The stilbenoids E-resveratrol (E-3,5,4'-trihydroxystilbene, 1), E-3,5,4'-trimethoxystilbene (2), E-3,4,4'-trimethoxystilbene (3) and E-3,4'-dimethoxy-5-hydroxystilbene (4) were converted by photoisomerization to their corresponding Z-isomers 5-8. Compounds 1-8 were subjected to antiproliferative activity bioassays towards a set of four different human cancer cell lines, namely DU-145 (androgen not responsive human prostate tumor), LNCaP (androgen responsive human prostate tumor), M-14 (human melanoma) and KB (human mouth epidermoid carcinoma). The methylated analogues of 1 are more active than the natural lead in the majority of bioassays. The most active compound was Z-3,5,4'-trimethoxystilbene (6), which showed against DU-145 and LNCaP cells GI50 values close to those of the anticancer drug vinorelbine; 6 resulted more active than its E-isomer 2 towards DU-145, LNCaP and especially KB cell lines. A number of methylated Z-isomers displayed a higher activity than their E-isomers, but E-resveratrol (1) was more active than Z-resveratrol (5) towards all the tested cell lines.
|Titolo:||Antiproliferative activity of methylated analogues of E- and Z- resveratrol|
TRINGALI, Corrado (Corresponding)
|Data di pubblicazione:||2007|
|Citazione:||Antiproliferative activity of methylated analogues of E- and Z- resveratrol / Cardile, Venera; Chillemi, ROSA GIOVANNA; Lombardo, L; Sciuto, Sebastiano; Spatafora, Carmela; Tringali, Corrado. - In: ZEITSCHRIFT FUR NATURFORSCHUNG. C, A JOURNAL OF BIOSCIENCES. - ISSN 0939-5075. - 62:3-4(2007), pp. 189-195.|
|Appare nelle tipologie:||1.1 Articolo in rivista|