Synthesis, antitumor evaluation, and apoptosis-inducing activity of hydroxylated (E)-stilbenes.
The parallel solution-phase synthesis of a series of 30 monohydroxylated (E)-stilbene analogues is described. In vitro screening revealed low micromolar activity (GI(50)) against the MDA MB 468 breast cancer cell line. Activity in MDA MB 468 cells correlated with the ability to induce apoptosis following drug treatment by the most potent agents in the series, e.g., 5dy and 5jy, an observation further reinforced by AnnexinV-FITC analysis and fluorescence microscopy.
Lion
Cedric J
CJ
Cancer Research U.K. Experimental Cancer Chemotherapy Research Group, Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, UK.
Matthews
Charles S
CS
Stevens
Malcolm F G
MF
Westwell
Andrew D
AD
D017304:Annexin A5; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis; D045744:Cell Line, Tumor; D020650:Combinatorial Chemistry Techniques; D004354:Drug Screening Assays, Antitumor; D005434:Flow Cytometry; D016650:Fluorescein-5-isothiocyanate; D005456:Fluorescent Dyes; D006801:Humans; D006900:Hydroxylation; D008856:Microscopy, Fluorescence; D011419:Propidium; D013237:Stereoisomerism; D013267:Stilbenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D017304:Annexin A5; D000970:Antineoplastic Agents; D005456:Fluorescent Dyes; D013267:Stilbenes; D011419:Propidium; D016650:Fluorescein-5-isothiocyanate