Benzocyclobutenes (BCBs) are of growing interest in materials and medicinal chemistry, although general routes for their provision remain underexplored. A modular, divergent, stereoselective Cu- Pd-catalyzed assembly/cyclization sequence allows the synthesis densely functionalized BCBs, from readily accessible imine, allene, diboron precursors. Preliminary results have identified enantioselecti...

Quinolines, an important class of potentially bioactive compounds, have been synthesized by treatment of O-aminoarylketones and carbonyl compounds utilizing niobium (V) chloride / polyethylenglycole(NbCl5.PEG) and niobium(V)chloride (NbCl5) as available and inexpensive catalysts. The quinoline derivatives were prepared in glycerol, an excellent solvent in terms of environmental impact, with hig...

A series of novel 10-N-substituted acridones, bearing alkyl side chains with tertiary amine groups at the terminal position, were designed, synthesized, and evaluated for the ability to enhance the potency of quinoline drugs against multidrug-resistant (MDR) Plasmodium falciparum malaria parasites. A number of acridone derivatives, with side chains bridged three or more carbon atoms apart betwe...

In the present work, novel 7-aryl-10, 11-dihydro-7H-chromeno [4, 3-b]quinoline-6, 8(9H, 12H)-dione derivatives were synthesized by oxidation of 7-aryl-8, 9, 10, 12-tetrahydro-7H-chromeno[4, 3-b]quinoline-6, 8-diones in the presence of silica sulfuric acid/NaNO2 with yields of 64-74%. Cytotoxic activity of synthesized compounds was assessed on three different human cancer cell lines (K562, LS180...

Targeted tricyclic quinolines were prepared from the corresponding aminoindazolic and indolic derivatives as starting materials using two comparative methods; conventional heating microwave irradiation. We noticed that syntheses of 5-amino-1-methylindazole 5-aminoindole abandoned due to their conversion fluorescent products one week after free contact with air acetone. As a result this finding,...

A new group of 4-(Imidazolylmethyl) quinoline derivatives possessing a methylsulfonyl COX-2 pharmacophore at the para position of the C-2 phenyl ring were designed and synthesized as selective COX-2 inhibitors and in-vitro anti breast cancer agents. In-vitro COX-1 and COX-2 inhibition studies showed that all the compounds were potent and selective inhibitors of the COX-2 isozyme with IC50 value...

A new group of 4-(Imidazolylmethyl) quinoline derivatives possessing a methylsulfonyl COX-2 pharmacophore at the para position of the C-2 phenyl ring were designed and synthesized as selective COX-2 inhibitors and in-vitro anti breast cancer agents. In-vitro COX-1 and COX-2 inhibition studies showed that all the compounds were potent and selective inhibitors of the COX-2 isozyme with IC50 value...

A new class of quinoline derivatives containing pyrazoline-5-one and pyrazole moiety (3a-j and 4a-j) have been synthesized by condensation of various oxobutyrates/pentane-2,4-dione derivatives with 8-quinolinoxyacetic acid hydrazide. Elemental analysis, IR, H NMR and mass spectral data support the structures of the newly synthesized compounds. The synthesized compounds have been evaluated for t...

A novel series of dihydropyrimidines (DHPMs) 4a-j; 2-oxopyran-3-carboxylate 7a,b; 1-amino-1,2-dihydropyridine-3-carboxylate 8; and 1,3,4-oxadiazole derivatives 12 with quinolinyl residues have been synthesized in fairly good yields. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. In vitro antimalarial evaluation of the synthesize...