Potent and selective [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines as retinoic acid metabolic blocking agents (RAMBAs)

Mark J Mulvihill; Julie L C Kan; Patricia Beck; Mark Bittner; Cara Cesario; Andrew Cooke; David M Keane; Anthony I Nigro; Christy Nillson; Vanessa Smith; Mary Srebernak; Feng-Lei Sun; Michael Vrkljan; Shannon L Winski; Arlindo L Castelhano; David Emerson; Neil Gibson

doi:10.1016/j.bmcl.2005.01.044

Potent and selective [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines as retinoic acid metabolic blocking agents (RAMBAs)

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1669-73. doi: 10.1016/j.bmcl.2005.01.044.

Authors

Mark J Mulvihill¹, Julie L C Kan, Patricia Beck, Mark Bittner, Cara Cesario, Andrew Cooke, David M Keane, Anthony I Nigro, Christy Nillson, Vanessa Smith, Mary Srebernak, Feng-Lei Sun, Michael Vrkljan, Shannon L Winski, Arlindo L Castelhano, David Emerson, Neil Gibson

Affiliation

¹ OSI Pharmaceuticals, Inc., 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. mark.mulvihill@osip.com

PMID: 15745819
DOI: 10.1016/j.bmcl.2005.01.044

Abstract

A series of [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines were designed and synthesized as CYP26 inhibitors, serving as retinoic acid metabolic blocking agents (RAMBA's).

MeSH terms

Animals
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Cell Line, Tumor
Cytochrome P-450 Enzyme Inhibitors*
Cytochrome P-450 Enzyme System
Dimethylamines / chemical synthesis
Dimethylamines / chemistry*
Dimethylamines / pharmacology*
Humans
Imidazoles / chemical synthesis
Imidazoles / chemistry*
Imidazoles / pharmacology*
Male
Microsomes / enzymology
Rats
Retinoic Acid 4-Hydroxylase

Substances

Antineoplastic Agents
Cytochrome P-450 Enzyme Inhibitors
Dimethylamines
Imidazoles
Cytochrome P-450 Enzyme System
Retinoic Acid 4-Hydroxylase