Antitumor activity of a novel antiestrogen (Analog II) on human breast cancer cells

Anti-cancer Drugs
P T JainJ T Pento

Abstract

Analog II (1,1-dichloro-cis-2,3-diarylcyclopropane), previously shown to be a pure antiestrogen in mice, was examined for potential antitumor activity on human breast cancer cells in culture. In this study, Analog II produced a dose-related antiproliferative effect on the growth of estrogen receptor (ER)-positive MCF-7 human breast cancer cells over a concentration range of 10(-11) to 10(-5) M. Analog II increased the fraction of MCF-7 cells in the G2/M phase of the cell cycle. Further, this compound inhibited the growth of ER-negative MDA-MB-231 human breast cancer cells over a concentration range of 10(-9) to 10(-6) M. Using scanning electron microscopy to evaluate drug-induced changes in cellular morphology, it was observed that Analog II decreased the length and density of microvilli on both MCF-7 and MDA-MB-231 cells. The effects of Analog II on MCF-7 and MDA-MB-231 cell proliferation and morphology were not reversed in the presence of estradiol. In addition, the induction of estrogen-dependent genes in MCF-7 cells was not reversed by Analog II. It was observed that non-specific cytotoxicity may be responsible for part of the Analog II-induced inhibition on MCF-7 and MDA-MB-231 cell proliferation. However, the antitumor ac...Continue Reading

Citations

Jul 27, 1999·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·C L MirandaD R Buhler
Sep 11, 2002·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Thao-Nguyen NguyenJ Thomas Pento
Feb 21, 2004·Natural Product Research·Saurabh ChattopadhyayA K Srivastava
Nov 17, 2001·In Vitro Cellular & Developmental Biology. Animal·G M TongJ T Pento
Sep 4, 1999·In Vitro Cellular & Developmental Biology. Animal·G M TongJ T Pento
Dec 14, 2006·Pharmacology·Gina M TongJ Thomas Pento

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