title: Halohydrin and oxime derivatives of radicicol: synthesis and antitumor activities.
abstract: Novel halohydrin and oxime derivatives of radicicol (1) were prepared and evaluated for their v-src tyrosine kinase inhibitory, antiproliferative, and antitumor activities. Some of the resulting derivatives showed significantly improved antitumor activities than those of 1 in vitro as tested in a cell proliferation assay and in vivo using sc-inoculated human breast carcinoma and epidermoid tumor models. Design and synthesis of radicicol-based novel affinity probes are also described.
authors.affiliation: Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., 3-6-6 Asahi-machi, Machida-shi, Tokyo, Japan. tsutomu.agatsuma@kyowa.co.jp
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Agatsuma
authors.forename: Harumi
authors.initials: H
authors.lastname: Ogawa
authors.forename: Kazuhito
authors.initials: K
authors.lastname: Akasaka
authors.forename: Akira
authors.initials: A
authors.lastname: Asai
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Yamashita
authors.forename: Tamio
authors.initials: T
authors.lastname: Mizukami
authors.forename: Shiro
authors.initials: S
authors.lastname: Akinaga
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Saitoh
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy / Q000473:pathology; D002851:Chromatography, High Pressure Liquid; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D005260:Female; D006801:Humans; D007202:Indicators and Reagents; D007783:Lactones / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D018942:Macrolides; D010091:Oximes / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D019061:src-Family Kinases / Q000037:antagonists & inhibitors
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D007783:Lactones; D018942:Macrolides; D010091:Oximes; D019061:src-Family Kinases; C035359:monorden