The bifunctional taxoid - colchicinoid hybrids 6-8 were synthesized and evaluated in assays of cytotoxicity and tubulin assembly/disassembly. All compounds showed a high degree of cytotoxicity, but, while 6 and 7 behaved as bifunctional tubulin binders not unlike an equimolecular mixture of taxol and thiocolchicine, 8 was surprisingly devoid of tubulin activity, acting on a distinct and yet to identify molecular target.
Synthesis and biological evaluation of paclitaxel-thiocoichicine hybrids / B. Danieli, A. Giardini, G. Lesma, D. Passarella, A. Silvani, G. Appendino, A. Noncovich, G. Fontana, E. Bombardelli, O. Sterner. - In: CHEMISTRY & BIODIVERSITY. - ISSN 1612-1872. - 1:2(2004), pp. 327-345.
Synthesis and biological evaluation of paclitaxel-thiocoichicine hybrids
B. DanieliPrimo
;G. Lesma;D. Passarella;A. Silvani;
2004
Abstract
The bifunctional taxoid - colchicinoid hybrids 6-8 were synthesized and evaluated in assays of cytotoxicity and tubulin assembly/disassembly. All compounds showed a high degree of cytotoxicity, but, while 6 and 7 behaved as bifunctional tubulin binders not unlike an equimolecular mixture of taxol and thiocolchicine, 8 was surprisingly devoid of tubulin activity, acting on a distinct and yet to identify molecular target.
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