title: Microwave-assisted synthesis of 2(1H)-pyridones and their glucosides as cell proliferation inhibitors.
abstract: A new series of substituted 2(1H)-pyridones (4a-i) and their glucosides (5, 6a-e) were prepared as potential agents against leukemia (HL-60) cells. Glucosides (5,6a-e) were synthesized using three independent methods. Microwave protocol as an ecologically new method was used to synthesize the target compounds. Structures of the new products were confirmed using one- and two-dimensional NMR spectroscopy. In vitro exposure of pyridones substituted at position 4 with a 2-thienyl or 2-(trifluoromethyl)phenyl were found to exhibit high antiproliferation activities; in particular, 3-cyano-4-(thien-2'-yl)-6-(4''-chlorophenyl)-2(1H)-pyridone (4c) and its glucoside analogue (6c) had the highest activity.
authors.affiliation: Department of Chemistry, Faculty of Science, United Arab Emirates University, Al-Ain, United Arab Emirates.
authors.forename: Shaikha S
authors.initials: SS
authors.lastname: Al-Neyadi
authors.forename: Ahmed H
authors.initials: AH
authors.lastname: Hassan
authors.forename: Ibrahim M
authors.initials: IM
authors.lastname: Abdou
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D005960:Glucosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008872:Microwaves; D015394:Molecular Structure; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D005960:Glucosides; D011728:Pyridones