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http://nopr.niscpr.res.in/handle/123456789/22125| Title: | Synthesis of sulpha drug acridine derivatives and their evaluation for anti-inflammatory, analgesic and anticancer activity |
| Authors: | M.Sondhi, Sham Johar, Monika Singh, Nirupama Shukla, Rakesh Raghubir, Ram Dastidar, Sunanda G. |
| Issue Date: | Dec-2002 |
| Publisher: | NISCAIR-CSIR, India |
| 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 been confirmed by spectroscopic methods. Anti-inflammatory activity evaluation of 3a,b,c 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,c 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 (DU 145) and CNS (U251) tumors was carried out. Best GI50 (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, 0.8μM (prostate tumor, cell line DU 145) and 4b, 1.4μ M (CNS tumor, cell line U251) respectively. Out of all the compounds reported here GI50 value shown by 4c i.e. 1.9μM against breast tumor (MCF7/ADR) is quite close to the GI50 value i.e.1.2μM of the sta ndard drug doxorubicin. Also it is worthwhile to mention here that compound 4b, has shown good anticancer activity against four tumor cell lines i.e. GI50 value < 1μ M. |
| Page(s): | 2659-2666 |
| ISSN: | 0975-0983(Online); 0376-4699(Print) |
| Appears in Collections: | IJC-B Vol.41B(12) December 2002] |
Files in This Item:
| File | Description | Size | Format | |
|---|---|---|---|---|
| IJCB 41B(12) 2659-2666.pdf | 1.53 MB | Adobe PDF | View/Open |
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