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1.
Bioorg Med Chem Lett ; 11(13): 1671-3, 2001 Jul 09.
Article in English | MEDLINE | ID: mdl-11425534

ABSTRACT

The synthesis and biological evaluation of novel sulfonate analogues of E-7010 are reported. Several of the compounds are potent inhibitors of cell proliferation and tubulin polymerization. Importantly, these compounds are also active against P-glycoprotein positive (+) cancer cells, which are resistant to many other antitumor agents.


Subject(s)
Aminophenols/chemistry , Antineoplastic Agents/pharmacology , Mitosis/drug effects , Sulfonamides/chemistry , Sulfonic Acids/pharmacology , Antineoplastic Agents/chemistry , Humans , Sulfonic Acids/chemistry , Tumor Cells, Cultured
2.
Bioorg Med Chem Lett ; 11(7): 871-4, 2001 Apr 09.
Article in English | MEDLINE | ID: mdl-11294380

ABSTRACT

Sulfonate analogues of combretastatin A-4 have been prepared. These compounds compete with colchicine and combretastatin A-4 for the colchicine binding site on tubulin and are potent inhibitors of tubulin polymerization and cell proliferation. Importantly, these compounds also inhibit the proliferation of P-glycoprotein positive (+) cancer cells, which are resistant to many other antitumor agents.


Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Colchicine/antagonists & inhibitors , Stilbenes/chemistry , Stilbenes/pharmacology , Tubulin Modulators , ATP Binding Cassette Transporter, Subfamily B, Member 1/biosynthesis , ATP Binding Cassette Transporter, Subfamily B, Member 1/genetics , Binding Sites/physiology , Binding, Competitive , Cell Division/drug effects , Colchicine/metabolism , Humans , Polymers/metabolism , Tubulin/metabolism , Tumor Cells, Cultured/cytology , Tumor Cells, Cultured/drug effects
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