title: Thio-sugar motif of functional CARB-pharmacophore for antineoplastic activity. Part 2.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Sciences, Nesbitt School of Pharmacy, Wilkes University, 84.W. South Street, Wilkes-Barre, PA 18766, USA. Electronic address: zbigniew.witczak@wilkes.edu.
authors.forename: Zbigniew J
authors.initials: ZJ
authors.lastname: Witczak
authors.affiliation: Department of Molecular Genetics, University of Lodz, Lodz 90-236, Poland.
authors.forename: Joanna
authors.initials: J
authors.lastname: Sarnik
authors.affiliation: Department of Molecular Genetics, University of Lodz, Lodz 90-236, Poland.
authors.forename: Anna
authors.initials: A
authors.lastname: Czubatka
authors.affiliation: Department of Cytobiochemistry, University of Lodz, 90-236 Lodz, Poland.
authors.forename: Ewa
authors.initials: E
authors.lastname: Forma
authors.affiliation: Department of Molecular Genetics, University of Lodz, Lodz 90-236, Poland. Electronic address: tomasz.poplawski@biol.uni.lodz.pl.
authors.forename: Tomasz
authors.initials: T
authors.lastname: Poplawski
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D004187:Disaccharides / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D008968:Molecular Conformation; D054330:Thiosugars / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D004187:Disaccharides; D054330:Thiosugars
keywords: 1-4-S-thiodisaccharides; Cancer cell lines; Functional CARB-pharmacophore (FCP); Thio-sugars