title: Synthesis of tetrocarcin derivatives with specific inhibitory activity towards Bcl-2 functions.
abstract: Tetrocarcin A was recently identified as an inhibitor of the anti-apoptotic function of Bcl-2. We synthesized novel tetrocarcin derivatives in order to increase their selective inhibitory activity against Bcl-2. It was found that 21-acetoxy-9-glycosyloxy derivatives had potent Bcl-2 inhibitory activity without significant antimicrobial activity.
authors: Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd, Machida, Tokyo, Japan. masami.kaneko@kyowa.co.jp
authors: M
authors: M
authors: Kaneko
authors: T
authors: T
authors: Nakashima
authors: Y
authors: Y
authors: Uosaki
authors: M
authors: M
authors: Hara
authors: S
authors: S
authors: Ikeda
authors: Y
authors: Y
authors: Kanda
mesh_terms: D000617:Aminoglycosides; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D020169:Caspases / Q000187:drug effects*; D005260:Female; D006367:HeLa Cells; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000037:antagonists & inhibitors* / Q000096:biosynthesis / Q000235:genetics; D013329:Structure-Activity Relationship
chemical_list: D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D000903:Antibiotics, Antineoplastic; D019253:Proto-Oncogene Proteins c-bcl-2; C025518:tetrocarcin A; D020169:Caspases