Possible antineoplastic agents: Part XIII. Synthesis, biological evaluation and QSAR studies of some 1-(substituted benzenesulphonyl)-5-oxopyrrolidine-2-carboxylic acid derivatives.
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.
Purkayastha
S K
SK
Department of Pharmaceutical Technology, Jadavpur University, Calcutta, India.
Jha
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Pal
D K
DK
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A U
AU
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002286:Carcinoma, Ehrlich Tumor; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D051379:Mice; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D011761:Pyrrolidonecarboxylic Acid