Thio-sugar motif of functional CARB-pharmacophore for antineoplastic activity. Part 2.

Bioorg Med Chem Lett

Department of Molecular Genetics, University of Lodz, Lodz 90-236, Poland. Electronic address:

Published: December 2014

Diverse functionalized representatives of (1-4)-S-thiodisaccharides, 6-9 were synthesized and assessed for cytotoxicity and apoptosis against human cancer cell lines (A549, LoVo, MCF-7 and HeLa). The FCP 6 was more active against MCF-7 cells (i.e., an estrogen-dependent breast cancer line), whereas other (1-4)-S-thiodisaccharides showed strongest activity against A549 cells (i.e., a lung adenocarcinoma line). We propose to use a concept of functional 'CARB-pharmacophores' when evaluating a potential for the compounds' general antineoplastic activity. Future studies will determine the reasons for cell-type specificity of these compounds. The thio-sugar motif appears to be a promising lead for future developments.

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http://dx.doi.org/10.1016/j.bmcl.2014.10.095DOI Listing

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