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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
VOLUME: 11
ISSUE: 3
DOI: 10.2174/15701808113106660086      Price:  $58









Synthesis of Sulfur Containing Colchicine Derivatives and their Biological Evaluation as Cytotoxic Agents

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Author(s): Joanna Kurek, Wladyslaw Boczon, Krzysztof Myszkowski, Marek Murias, Teresa Borowiak and Irena Wolska
Pages 279-289 (11)
Abstract:
Semi-synthetic C-10 alkyl thio analogues of the cytotoxic natural alkaloid colchicine have been found to exhibit cytotoxicity towards tumour cell lines at levels comparable to that of the natural product. An efficient synthesis of 10-alkyl thiocolchicines in mild conditions is proposed and the products are studied by 1H and 13C NMR, FT-IR, MS-EI methods and elementary analysis. The crystal structure of 10-ethylthiocolchicine is characterised using X-ray diffraction methods. Cytotoxic activity against selected cancer cell lines for all obtained 10-alkylthio analogues of colchicine is also reported.
Keywords:
10-alkylthiolcolchicine derivatives, Spectral characterisation, Cytotoxic activity, Crystal structure of 10-ethylthiocolchicine.
Affiliation:
Laboratory for Chemistry of Heterocyclic Compounds, Faculty of Chemistry, Adam Mickiewicz University, Grunwaldzka 6, 60-780 Poznan, Poland.