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  • Synthesis, anti-inflammatory and anticancer activity evaluation of some novel acridine derivatives.

Synthesis, anti-inflammatory and anticancer activity evaluation of some novel acridine derivatives.

European journal of medicinal chemistry (2009-11-21)
Sham M Sondhi, Jaiveer Singh, Reshma Rani, P P Gupta, S K Agrawal, A K Saxena
摘要

Condensation of 9-chloro-2,4-(un)substituted acridines (1a-c) with various amines (2a-e) and 9-isothiocyanato-2,4-(un)substituted acridines (4a,b) with different amines (2a,b,d,e) gave condensed products 3a-o and 5a-g respectively. Compounds 3a-o and 5a-g were screened for anti-inflammatory activity at a dose of 50mg/kg p.o. Compound 3e exhibited 41.17% anti-inflammatory activity which is better than most commonly used standard drug ibuprofen which showed 39% anti-inflammatory (at 50mg/kg p.o.) activity. Anticancer activity evaluation of compounds 3a-o and 5a-g was carried out against a small panel of human cancer cell lines and compounds 3g, 3m and 5g exhibited good anticancer activity against breast (MCF-7), liver (HEP-2), colon (COLO-205, 502713, HCT-15), lung (A-549) and neuroblastoma (IMR-32) cancer cell lines at a concentration of 1 x 10(-5)M.

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Sigma-Aldrich
5-氟脲嘧啶, ≥99% (HPLC), powder
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布洛芬, ≥98% (GC)
Supelco
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布洛芬, meets USP testing specifications
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