レチノイド同効物質及び拮抗物質の医薬化学

概要

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Retinoic acid acts as a specific modulator of cellular differentiation and proliferation. Its natural and synthetic analogs, classified as retinoids, can be applied to the chemotherapy in the field of dermatology and oncology. Various benzoic acid derivatives exhibited the specific biological responses of retinoic acid and were named retinobenzoic acids. Especially, the aromatic amides such as Am80 and Am580 have better therapeutic effects than retinoic acid. N-Methylation of these highly active aromatic secondary amides caused the disappearance of the activity due to the change of the amide conformation from trans into cis. From such observations, the conformation of the linking group between alkyl-substituted benzene ring and benzoic acid moiety is an important factor for the activity. Some retinobenzoic acids do not bind to the cellularretinoic acid-binding protein, but bind to nuclear retinoic acid receptors (RARs) with the binding affinity corresponding to the potency of their biological activities. Among them, Am80 can bind to two of the three RAR subtypes (RAR α and β). The selectivity is favorable for the clinical application of retinoid since it has possibility to elicit a part of a number of the biological activities of retinoic acid.
公益社団法人日本薬学会の論文
1994-11-25