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