POSSIBLE ANTINEOPLASTIC AGENTS .13. SYNTHESIS, BIOLOGICAL EVALUATION AND QSAR STUDIES OF SOME 1-(SUBSTITUTED BENZENESULFONYL)-5-OXOPYRROLIDINE-2-CARBOXYLIC ACID-DERIVATIVES

Authors
PURKAYASTHA SK JHA T PAL DK DE AU
Citation
Sk. Purkayastha et al., POSSIBLE ANTINEOPLASTIC AGENTS .13. SYNTHESIS, BIOLOGICAL EVALUATION AND QSAR STUDIES OF SOME 1-(SUBSTITUTED BENZENESULFONYL)-5-OXOPYRROLIDINE-2-CARBOXYLIC ACID-DERIVATIVES, Anti-cancer drug design, 8(2), 1993, pp. 95-100
Citations number
14
Categorie Soggetti
Pharmacology & Pharmacy",Oncology
Journal title
Anti-cancer drug design → ACNP
ISSN journal
02669536
Volume
8
Issue
2
Year of publication
1993
Pages
95 - 100
Database
ISI
SICI code
0266-9536(1993)8:2<95:PAA.SB>2.0.ZU;2-C
Abstract
Twelve analogues of 1-(substituted benzenesulphonyl)-5-oxopyrrolidine- 2-carboxylic acid have been synthesized and tested for antineoplastic activity in Swiss albino mice with an Ehrlich ascites carcinoma (EAC) cell line. The values of percent inhibition of growth, both in ascitic cell count and fluid weight, have been taken as activity parameters. Quantitative structure-activity relationships (QSAR) have been studied using the LFER model. The best correlation (R2 = 93.0%) was found usi ng molar refractivity (MR), which measures the molar volume and polari zability of the substituents.