Cytotoxic evaluation of substituted benzaldehydes.
Authors: Rodrigues, F.A.R.; Oliveira, A.C.A.; Cavalcanti, B.C.; Costa, P.M.; Pessoa, C.O.; Pinheiro, A.C.; De Souza, M.V.N. Source: European Chemical Bulletin, v. 3, p. 555-558, 2014. Publisher: Deuton-X Ltd. by support of Research Centre for Natural Sciences, Hungarian Academy of Sciences. Abstract A series of fifty-four commercial aldehydes have been synthesized and evaluated for their activity […]
Anti-Tuberculosis Evaluation and Conformational Study of N -Acylhydrazones Containing the Thiophene Nucleus.
Authors: Cardoso, L.N.F.; Bispo, M.L.F.; Kaiser, C.R.; Wardell, J.L.; Wardell, S.M.S.V.; Lourenço, M.C.S.; Bezerra, F.A.F.M.; Soares, R.P.P. Rocha, M.N.; De Souza, M.V.N. Source: Archiv der Pharmazie (Weinheim), v. 347, p. 432-448, 2014. Publisher: John Wiley & Sons Abstract A series of N-acylhydrazonyl-thienyl derivatives (compounds 2 and 3), mainly of the type 2-(aryl-CHNNHCOCH2)-thiene (2: aryl = substituted-phenyl; 3: […]
7-Chloro-4-(2-hydroxyethylamino)quinolin-1-ium chloride
Authors: Gama, I.L.; De Souza, M.V.N.; Wardell, J.L.; Tiekink, E.R.T. Source: Acta Crystallographica. Section E, v. 70, p. 385-386, 2014. Publisher: International Union of Crystallography Abstract In the title salt, C11H12ClN2O+·Cl–, the ten non-H atoms comprising the quinolinium residue are coplanar (r.m.s. deviation = 0.041 Å) and the hydroxyethyl group is approximately perpendicular to this plane […]
Biological Evaluation of Isoniazid Derivatives as an Anticancer Class
Authors: Rodrigues, F.A.R.; Oliveira, A.C.A.; Cavalcanti, B.C.; Pessoa, C.O.; Pinheiro, A.C.; De Souza, M.V.N. Source: Scientia Pharmaceutica, v. 84, p. 21-28, 2014. Publisher: Austrian Pharmaceutical Society Abstract A series of thirty-two isoniazid derivatives have been evaluated for their activity against four human cancer cell lines with potent cytotoxicity (IC50 ranging from 0.61 to 3.36 μg/mL). […]
Design, synthesis and biological evaluation of (E)-2-(2-arylhydrazinyl)quinoxalines, a promising and potent new class of anticancer agents
Authors: Rodrigues, F.A.R.; Bomfim, I.S.; Cavalcanti, B.C.; Pessoa, C.O.; Wardell, J.L.; Wardell, S.M.S.V.; Pinheiro, A.C.; Kaiser, C.R.; Nogueira, T.C.M.; Low, J.N.; Gomes, L.R.; De Souza, M.V.N. Source: Bioorganic & Medicinal Chemistry Letters (Print), v. 24, p. 934-939, 2014. Publisher: Elsevier Abstract A series of forty-seven quinoxaline derivatives, 2-(XYZC6H2CHN–NH)-quinoxalines, 1, have been synthesized and […]
2-[(E)-2-(3,4-Dichlorobenzylidene)hydrazin-1-yl]quinoxaline
Authors: Nogueira, T.C.M.; Pinheiro, A.C.; De Souza, M.V.N.; Wardell, J.L.; Tiekink, E.R.T. Source: Acta Crystallographica. Section E, v. 70, p. 125, 2014 Publisher: International Union of Crystallography Abstract The 21 non-H atoms of the title compound, C15H10Cl2N4, are almost planar (r.m.s. deviation = 0.032 Å); the conformation about the N=C bond [1.277 (6) Å] is E. In the […]
Biological evaluation of pyrazinamide derivatives as an anticancer class
Authors: Rodrigues, F.A.R.; Bomfim, I.S.; Cavalcanti, B.C.; Pessoa, C.O.; Pinheiro, A.C.; Lima, C.H.S.; De Souza, M.V.N. Source: European Chemical Bulletin, v. 3, p. 358-361-361, 2014. Publisher: Deuton-X Ltd. by support of Research Centre for Natural Sciences, Hungarian Academy of Sciences. Abstract A series of fifty one pyrazinyl derivatives have been synthesized and evaluated for their […]
Syntheses and Antimycobacterial Activities of [(2S,3R)-2-(Amino)-4- (Arenesulfonamido)-3-Hydroxy-1-Phenylbutane Derivatives.
