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

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

Volume: 3 Issue: 2

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Wada Akimori, Mizuguchi Yukari, Shinmen Masaki, Ito Masayoshi, Nakagawa Kimie and Okano Toshio, Preparation and Biological Activity of Retinoic Acid Analogs Containing an Aromatic Ring, Letters in Drug Design & Discovery 2006; 3 (2) . https://dx.doi.org/10.2174/157018006775789711