Remarkable tethering effect on DNA cleavage of propargylic sulfone conjugates with intercalating moieties.
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.
Dai
W M
WM
Department of Chemistry, Hong Kong University of Science and Technology, Kowloon, China.
Li
Q
Q
Fong
K C
KC
Chow
C W
CW
Zhou
L
L
Hamaguchi
W
W
Nishimoto
S
S
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
D000480:Alkynes; D004279:DNA, Viral; D007364:Intercalating Agents; C116442:propargylic sulfone; D007510:Isatin