Structural modifications of 6-naphthalene-2-carboxylate retinoids

KL Yu, J Ostrowski, S Chen, KM Tramposch…

Index: Yu, Kuo-Long; Ostrowski, Jacek; Chen, Simon; Tramposch, Kenneth M.; Reczek, Peter R.; Mansuri, Muzammil M.; Starrett Jr., John E. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 23 p. 2865 - 2870

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Citation Number: 6

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.