Synthesis and biological activities of phthalocyanine-estradiol conjugates
Ehtsham H Khan1, Hasrat Ali, Hongjian Tian
1Department of Chemistry, A.M.U. Aligarh (U.P.) India.
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.
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