STRUCTURAL MODIFICATIONS OF 6-NAPHTHALENE-2-CARBOXYLATE RETINOIDS

Authors
YU KL OSTROWSKI J CHEN S TRAMPOSCH KM RECZEK PR MANSURI MM STARRETT JE
Citation
Kl. Yu et al., STRUCTURAL MODIFICATIONS OF 6-NAPHTHALENE-2-CARBOXYLATE RETINOIDS, Bioorganic & medicinal chemistry letters, 6(23), 1996, pp. 2865-2870
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
23
Year of publication
1996
Pages
2865 - 2870
Database
ISI
SICI code
0960-894X(1996)6:23<2865:SMO6R>2.0.ZU;2-0
Abstract
The keto linker of 2-naphthoate retinoid 1 has been found nonessential for RAR transactivation activity and can be replaced with heteroatoms such as S, O, N without significant reduction of the activity. On the other hand, substitutions on the aromatic rings of retinoids 1 and 2 resulted in analogs with reduced potentcy and RAR selectivity. Copyrig ht (C) 1996 Elsevier Science Ltd