Authors: Moreth, M.; Gomes, C.R.B.; Lourenço, M.C.; Soares, R.; Rocha, M.; Kaiser, C.R.; De Souza, M.V.N.; Wardell, S.M.S.V.; Wardell, J. Source: Medicinal Chemistry (Hilversum), v. 10, p. 189-200, 2014. Publisher: Bentham Science Abstract The syntheses of hydroxyethylsulfonamides, (2S,3R)-tert-butyl N-[4-(N-benzyl-4-R-phenylsulfonamido)-3- hydroxy-1-phenylbutan-2-yl]carbamates and (5) (2S,3R)-2-amino-4-[N-benzyl-4-R-benzenesulfonamido]-3-hydroxy-1- phenylbutane hydrochlorides (6), derived from (2S,3S)-Boc-phenylalanine epoxide, are reported. None of the compounds, […]
Mefloquine-Oxazolidine Derivatives: A New Class of Anticancer Agents
Authors: Rodrigues, F.A.R.; Bomfim, I.S.; Cavalcanti, B.C.; Pessoa, C.O.; Gonçalves, R.S.B.; Wardell, J.L.; Wardell, S.M.S.V.; De Souza, M.V.N. Source: Chemical Biology & Drug Design (Print), v. 83, p. 126-131, 2014. Publisher: John Wiley & Sons, Inc. Abstract A series of 23 racemic mefloquine–oxazolidine derivatives, 4-[3-(aryl)hexahydro[1,3]oxazolo[3,4-a]pyridin-1-yl]-2,8-bis(trifluoromethyl)quinolines, derived from (R*, S*)-(±)-mefloquine and arenealdehydes, have been evaluated […]
Synthesis and antitubercular evaluation of aryl substituted – 2 – oxazolines from L – amino acids
Authors: Souza, L.A.; Da Silva, E.T.; Lourenço, M.C.S.; De Souza, M.V.N. Source: Mediterranean Journal of Chemistry, v. 2(5), p. 648-657, 2014. Publisher: Astucia Group Abstract This paper describes the synthesis and the in vitro antibacterial activity of a series of twelve substituted aryl-2-oxazolines against Mycobacterium tuberculosis. Seven compounds showed activity and two compounds exhibited a […]
Crystal structures of mefloquine-oxazolidine derivatives, 4-[3-(halophenyl)hexahydro[1,3]oxazolo[3,4-a]pyridin-1-yl]- 2,8-bis(trifluoromethyl)quinolines.
Authors: Gonçalves,R.S.B.; De Souza, M.V.N.; Wardell, J.L.; Wardell, S.M.S.V. Source: Zeitschrift für Kristallographie, v. 228, p. 1-13, 2013. Publisher: De Gruyter Abstract Crystal structures are reported for five racemic 4-{3-(halophenyl)hexahydro[1,3]oxazolo[3,4-a]pyridin-1- yl}-2,8-bis(trifluoromethyl)quinolines, 2, namely (2: X = 2-F, 3-Br, 4-Cl, 4-Br and 4-F), prepared from mefloquine and XC6H5CHO. In each case, the compound crystallizes in the […]
Structures of Two Rotamers of the HCl Salt of 4-Methyl-2-[(1E)-[2-(quinolin-4-yl)hydrazin-1-ylidene]methyl]phenol: Different Supramolecular Arrays
Authors: Ferreira, M.L.; Milne, B.F.; De Souza, M.V.N.; Tiekink, E.R.T.; Wardell, J.L.; Wardell, S.M.S.V. Source: Journal of Chemical Crystallography, v. 44, p. 36-41, 2013. Publisher: Springer International Publishing AG Abstract Crystallography reveals the rotomer in the salt isolated from EtOH solution has an anti disposition of the OH and imine-NH hydrogen atoms while that from EtOCH2CH2OH […]
