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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Preparation and Biological Activity of Retinoic Acid Analogs Containing an Aromatic Ring

Author(s): Akimori Wada, Yukari Mizuguchi, Masaki Shinmen, Masayoshi Ito, Kimie Nakagawa and Toshio Okano

Volume 3 , Issue 2 , 2006

Page: [118 - 122] Pages: 5

DOI: 10.2174/157018006775789711

Price: $65


Retinoic acid analogs, which contain an aromatic ring fixed between the 5 and 8 positions of retinoic acid, were synthesized by a palladium catalyzed coupling reaction between an enol triflate and a tributylstannylolefin and their biological activities were subsequently evaluated. None of the analogs exhibited antiproliferative, differentiation-inducing, or apoptosis-inducing activities in HL 60 cells. However, the 9Z-derivatives of indene and benzofuran showed a strong binding affinity for the RXR receptor compared to that of 9CRA.

Keywords: retinoic acid analogs, enol triflate, coupling reaction, RAR, RXR

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