Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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

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


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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Article Details

Year: 2006
Page: [118 - 122]
Pages: 5
DOI: 10.2174/157018006775789711
Price: $58