SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 3',4',5'-TRIHYDROXY ETOPOSIDE

Authors
SAULNIER MG LEBOULLUEC KL MCGEE DPC LONG BH CROSSWELL AR VYAS DM
Citation
Mg. Saulnier et al., SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 3',4',5'-TRIHYDROXY ETOPOSIDE, Bioorganic & medicinal chemistry letters, 3(8), 1993, pp. 1619-1624
Citations number
8
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
8
Year of publication
1993
Pages
1619 - 1624
Database
ISI
SICI code
0960-894X(1993)3:8<1619:SABO3E>2.0.ZU;2-Y
Abstract
The E-ring 3,4,5'-trihydroxy etoposide analog 3 of the clinical antitu mor agent etoposide 1 was synthesized from the corresponding etoposide ortho-quinone 2. This analog is twice as potent as etoposide in its a bility to elicit topoisomerase II mediated DNA double strand breaks. H owever, our in vitro cytotoxicity assay, using human colon tumor cells grown in culture, and our in vivo P388 murine leukemia screen reveal considerable loss of potency and/or activity vis-a-vis etoposide.