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Synthesis of 1,1,2-triphenylethylenes and their antiproliferative effect on human cancer cell lines.

Anti-cancer drugs (2007-08-21)
Lifang Zheng, Qingyi Wei, Bo Zhou, Li Yang, Zhong-Li Liu
ABSTRACT

Tamoxifen analogs (1-3) and 1,1,2-triphenylethylenes (4-7) have been synthesized by the McMurry coupling reaction. Their antiproliferative effects on MCF-7 human breast-cancer cells, HO-8910 human ovarian-carcinoma cells, and (HL)-60 human promyelocytic-leukemia cells were studied by use of the colorimetric MTT assay or sulphorhodamine B assay. Compounds 2 and 3 exhibited significantly higher antiproliferative activity on all the three cell lines, and compound 6 exhibited a remarkably higher antiproliferative activity on HO-8910 and human peripheral blood HL-60 cell lines, than did tamoxifen. Structure-activity relationship analysis demonstrates that the methoxyl group on the 2-phenyl ring contributes critically to the activity.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Triphenylethylene, 99%