Possible antineoplastic agents: Part XIII. Synthesis, biological evaluation and QSAR studies of some 1- (substituted benzenesulphonyl) -5-oxopyrrolidine-2-carboxylic acid derivatives
Purkayastha, S.K.; Jha, T.; Pal, D.K.; De, A.U.
Anti-Cancer Drug Design 8(2): 95-100
1993
ISSN/ISBN: 0266-9536 PMID: 8494605 Document Number: 417548
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 using molar refractivity (MR), which measures the molar volume and polarizability of the substituents.