 10 μMU. Structure-activity relationships (SARs) data for the compounds were investigated and are discussed.

KW - Basement membrane invasion

KW - Gelatinase

KW - Matrix Metallo-proteinase

KW - Organoboronates

KW - Structure-activity relationships

UR - https://www.scopus.com/pages/publications/3042741361

U2 - 10.1002/ardp.200300827

DO - 10.1002/ardp.200300827

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AN - SCOPUS:3042741361

SN - 0365-6233

VL - 337

SP - 183

EP - 187

JO - Archiv der Pharmazie

JF - Archiv der Pharmazie

IS - 4

ER -

Matrix metallo-proteinase (MMP-2) organoboronate inhibitors

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Keywords

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