title: Design and synthesis of harzialactone analogues: promising anticancer agents.
abstract: New homologues of harzialactone were synthesized using D-glucose as chiral template. Wittig reaction to introduce aromatic moiety in 10 and chemoselective anomeric oxidation of 13 were used as key reactions in our synthesis. Anticancer activity of these target molecules was assessed against five cancer cell lines, P388D1, HL60, COLO-205, Zr-75-1 and HeLa. Both compound 5 and 6, showed significant activity against colon cancer (COLO-205) and cervical cancer (HeLa) and moderate with others. To the best of our knowledge, this is the first report of harzialactone analogues as potent inhibitors of human colon and cervical cancer.
authors.affiliation: Garware Research Centre, Department of Chemistry, University of Pune, Pune, India.
authors.forename: Vishwas U
authors.initials: VU
authors.lastname: Pawar
authors.forename: Sougata
authors.initials: S
authors.lastname: Ghosh
authors.forename: Balu A
authors.initials: BA
authors.lastname: Chopade
authors.forename: Vaishali S
authors.initials: VS
authors.lastname: Shinde
mesh_terms: D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D045744:Cell Line, Tumor; D003110:Colonic Neoplasms / Q000188:drug therapy; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D005947:Glucose / Q000737:chemistry; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D010084:Oxidation-Reduction; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D002583:Uterine Cervical Neoplasms / Q000188:drug therapy
chemical_list: D000970:Antineoplastic Agents; D007783:Lactones; D005947:Glucose; D015107:4-Butyrolactone