2-[N-1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: A potent antitumor agent

Authors
Huang, ZH Yang, GJ Lin, ZL Huang, JL
Citation
Zh. Huang et al., 2-[N-1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: A potent antitumor agent, BIOORG MED, 11(9), 2001, pp. 1099-1103
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
9
Year of publication
2001
Pages
1099 - 1103
Database
ISI
SICI code
0960-894X(20010507)11:9<1099:2E4A>2.0.ZU;2-R
Abstract
2-[N-1-2-Pyrimidyl-aminobenzensulfonamido] ethyl 4-bis(2-chloroethyl) amino phenyl butyrate has been prepared by reaction of chlorambucil with sulfadia zine derivative. Schiff's base has been used as the protective group of the ;aromatic amine in the synthesis. It can be completely removed by the irrad iation of 365 nm UV light at room temperature. The title compound exhibits a high antitumor activity with a therapeutic index (TI) of 47.55 which is t wice that of chlorambucil's (TI: 22.84). (C) 2001 Elsevier Science Ltd. All rights reserved.