Synthesis and structure-activity relationships of 2-pyrazinylcarboxamido-benzoates and β-Ionylideneacetamidobenzoates with retinoidal activity

…, AM Lebuis, JM Finkelstein, BJ Gour-Salin…

文献索引：Jones, Paul; Villeneuve, Gerald B.; Fei, Chengpei; DeMarte, Josie; Haggarty, Allison J.; Nwe, Khin Than; Martin, Deborah A.; Lebuis, Anne-Marie; Finkelstein, Joshua M.; Gour-Salin, Barbara J.; Chan, Tak Hang; Leyland-Jones, Brian R. Journal of Medicinal Chemistry, 1998 , vol. 41, # 16 p. 3062 - 3077

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被引用次数: 28

摘要

The structure-activity relationships of two series of novel retinoids (2- pyrazinylcarboxamidobenzoates and β-ionylideneacetamidobenzoates) have been investigated by evaluating their ability to induce differentiation in both human promyelocytic leukemia (HL60) cells and mouse embryonal carcinoma (P19) cells. The most active compound (ED50= 8.3× 10-9 M) of the 2-pyrazinylcarboxamidobenzoates is 4-[2-(5, 6, 7, ...