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Remarkable tethering effect on DNA cleavage of propargylic sulfone conjugates with intercalating moieties
1Department of Chemistry, Hong Kong University of Science and Technology, Kowloon, China.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
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.