2 documents found, page 1 of 1
Synthesis and biological activity of sulfur compounds showing structural analog...
Santos,Edson dos A. dos; Prado,Paulo C.; Carvalho,Wanderley R. de; Lima,Ricardo V. de; Beatriz,Adilson; Lima,Dênis P. de; Hamel,Ernest; Dyba,Marzena A.We extended our previous exploration of sulfur bridges as bioisosteric replacements for atoms forming the bridge between the aromatic rings of combretastatin A-4. Employing coupling reactions between 5-iodo-1,2,3-trimethoxybenzene and substituted thiols, followed by oxidation to sulfones with m-CPBA, different locations for attaching the sulfur atom to ring A through the synthesis of nine compounds were examine...
Synthesis and biological evaluation of biaryl analogs of antitubulin compounds
Tozatti,Camila Santos Suniga; Khodyuk,Rejane Gonçalves Diniz; Silva,Adriano Olimpio da; Santos,Edson dos Anjos dos; Amaral,Marcos Serrou doThis 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 [³H] colchicine to tubulin, suggesting that, akin to phenstatin and combretastatin A-4, they can bin...