title: Synthesis and biological evaluation of conformationally flexible as well as restricted dimers of monastrol and related dihydropyrimidones.
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.
authors.affiliation: Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 607, India. ahmedkamal@iict.res.in
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.forename: M
authors.initials: M
authors.lastname: Shaheer Malik
authors.forename: Shaik
authors.initials: S
authors.lastname: Bajee
authors.forename: Shaik
authors.initials: S
authors.lastname: Azeeza
authors.forename: Shaikh
authors.initials: S
authors.lastname: Faazil
authors.forename: Sistla
authors.initials: S
authors.lastname: Ramakrishna
authors.forename: V G M
authors.initials: VG
authors.lastname: Naidu
authors.forename: M V P S
authors.initials: MV
authors.lastname: Vishnuwardhan
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D004247:DNA / Q000378:metabolism; D004055:Differential Thermal Analysis; D019281:Dimerization; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006090:Gram-Negative Bacteria / Q000187:drug effects* / Q000254:growth & development; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000254:growth & development; D006801:Humans; D020128:Inhibitory Concentration 50; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D011743:Pyrimidines / Q000494:pharmacology; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000494:pharmacology*; D012878:Skin Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship; D013871:Thiones / Q000494:pharmacology
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D011743:Pyrimidines; D011744:Pyrimidinones; D013871:Thiones; C400223:monastrol; D004247:DNA; C427203:calf thymus DNA