Synthesis of bicyclic enediynes that possess a photosensitive triggering device and exhibit strong DNA cleaving activity.
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.
Tanaka
Hiroshi
H
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
Tanaka
Yoshikazu
Y
Minoshima
Masafumi
M
Yamaguchi
Sho
S
Fuse
Shinichiro
S
Doi
Takayuki
T
Kawauchi
Susumu
S
Sugiyama
Hiroshi
H
Takahashi
Takashi
T
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
D053281:Enediynes; D007093:Imidazoles; D009757:Nylons; D017319:Photosensitizing Agents; D011758:Pyrroles; C029899:imidazole; D004247:DNA