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Synthesis And Anticancer Activity Some L-Cystine Derivatives

Author(s): S. V Sharma, S Sankar, G. V. S Rama Sarma, Girija Kuttan, B Suresh

Eight 3,3'-dithio bis-(2-amino-N-alkyl/aryl propanamides) (la-h), four 3,3'-dithio bis-[2-(Nacetamido)-N-aryl propanamids] (Ila-d) and five 3,3'-dithio bis-[2-(aryl amino) acetamido propanoic acids] (Illa-e) were synthesised from appropriate L-cystine or N,N’-bis acetyl cystine in satisfactory yields. All these compounds were purified and characterised by analytical and spectral data. Antitumour activity of selected drugs was studied by employing in vitro cytotoxicity assays and in vitro tumour growth inhibition studies. In vitro short term cytotoxicity studies indicated that six of the test compounds (la,b,d; Ilb; Illa,b) produced significant cytotoxicity in Ehrlich ascites carcinoma (EAC) and Dalton's lymphoma ascites (DLA) tumour cells at a concentration upto 400 µg/ml. Tissue culture studies using L929 tumour cells resulted In more than 50% growth inhibition at 1.25 µg/mg concentration for the four test compounds. Administration of selected drugs (25 µg I.p. for 5 alternate days) resulted in an increase in life span of ascites tumour-bearing mice upto 102% (EAC tumour) and 68% (DLA tumour) treated with IIIb as compared with control. All the test compounds were found to possess significant antitumour activity against experimental tumours.


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Citations : 53647

Indian Journal of Pharmaceutical Sciences received 53647 citations as per google scholar report