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Synthesis and Biological Evaluation of PaclitaxelThiocolchicine Hybrids
Author(s) -
Danieli Bruno,
Giardini Alessandra,
Lesma Giordano,
Passarella Daniele,
Silvani Alessandra,
Appendino Giovanni,
covich Alain,
Fontana Gabriele,
Bombardelli Ezio,
Sterner Olov
Publication year - 2004
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200490029
Subject(s) - taxoid , bifunctional , chemistry , cytotoxicity , paclitaxel , tubulin , biochemistry , stereochemistry , in vitro , microtubule , microbiology and biotechnology , biology , genetics , chemotherapy , catalysis
The bifunctional taxoidcolchicinoid 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.