title: Ecteinascidins. A review of the chemistry, biology and clinical utility of potent tetrahydroisoquinoline antitumor antibiotics.
abstract: The ecteinascidin family comprises a number of biologically active compounds, containing two to three tetrahydroisoquinoline subunits. Although isolated from marine tunicates, these compounds share a common pentacyclic core with several antimicrobial compounds found in terrestrial bacteria. Among the tetrahydroisoquinoline natural products, ecteinascidin 743 (Et-743) stands out as the most potent antitumor antibiotics that it is recently approved for treatment of a number of soft tissue sarcomas. In this article, we will review the backgrounds, the mechanism of action, the biosynthesis, and the synthetic studies of Et-743. Also, the development of Et-743 as an antitumor drug is discussed.
authors.affiliation: Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA. rmw@lamar.colostate.edu.
authors.forename: V H
authors.initials: VH
authors.lastname: Le
authors.forename: M
authors.initials: M
authors.lastname: Inai
authors.forename: R M
authors.initials: RM
authors.lastname: Williams
authors.forename: T
authors.initials: T
authors.lastname: Kan
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D004149:Dioxoles / Q000737:chemistry / Q000494:pharmacology; D008386:Marine Biology; D015394:Molecular Structure; D044005:Tetrahydroisoquinolines / Q000737:chemistry / Q000494:pharmacology; D000077606:Trabectedin; D014561:Urochordata / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004149:Dioxoles; D044005:Tetrahydroisoquinolines; D000077606:Trabectedin