THE SYNTHESIS OF 5-SUBSTITUTED CAMPTOTHECINS AS POTENTIAL INHIBITORS OF DNA TOPOISOMERASE-I

Authors
WANG HK LIU SY HWANG KM MCPHAIL AT LEE KH
Citation
Hk. Wang et al., THE SYNTHESIS OF 5-SUBSTITUTED CAMPTOTHECINS AS POTENTIAL INHIBITORS OF DNA TOPOISOMERASE-I, Bioorganic & medicinal chemistry letters, 5(1), 1995, pp. 77-82
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
1
Year of publication
1995
Pages
77 - 82
Database
ISI
SICI code
0960-894X(1995)5:1<77:TSO5CA>2.0.ZU;2-S
Abstract
Four new 5-substituted camptothecins (4-7) have been synthesized and e valuated for DNA topoisomerase I inhibition. The results suggested tha t the pyridone moiety in the D ring of camptothecin plays a crucial ro le in determining its activity and that the 5 position of the C ring s hould be unsubstituted for retention of activity.