2-Methoxyestradiol and analogs as novel antiproliferative agents: analysis of three-dimensional quantitative structure-activity relationships for DNA synthesis inhibition …

…, D McAllister, R Vlahos, A Robertson, M Cushman…

Index: Hughes, Richard A.; Harris, Trudi; Altmann, Emile; McAllister, David; Vlahos, Ross; Robertson, Alan; Cushman, Mark; Wang, Zhiqiang; Stewart, Alastair G. Molecular Pharmacology, 2002 , vol. 61, # 5 p. 1053 - 1069

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Citation Number: 46

Abstract

Abstract 2-Methoxyestradiol (2-MEO), a metabolite of estrogen, is an attractive lead compound for the development of novel antitumor and anti-inflammatory agents, because it embodies antiproliferative and antiangiogenic activities in one molecule. However, the affinity of 2-MEO for the estrogen receptor would lead to undesirable side effects. As a prelude to the design of 2-MEO–like compounds with an optimal activity profile, we ...