title: Synthesis and anticancer activity of geldanamycin derivatives derived from biosynthetically generated metabolites.
abstract: A new series of geldanamycin derivatives were synthesized using a semi-synthetic approach involving genetically engineered biosynthetic intermediates. These analogues were then evaluated for anti-proliferation activity in human cancer cell lines, SK-Br3 and SK-Ov3. Most of the synthesized compounds exhibited potent in vitro anti-proliferation activity toward both cell lines. Such compounds potently inhibited the expression of the Hsp90 client protein ErbB2.
authors.affiliation: Korea Research Institute of Bioscience & Biotechnology, 52 Eoeundong, Yuseonggu, Daejeon, 305-806, Korea. kaylee@kribb.re.kr
authors.forename: Kyeong
authors.initials: K
authors.lastname: Lee
authors.forename: Jung S
authors.initials: JS
authors.lastname: Ryu
authors.forename: Yinglan
authors.initials: Y
authors.lastname: Jin
authors.forename: Woncheol
authors.initials: W
authors.lastname: Kim
authors.forename: Navneet
authors.initials: N
authors.lastname: Kaur
authors.forename: Sang J
authors.initials: SJ
authors.lastname: Chung
authors.forename: Yong-Jin
authors.initials: YJ
authors.lastname: Jeon
authors.forename: Joon-Tae
authors.initials: JT
authors.lastname: Park
authors.forename: Ji S
authors.initials: JS
authors.lastname: Bang
authors.forename: Hong S
authors.initials: HS
authors.lastname: Lee
authors.forename: Tae Y
authors.initials: TY
authors.lastname: Kim
authors.forename: Jung J
authors.initials: JJ
authors.lastname: Lee
authors.forename: Young-Soo
authors.initials: YS
authors.lastname: Hong
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016227:Benzoquinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D005818:Genetic Engineering; D018841:HSP90 Heat-Shock Proteins / Q000037:antagonists & inhibitors; D006801:Humans; D047029:Lactams, Macrocyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008968:Molecular Conformation; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000037:antagonists & inhibitors; D013237:Stereoisomerism
chemical_list: D000970:Antineoplastic Agents; D016227:Benzoquinones; D018841:HSP90 Heat-Shock Proteins; D047029:Lactams, Macrocyclic; D018719:Erb-b2 Receptor Tyrosine Kinases; C508053:ERBB2 protein, human; C001277:geldanamycin