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Bioorg Med Chem ; 16(17): 8161-71, 2008 Sep 01.
Article in English | MEDLINE | ID: mdl-18722127

ABSTRACT

A novel series of dihydronaphthalene and benzosuberene analogs bearing structural similarity to the combretastatins in terms of 1,2-diarylethene, trimethoxyphenyl, and biaryl functionality has been synthesized. The compounds have been evaluated in regard to their ability to inhibit tubulin assembly and for their cytotoxicity against selected human cancer cell lines. From this series of compounds, benzosuberene analogs 2 and 4 inhibited tubulin assembly at concentrations comparable to that of combretastatin A-4 (CA4) and combretastatin A-1 (CA1). Furthermore, analog 4 demonstrated remarkable cytotoxicity against the three human cancer cell lines evaluated (for example GI(50)=0.0000032 microM against DU-145 prostate carcinoma).


Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Benzocycloheptenes/chemical synthesis , Bibenzyls/chemistry , Naphthalenes/chemical synthesis , Neoplasms/drug therapy , Tubulin/drug effects , Antineoplastic Agents/chemistry , Benzocycloheptenes/chemistry , Bibenzyls/pharmacology , Cell Line, Tumor , Cell Proliferation/drug effects , Crystallography, X-Ray , Dose-Response Relationship, Drug , Drug Design , Drug Screening Assays, Antitumor , Humans , Models, Molecular , Molecular Structure , Naphthalenes/chemistry , Stereoisomerism , Structure-Activity Relationship , Tubulin/metabolism
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