Synthesis of argentatin A derivatives as growth inhibitors of human cancer cell lines in vitro |
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Authors: | Parra-Delgado Hortensia Ramírez-Apan Teresa Martínez-Vázquez Mariano |
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Affiliation: | Instituto de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, Circuito Exterior, Coyoacán C. P. 04510, México, DF. |
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Abstract: | The syntheses of nine argentatin A analogs are described. These compounds were assessed for their ability to inhibit growth in vitro in four human cancer cell lines. Our results showed that the presence of either a double bond at C-1/C-2, or a bromine atom or formyl moiety at C-2 as well as the presence of an isoxazol ring in argentatin A enhanced its potency in all cell lines tested. In addition, an X-ray study of (16S,17R,20S,24R)-3-oxime-20,24-epoxy-16,25-dihydroxy-cycloartan-3-one led to the determination of the correct stereochemistry of argentatin A. |
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