Fumitremorgin C analogs that reverse mitoxantrone resistance in human colon carcinoma cells

Authors
He, HY Rabindran, SG Greenberger, LM Carter, GT
Citation
Hy. He et al., Fumitremorgin C analogs that reverse mitoxantrone resistance in human colon carcinoma cells, MED CHEM RE, 9(6), 1999, pp. 424-437
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
MEDICINAL CHEMISTRY RESEARCH
ISSN journal
10542523 → ACNP
Volume
9
Issue
6
Year of publication
1999
Pages
424 - 437
Database
ISI
SICI code
1054-2523(1999)9:6<424:FCATRM>2.0.ZU;2-W
Abstract
A series of diketopiperazines (1a) that mimic the natural product, fumitrem orgin C (1), were synthesized. This class of compounds enhanced the sensiti vity of a mitoxantrone-selected colon carcinoma cell line, S1-M1-3.2, to va rious antitumor agents, thereby reversing multidrug resistance. An SAR stud y showed that the presence of a lipid chain at C-x in the S configuration i s essential for retaining strong chemosensitizing activity.