title: Remarkable tethering effect on DNA cleavage of propargylic sulfone conjugates with intercalating moieties.
abstract: A number of novel propargylic sulfone conjugates 3 and 4 with intercalating moieties were synthesized and evaluated for DNA cleavage activity through nucleic base alkylation. A remarkable enhancement in DNA cleaving potency was observed with those conjugates 3 possessing a suitable spacer, a right attachment point at the aromatic ring, and a good intercalator.
authors.affiliation: Department of Chemistry, Hong Kong University of Science and Technology, Kowloon, China.
authors.forename: W M
authors.initials: WM
authors.lastname: Dai
authors.forename: Q
authors.initials: Q
authors.lastname: Li
authors.forename: K C
authors.initials: KC
authors.lastname: Fong
authors.forename: C W
authors.initials: CW
authors.lastname: Chow
authors.forename: L
authors.initials: L
authors.lastname: Zhou
authors.forename: W
authors.initials: W
authors.lastname: Hamaguchi
authors.forename: S
authors.initials: S
authors.lastname: Nishimoto
mesh_terms: D000480:Alkynes / Q000737:chemistry*; D010584:Bacteriophage phi X 174 / Q000235:genetics; D004279:DNA, Viral / Q000737:chemistry*; D004587:Electrophoresis, Agar Gel; D006868:Hydrolysis; D007364:Intercalating Agents / Q000737:chemistry*; D007510:Isatin / Q000031:analogs & derivatives* / Q000737:chemistry
chemical_list: D000480:Alkynes; D004279:DNA, Viral; D007364:Intercalating Agents; C116442:propargylic sulfone; D007510:Isatin