NOVEL A-RING MODIFIED CAMPTOTHECINS AS TOPOISOMERASE-I INHIBITORS

Authors
PEEL MR MILSTEAD MW STERNBACH DD BESTERMAN JM LEITNER P MORTON B WALL ME WANI MC
Citation
Mr. Peel et al., NOVEL A-RING MODIFIED CAMPTOTHECINS AS TOPOISOMERASE-I INHIBITORS, Bioorganic & medicinal chemistry letters, 5(18), 1995, pp. 2129-2132
Citations number
14
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
18
Year of publication
1995
Pages
2129 - 2132
Database
ISI
SICI code
0960-894X(1995)5:18<2129:NAMCAT>2.0.ZU;2-3
Abstract
A camptothecin derivative has been prepared wherein the A-ring is fuse d to an oxazole ring. The compound was prepared via a Friedlander cond ensation involving benzoxazole 8 and tricyclic ketone 9. This derivati ve displays potent topoisomerase I inhibition (IC50 150 nM) when assay ed in the 'cleavable complex' assay.