Remarkable tethering effect on DNA cleavage of propargylic sulfone conjugates with intercalating moieties
摘要:
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.
Remarkable tethering effect on DNA cleavage of propargylic sulfone conjugates with intercalating moieties
摘要:
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.
number of novel 2-naphthyl propargylic sulfones were synthesized as nucleic base alkylating agents. Extremely high DNA cleavage activity was observed for the sulfones with a free omega-hydroxyl group in the carbon chain in contrast to the ester conjugates possessing an additional intercalating unit.
Remarkable tethering effect on DNA cleavage of propargylic sulfone conjugates with intercalating moieties
作者:Wei-Min Dai、Quan Li、Kin Chiu Fong、Chun Wo Chow、Ling Zhou、Wataru Hamaguchi、Sei-ichi Nishimoto
DOI:10.1016/s0960-894x(97)10203-7
日期:1998.1
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.