Pyrazolone-fused combretastatins and their precursors : synthesis, cytotoxicity, antitubulin activity and molecular modeling studies (CROSBI ID 159366)
Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija
Podaci o odgovornosti
Burja, Bojan ; Čimbora-Zovko, Tamara ; Tomić, Sanja ; Jelušić, Tihana ; Kočevar, Marijan ; Polanc, Slovenko ; Osmak, Maja
engleski
Pyrazolone-fused combretastatins and their precursors : synthesis, cytotoxicity, antitubulin activity and molecular modeling studies
A series of pyrazolone-fused combretastatins and precursors were synthesized and their cytotoxicity as well as antitubulin potential was evaluated. The hydrazide 9f and the pyrazolone-fused combreta¬statins 12a, 12b and 12c were highly cytotoxic against various tumor cell lines including cisplatin resistant cells. The same compounds were also the best inhibitors of tubulin polymerization. Molecular modeling results showed that they bind the colchicine binding site at the tubulin heterodimer. The hydrazide 9f arrested HeLa cells in the G2/M phase of the cell cycle and strongly affected cell shape and microtubule network.
Combretastatin CA-4 derivatives ; Cytotoxicity ; Tubulin ; Molecular modeling
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Podaci o izdanju
18 (7)
2010.
2375-2387
objavljeno
0968-0896
1464-3391
10.1016/j.bmc.2010.03.006