Preparation and biological activity of 13-substituted retinoic acids

…, K Fukunaga, M Ito, Y Mizuguchi, K Nakagawa…

文献索引：Wada, Akimori; Fukunaga, Kouki; Ito, Masayoshi; Mizuguchi, Yukari; Nakagawa, Kimie; Okano, Toshio Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 14 p. 3931 - 3942

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被引用次数: 16

摘要

13-Demethyl or 13-substituted all-E-and 9Z-retinoic acids were synthesized using a palladium-catalyzed coupling reaction of enol triflates and tributylstannylolefins. Their biological activities were then measured. The 13-ethyl analogs exhibited approximately one- half of the antiproliferative and differentiation-inducing activity of ATRA in HL-60 cells. In contrast, in the 9Z-derivatives, all analogs, except for the 13-butyl derivatives, showed ...