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Synthesis, anti-inflammatory and anticancer activity evaluation of some novel acridine derivatives. 2010

Sham M Sondhi, and Jaiveer Singh, and Reshma Rani, and P P Gupta, and S K Agrawal, and A K Saxena
Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee 247667 UK, India. sondifcy@iitr.ernet.in

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.

UI MeSH Term Description Entries
D008297 Male Males
D002351 Carrageenan A water-soluble extractive mixture of sulfated polysaccharides from RED ALGAE. Chief sources are the Irish moss CHONDRUS CRISPUS (Carrageen), and Gigartina stellata. It is used as a stabilizer, for suspending COCOA in chocolate manufacture, and to clarify BEVERAGES. Carrageenin,iota-Carrageenan,kappa-Carrageenan,lambda-Carrageenan,iota Carrageenan,kappa Carrageenan,lambda Carrageenan
D004487 Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE. Dropsy,Hydrops,Anasarca
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000166 Acridines Compounds that include the structure of acridine. Acridine
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000893 Anti-Inflammatory Agents Substances that reduce or suppress INFLAMMATION. Anti-Inflammatory Agent,Antiinflammatory Agent,Agents, Anti-Inflammatory,Agents, Antiinflammatory,Anti-Inflammatories,Antiinflammatories,Antiinflammatory Agents,Agent, Anti-Inflammatory,Agent, Antiinflammatory,Agents, Anti Inflammatory,Anti Inflammatories,Anti Inflammatory Agent,Anti Inflammatory Agents
D000970 Antineoplastic Agents Substances that inhibit or prevent the proliferation of NEOPLASMS. Anticancer Agent,Antineoplastic,Antineoplastic Agent,Antineoplastic Drug,Antitumor Agent,Antitumor Drug,Cancer Chemotherapy Agent,Cancer Chemotherapy Drug,Anticancer Agents,Antineoplastic Drugs,Antineoplastics,Antitumor Agents,Antitumor Drugs,Cancer Chemotherapy Agents,Cancer Chemotherapy Drugs,Chemotherapeutic Anticancer Agents,Chemotherapeutic Anticancer Drug,Agent, Anticancer,Agent, Antineoplastic,Agent, Antitumor,Agent, Cancer Chemotherapy,Agents, Anticancer,Agents, Antineoplastic,Agents, Antitumor,Agents, Cancer Chemotherapy,Agents, Chemotherapeutic Anticancer,Chemotherapy Agent, Cancer,Chemotherapy Agents, Cancer,Chemotherapy Drug, Cancer,Chemotherapy Drugs, Cancer,Drug, Antineoplastic,Drug, Antitumor,Drug, Cancer Chemotherapy,Drug, Chemotherapeutic Anticancer,Drugs, Antineoplastic,Drugs, Antitumor,Drugs, Cancer Chemotherapy
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships

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