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Eur J Med Chem ; 46(8): 3274-81, 2011 Aug.
Article in English | MEDLINE | ID: mdl-21620531

ABSTRACT

A series of conformationally flexible and restricted dimers of monastrol as well as related dihydropyrimidones have been synthesized by employing one-pot Biginelli multicomponent reaction. These dimers have been evaluated for cytotoxic potency against selected human cancer cell lines and some of the compounds have exhibited more cytotoxic potency than the parent monastrol. Further, the DNA binding ability by thermal denaturation studies and antimicrobial activities of these compounds are also discussed.


Subject(s)
Anti-Infective Agents/pharmacology , Antineoplastic Agents/pharmacology , Breast Neoplasms/drug therapy , Colonic Neoplasms/drug therapy , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Lung Neoplasms/drug therapy , Pyrimidinones/pharmacology , Skin Neoplasms/drug therapy , Anti-Infective Agents/chemical synthesis , Antineoplastic Agents/chemical synthesis , Breast Neoplasms/pathology , Cell Line, Tumor , Colonic Neoplasms/pathology , DNA/metabolism , Differential Thermal Analysis , Dimerization , Drug Screening Assays, Antitumor , Female , Gram-Negative Bacteria/growth & development , Gram-Positive Bacteria/growth & development , Humans , Inhibitory Concentration 50 , Lung Neoplasms/pathology , Microbial Sensitivity Tests , Molecular Conformation , Pyrimidines/pharmacology , Pyrimidinones/chemical synthesis , Skin Neoplasms/pathology , Structure-Activity Relationship , Thiones/pharmacology
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