Design, synthesis and potential anti-proliferative activity of some novel 4-aminoquinoline derivatives

Novel nineteen compounds based on a 4-aminoquinoline scaffold were designed and synthesized as potential anti-proliferative agents. The new compounds were N-substituted at the 4-position by aryl or heteroaryl 1-9, quinolin-3-yl 10, 2-methylquinolin-3-yl 11, thiazol-2-yl 12, and dapsone moieties 13, 14 and 18. Bis-compounds 15, 16 and 19 were also synthesized to assess their biological activity. All the newly synthesized comounds were tested for in vitro antiproliferative activity against the MCF-7 breast cancer cell line. Seventeen of the novel compounds showed higher activity than the reference drug doxorubicin. The corresponding 7-(trifluoromethyl)-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine 1, N-(7-(trifluoromethyl)quinolin-4-yl)quinolin-3-amine (10), 2-methyl-N-(7-trifluorome-thyl)quinolin-4-yl)quinolin-3-amine (11) and N-(4-(4-aminophenylsulf-onyl)phenyl)-7-chloroquinolin-4-amine (13) were almost twice to thrice as potent as doxorubicin

Novel thiophene derivatives with sulfonamide, isoxazole, benzothiazole, quinoline and anthracene moieties as potential anticancer agents

A novel series of thiophenes having biologically active sulfonamide (2-11), 3-methylisoxazole (12), 4-methoxybenzo[d]thiazole (13), quinoline (14, 15), benzoylphenylamino (16) and anthracene-9,10-dione (17) moieties were prepared. Structures of the newly synthesized compounds were established by elemental analysis and spectral data. All newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7). Most of the screened compounds showed cytotoxic activities compared to doxorubicin as a positive control. Compounds 6, 7, 9 and 13 (IC50 values 10.25, 9.70, 9.55 and 9.39 µmol L–1 revealed higher cytotoxic activities than that of doxorubicin (IC50 = 32.00 µmol L). Also, compounds 5, 8 and 10 were found nearly as active as doxorubicin (IC50 values 28.85, 23.48 and 27.51 µmol L–1)

(3Z,3′Z)-3,3′-(3,5-Dimethyl­furan-2,4-diyl)bis­(4-hy­droxy­pent-3-en-2-one)

In the title mol­ecule, C16H20O5, the two 4-hy­droxy­pent-3-en-2-one units are essentially planar, with r.m.s. deviations of 0.0183 (2) and 0.0134 (2) Å for the non-H atoms, and make dihedral angles of 81.20 (10) and 84.44 (10)° with the central furan ring. The dihedral angle between these two side units is 22.06 (9)°. Two intra­molecular O—H⋯O hydrogen bonds generate two S(6) ring motifs. A weak inter­molecular C—H⋯O inter­action is also observed

New Mixed Ligand Complexes of Ditertiary Phosphanes with Ni(II) Alkylxanthates

Mixed Iigand complexes of Ni(II) with alkylxanthates and ditertiary phosphanes of the composition Ni(ROCSSb(diphoshhave been prepared, where R = methyl, ethyl, propyl, butyl, and cyclohexyl and diphos = bis(diphenylphosphino)ethane (dpe) and bis- (diphenylphosphino)butane (dpb). The newly prepared compounds were characterized on the basis of chemical analyses, infrared and electronic spectra, lH-NMR, molar conductance, and thermal analysis. A square planar structure was proposed for the complexes

1-(3-Ethyl­phen­yl)-4,6-dimethyl-2-oxo-1,2-dihydro­pyridine-3-carbonitrile

In the title compound, C16H16N2O, the essentially planar 1,2-dihydro­pyridine ring [maximum deviation = 0.021 (1) Å] makes a dihedral angle of 85.33 (8)° with the benzene ring. In the crystal, mol­ecules are linked into a chain along the b axis via C—H⋯O inter­actions

(E)-3-Dimethyl­amino-1-(2,5-dimethyl­thio­phen-3-yl)prop-2-en-1-one

In the title compound, C11H15NOS, the 3-(dimethyl­amino)­prop-2-en-1-one unit is approximately planar [maximum deviation = 0.0975 (14) Å] and its mean plane of seven non-H atoms makes a dihedral angle of 6.96 (10)° with the thio­phene ring. In the crystal, mol­ecules are linked by pairs of C—H⋯O hydrogen bonds into inversion dimers with R 2 2(14) ring motifs. The dimers are stacked along the c axis through C—H⋯π inter­actions. The two methyl groups, attached to the thio­phene ring and the amino N atom, are each disordered over two orientations, with site-occupancy ratios of 0.59 (4):0.41 (4) and 0.74 (4):0.26 (4), respectively

(E)-4-Amino-N-(1,2-dihydro­pyridin-2-yl­idene)benzene­sulfonamide nitro­methane monosolvate

In the title solvate, C11H11N3O2S·CH3NO2, the dihedral angle between the benzene ring and the N-containing ring is 85.94 (11)°, and an approximate V shape arises for the sulfonamide mol­ecule. In the crystal, N—H⋯O and N—H⋯N hydrogen bonds and weak C—H⋯O inter­actions link the sulfonamide mol­ecules into a three-dimensional network. The nitro­methane solvent mol­ecules are located in the inter­stitial sites in the sulfonamide network

Role of nanoparticles in diagnosis and management of parasitic diseases: Review article

Background: An extensive class of materials, nanoparticles (NPs) include particulate compounds with a minimum diameter of 100 nanometers (nm). This is because of their tiny size and huge surface area, which allows them to traverse the blood-brain barrier, enter the respiratory system and be adsorbable through endothelial cells. Today, nanoparticles for drug administration are being studied to increase their sustained release, intracellular penetrability as well as bioavailability, due to the constant development and innovation of nanomedicine.Objective: To determine how nanoparticles can help diagnose and treat parasitic diseases.Conclusion: Nanoparticles could be conjugated with proteins and immunoglobulins that could help in specific diagnosis of several parasitic diseases, in addition, improved efficacy and reduced harmful side effects can be achieved by immobilizing antiparasitic medicines on or inside nanomaterials