title: Synthesis of bicyclic enediynes that possess a photosensitive triggering device and exhibit strong DNA cleaving activity.
abstract: The synthesis of a bicyclic enediyne capable of photosensitive triggering and conjugated to a pyrrole-imidazole polyamide is described. Using UV irradiation, this hybrid molecule is shown to exhibit 100-fold stronger potency for DNA cleavage, in an in vitro assay, as compared to the enediyne without the DNA-localizing pyrrole-imidazole.
authors.affiliation: Department of Applied Chemistry, Graduate School of Science and Engineering, Tokyo Institute of Technology, 2-12-1-H-101 Ookayama, Meguro, Tokyo 152-8552, Japan. thiroshi@apc.titech.ac.jp
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tanaka
authors.forename: Yoshikazu
authors.initials: Y
authors.lastname: Tanaka
authors.forename: Masafumi
authors.initials: M
authors.lastname: Minoshima
authors.forename: Sho
authors.initials: S
authors.lastname: Yamaguchi
authors.forename: Shinichiro
authors.initials: S
authors.lastname: Fuse
authors.forename: Takayuki
authors.initials: T
authors.lastname: Doi
authors.forename: Susumu
authors.initials: S
authors.lastname: Kawauchi
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Sugiyama
authors.forename: Takashi
authors.initials: T
authors.lastname: Takahashi
mesh_terms: D004247:DNA / Q000737:chemistry*; D053837:DNA Cleavage; D053281:Enediynes / Q000138:chemical synthesis* / Q000737:chemistry; D007093:Imidazoles / Q000737:chemistry; D009757:Nylons / Q000737:chemistry; D017319:Photosensitizing Agents / Q000737:chemistry*; D011758:Pyrroles / Q000737:chemistry; D014466:Ultraviolet Rays
chemical_list: D053281:Enediynes; D007093:Imidazoles; D009757:Nylons; D017319:Photosensitizing Agents; D011758:Pyrroles; C029899:imidazole; D004247:DNA