Synthesis and Biological Evaluation of PaclitaxelThiocolchicine Hybrids | Zendy

Danieli Bruno | Zendy; Giardini Alessandra | Zendy; Lesma Giordano | Zendy; Passarella Daniele | Zendy; Silvani Alessandra | Zendy; Appendino Giovanni | Zendy; covich Alain | Zendy; Fontana Gabriele | Zendy; Bombardelli Ezio | Zendy; Sterner Olov | Zendy

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Synthesis and Biological Evaluation of PaclitaxelThiocolchicine 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.

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