Potent inhibition of retinoic acid metabolism enzyme(s) by novel azolyl retinoids

Bioorganic & Medicinal Chemistry Letters
2000.0

Abstract

Novel (+/-)-4-azolyl retinoic acid analogues 4, 5, 7 and 8 have been designed and synthesized and have been shown to be powerful inhibitors of hamster microsomal all-trans-retinoic acid 4-hydroxylase enzyme(s). (+/-)-4-(1H-Imidazol-1-yl)retinoic acid (4) is the most potent inhibitor of this enzyme reported to date.

Knowledge Graph

Similar Paper

Potent inhibition of retinoic acid metabolism enzyme(s) by novel azolyl retinoids
Bioorganic & Medicinal Chemistry Letters 2000.0
Novel Retinoic Acid Metabolism Blocking Agents Endowed with Multiple Biological Activities Are Efficient Growth Inhibitors of Human Breast and Prostate Cancer Cells in Vitro and a Human Breast Tumor Xenograft in Nude Mice
Journal of Medicinal Chemistry 2004.0
Novel Tetralone-Derived Retinoic Acid Metabolism Blocking Agents:  Synthesis and in Vitro Evaluation with Liver Microsomal and MCF-7 CYP26A1 Cell Assays
Journal of Medicinal Chemistry 2005.0
Retinoic Acid Conjugates as Potential Antitumor Agents:  Synthesis and Biological Activity of Conjugates with Ara-A, Ara-C, 3(2H)-Furanone, and Aniline Mustard Moieties
Journal of Medicinal Chemistry 1997.0
Examination of aminophenol-containing compounds designed as antiproliferative agents and potential atypical retinoids
Bioorganic & Medicinal Chemistry 2023.0
Retinobenzoic acids. 1. Structure-activity relationships of aromatic amides with retinoidal activity
Journal of Medicinal Chemistry 1988.0
Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides
Bioorganic & Medicinal Chemistry 2010.0
Synthesis, molecular modelling and CYP24A1 inhibitory activity of novel of ( E )- N -(2-(1 H -imidazol-1-yl)-2-(phenylethyl)-3/4-styrylbenzamides
Bioorganic & Medicinal Chemistry 2017.0
Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-substituted phenyl alkyl imidazole-based inhibitors of the enzyme complex 17α-hydroxylase/17,20-lyase (P45017α)
Bioorganic & Medicinal Chemistry Letters 2006.0
Preparation and pharmacological profile of 7-(α-Azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors
Bioorganic & Medicinal Chemistry Letters 2003.0