A series of novel N-Sulphonamidomethyl piperzinyl fluoroquinolones were synthesized and screened antiviral activity. Eight compounds were synthesized through modifying the N4-hydrogen of piperazine in fluoroquinolones with formaldehyde and sulphanomides by Mannich reactions. The structures of the synthesized compounds were characterized by means of their IR and 1H-NMR spectral data. Synthesized compounds were screened for antiviral activity against influenza A (H1N1, H3N2, H5N1) and influenza B viruses in MDCK cell culture. The antiHIV activities of the new compounds were screened for antiviral activity against replication of HIV-1(IIIB) in MT-4 cells. Cytotoxicity of the synthesized compounds was also tested in mock-infected MDCK and MT-4 cells. Compound CF-SD and CF-SDM inhibits the influenza A (H1N1) and compound GF-SDM inhibit the replication of influenza A (H5N1) and B in MDCK cells. All compounds displayed cytostatic propertity in MT-4 cells. Among the compounds tested, GF-SDM (CC50=39.44 μM) most toxic compound in this series.
In the present study, a few D ring substituted pyrazolecarboxamide derivatives were synthesized from the key intermediate 2,3-dihydrothiopyrano[3,2-c]thiochromen-4(5H)-one(2). In order to determine the structure-activity relationships, the pyrazolecarboxamide derivatives (7 a-m) were analyzed for anticancer activity and molecular docking studies were carried out against two cancer cell lines (HeLa and HCT116). The structures of all these compounds have treating been elucidated on the basis of their spectral data. We performed docking studies with the selective inhibitor proteins 4J96 (HeLa) and 5FGK (HCT 116). The binding energy of compound 7k (-9.6 Kcal/mol-HeLa and -10.1 Kcal/mol-HCT116) was found to be lower than that of all other pyrazole derivatives as well as standard doxorubicin. Furthermore, compound 7k was also found to be a promising anticancer agent against 4J96 and 5FGK cells, given its significant inhibitory effect [IC50=20.56μM (HeLa) and 18.19μM (HCT116)] compared to doxorubicin [IC50=21.32 μM (HeLa) and 19.58 μM (HCT116)]. Hence it is understood that, the pyrazole carboxamide derivatives (7k) has selectivity for inhibitor proteins having anticancer activity against HeLa and HCT116 compared with doxorubicin.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.