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- W2950796721 abstract "Various sulpha drugs i.e. sulphaacetamide, sulphathiazole, sulphadiazine and sulphamerazine are coupled with 9-chloro-2,4(un)substituted acridines and 9-isothiocyanato-2, 4(un) substituted acridines to give corresponding coupled products 3a-f and 4a-h respectively. The structures of all synthesized compounds have beem confirmed by spectroscopic methods. Anti-inflammatory activity evaluation of 3a,b,e and 4a-h was carried out and compounds 4a, 4d, 4g and 4h showed 8,13, 22 and 3% activity respectively at 100mg/ kg p.o. Analgesic activity evaluation of 3a,b,e and 4a-h indicated that these compounds possess 25,75,50, 25, 50,50, 0, 75, 50, 50 and 50% analgesic activity at 100mg/kg p.o. Anticancer activity evaluation of 3a-f and 4a-h against a small panel of seven cancer cell lines consisting of lung (NCIH 460);colon (HT 29); melanoma (LOX); breast (MCF 7 and MCF 7 / ADR); prostate (DU145) and CNS (U251) tumors was carried out. Best GI 5 0 (concentration which inhibits the cell growth by 50%) values are shown by 4b, 0.4 μM (lung carcinoma, cell line NCIH 460); 4b, 0.3 μM (colon tumor, cell line HT29); 3e, 7.2μm (melanoma tumor, cell line LOX); 4b, 0.7μM (breast tumor, cell line MCF7); 4c, 1.9μM (breast tumor, cell line MCF7/ADR); 4b, 0.8 μM (prostate tumor, cell line DU 145) and 4b, 1.4 μM(CNS tumor, cell line U251) respectively. Out of all the compounds reported here GI 5 0 value shown by 4c i.e. 1.9 μM against breast tumor (MCF7/ADR) is quite close to the GI 5 0 value i.e. 1.2 μM of the standard drug doxorubicin. Also it is worthwhile to mention here that compound 4b, has shown good anticancer activity against four tumor cell lines i.e. GI 5 0 value < I μM." @default.
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- W2950796721 date "2002-12-01" @default.
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- W2950796721 title "Synthesis of sulpha drug acridine derivatives and their evaluation for anti-inflammatory, analgesic and anticancer activity" @default.
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