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SYNTHESIS AND BIOLOGICAL EVALUATION OF BIARYL ANALOGS OF ANTITUBULIN COMPOUNDS.

ABSTRACT: This paper reports the synthesis of methanones and esters bearing different substitution patterns as spacer groups between aromatic rings. This series of compounds can be considered phenstatin analogs. Two of the newly synthesized compounds, 5a and 5c, strongly inhibited tubulin polymerization and the binding of [(3)H] colchicine to tubulin, suggesting that, akin to phenstatin and combretastatin A-4, they can bind to tubulin at the colchicine site.

SUBMITTER: Tozatti CS

PROVIDER: S-EPMC3472429 | biostudies-literature | 2012 Jan

REPOSITORIES: biostudies-literature

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SYNTHESIS AND BIOLOGICAL EVALUATION OF BIARYL ANALOGS OF ANTITUBULIN COMPOUNDS.

Tozatti Camila Santos Suniga CS Khodyuk Rejane Gonçalves Diniz RG da Silva Adriano Olimpio AO Dos Santos Edson Dos Anjos ED de Lima Marcos Serrou do Amaral E Dênis Pires MS Hamel Ernest E

Quimica nova 20120101 9

This paper reports the synthesis of methanones and esters bearing different substitution patterns as spacer groups between aromatic rings. This series of compounds can be considered phenstatin analogs. Two of the newly synthesized compounds, 5a and 5c, strongly inhibited tubulin polymerization and the binding of [(3)H] colchicine to tubulin, suggesting that, akin to phenstatin and combretastatin A-4, they can bind to tubulin at the colchicine site. ...[more]

PMID: 23087491

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