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ID: ALA1136680
Journal: Bioorg Med Chem Lett
Title: Synthesis and biological activities of phthalocyanine-estradiol conjugates.
Authors: Khan EH, Ali H, Tian H, Rousseau J, Tessier G, Shafiullah, van Lier JE.
Abstract: Phthalocyanine-based photosensitizers, coupled via a 17alpha-ethynyl group to estradiol using Pd(II) as a catalyst, were synthesized and evaluated for their estrogen receptor binding affinity and in vitro photocytotoxicity. The highest receptor binding affinities (RBA=8-13) were observed with lipophilic conjugates coupled via a relative long spacer group while the sulfonated analogues showed little binding affinities (RBA <2). The highest photocytotoxicity was observed with the sulfonated conjugates, the nature of the spacer group did not have a pronounced effect.
CiteXplore: 12657265