Syntheses and evaluation of naphthalenyl- and chromenyl-pyrrolyl-benzoic acids as potent and selective retinoic acid receptor α agonists

Synthesis and structure activity relationships (SAR) of RAR alpha-selective agonists are discussed. 4-[5-(5,8-Dimethyl-2H-3-chromenyl)-1H-2-pyrrolyl]benzoic acid (12a), which possesses a flat structural moiety and an oxygen atom at the hydrophobic part, showed highly selective transactivation activi...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-04, Vol.10 (7), p.623-625
Main Authors: HIBI, S, TAGAMI, K, KIKUCHI, K, YOSHIMURA, H, TAI, K, HIDA, T, TOKUHARA, N, YAMAUCHI, T, NAGAI, M
Format: Article
Language:English
Subjects:
Antineoplastic agents
Benzoates - chemical synthesis
Benzoates - pharmacology
Benzopyrans - chemical synthesis
Benzopyrans - pharmacology
Biological and medical sciences
Cell Differentiation - drug effects
General aspects
HL-60 Cells
Humans
Medical sciences
Naphthalenes - chemical synthesis
Naphthalenes - pharmacology
Pharmacology. Drug treatments
Pyrroles - chemical synthesis
Pyrroles - pharmacology
Receptors, Retinoic Acid - agonists
Retinoic Acid Receptor alpha
Structure-Activity Relationship
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Summary:Synthesis and structure activity relationships (SAR) of RAR alpha-selective agonists are discussed. 4-[5-(5,8-Dimethyl-2H-3-chromenyl)-1H-2-pyrrolyl]benzoic acid (12a), which possesses a flat structural moiety and an oxygen atom at the hydrophobic part, showed highly selective transactivation activity at the RAR alpha receptor.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00067-6