Synthesis and evaluation of anticancer activities of 2- or 4-substituted 3-(N-benzyltriazolylmethyl)-13α-oestrone derivatives
Copyright policy )Synthesis and evaluation of anticancer activities of 2- or 4-substituted 3-(N-benzyltriazolylmethyl)-13α-oestrone derivatives
2- or 4-Substituted 3-N-benzyltriazolylmethyl-13α-oestrone derivatives were synthesised via bromination of ring A and subsequent microwave-assisted, Pd-catalysed C(sp2)–P couplings. The antiproliferative activities of the newly synthesised brominated and phosphonated compounds against a panel of human cancer cell lines (A2780, MCF-7, MDA-MB 231) were investigated by means of MTT assays. The most potent compound, the 3-N-benzyltriazolylmethyl-4-bromo-13α-oestrone derivative exerted substantial selective cell growth-inhibitory activity against A2780 cell line with a submicromolar IC50 value. Computational calculations reveal strong interactions of the 4-bromo derivative with both colchicine and taxoid binding sites of tubulin. Disturbance of tubulin function has been confirmed by photometric polymerisation assay.
Models, Molecular, Dose-Response Relationship, Drug, Molecular Structure, Estrone, tubulin polymerisation, Antineoplastic Agents, RM1-950, hirao reaction, molecular dynamics, Polymerization, Mice, Structure-Activity Relationship, antiproliferative effect, Tubulin, Cell Line, Tumor, QD04 Organic chemistry / szerves kémia, NIH 3T3 Cells, Animals, Humans, azide–alkyne cycloaddition, Therapeutics. Pharmacology, Drug Screening Assays, Antitumor, Research Paper, Cell Proliferation
Models, Molecular, Dose-Response Relationship, Drug, Molecular Structure, Estrone, tubulin polymerisation, Antineoplastic Agents, RM1-950, hirao reaction, molecular dynamics, Polymerization, Mice, Structure-Activity Relationship, antiproliferative effect, Tubulin, Cell Line, Tumor, QD04 Organic chemistry / szerves kémia, NIH 3T3 Cells, Animals, Humans, azide–alkyne cycloaddition, Therapeutics. Pharmacology, Drug Screening Assays, Antitumor, Research Paper, Cell Proliferation
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