Naphthazarin derivatives (VI): synthesis, inhibitory effect on DNA topoisomerase-I and antiproliferative activity of 2- or 6-(1-oxyiminoalkyl)-5,8-dimethoxy-1,4-naphthoquinones.

abstract：:Diverse biological activities have been found in compounds having a quinazolinone ring system. A large number of 4(3H)-quinazolinones, in particular those possessing 2-alkyl-3-aryl, 2,3-dialkyl, and 2-alkyl-3-amino substitution, have been evaluated for pharmacological activity. On the other hand, thiazolidone derivati...

journal_title：Archiv der Pharmazie

authors： el-Feky SA,Abd el-Samii ZK

更新日期：1991-06-01 00:00:00

abstract：:Various aryl 1-pyrryl sulfones were synthesized and tested as inhibitors of HIV-1. 2-Nitrophenyl-2-ethoxycarbonyl-1-pyrryl sulfone, the most active among test derivatives, was selected as lead compound of the aryl pyrryl sulfone series. The in vitro anti-HIV-1 activity and cytotoxicity of 41 compounds is reported. Som...

journal_title：Archiv der Pharmazie

authors： Artico M,Silvestri R,Stefancich G,Massa S,Pagnozzi E,Musu D,Scintu F,Pinna E,Tinti E,La Colla P

更新日期：1995-03-01 00:00:00

abstract：:New series of perimidine derivatives and fused perimidines were derived from the reaction of ketene aminals 1 and 2 with diazotized anilines or hydrazonoyl chlorides. In addition, 8,10-disubstituted-[1,2,4]triazolo[4,3-a]perimidines (20a-m) were prepared through the reaction of perimidine-2-thione (15) with hydrazonoy...

journal_title：Archiv der Pharmazie

authors： Farghaly TA,Mahmoud HK

更新日期：2013-05-01 00:00:00

abstract：:A series of homochiral 7-substituted 1-aminoindans was prepared by means of asymmetric reductive amination from racemic 7-substituted 1-indanones via E-imines and E-imine/enamine mixtures, respectively, and subjected to 5-hydroxytryptamine (5-HT) receptor subtype binding studies. The ee's of the title compounds were d...

journal_title：Archiv der Pharmazie

authors： Landsiedel-Maier D,Frahm AW

更新日期：1998-02-01 00:00:00

abstract：:Both 2-nitrooxymethyl-4-phenyl- (2) and 4-nitrooxymethylphenyl-1,4-dihydropyridines (3) represent new combinations of two different vasodilating structures. 2 could not be isolated due to its spontaneous lactonization. Derivatives of 3 were obtained via Hantzsch synthesis using nitrooxymethylated benzaldehydes. The in...

journal_title：Archiv der Pharmazie

authors： Lehmann J,Kahlich R,Meyer zum Gottesberge C,Fricke U

更新日期：1997-08-01 00:00:00

abstract：:The aim of this study was to develop a novel nanosize drug candidate for cancer therapy. For this purpose, (S)-methyl 2-[(7-hydroxy-2-oxo-4-phenyl-2H-chromen-8-yl)methyleneamino]-3-(1H-indol-3-yl)propanoate (ND3) was synthesized by the condensation reaction of 8-formyl-7-hydroxy-4-phenylcoumarin with l-tryptophan meth...

journal_title：Archiv der Pharmazie

authors： Budama-Kilinc Y,Kecel-Gunduz S,Ozdemir B,Bicak B,Akman G,Arvas B,Aydogan F,Yolacan C

更新日期：2020-11-01 00:00:00

abstract：:The butadiene derivatives 10a-c react with the oxa-bicyclooctanone 9 to give the cyclohexene annulated oxatropanes 11a-c. The acetoxyderivatives 11b and 11c can be transformed into the cyclohexadiene or benzene derivatives 13 and 12, respectively. 11a reacts with HN3 to afford the tricyclic oxazepanone 14 which can be...

journal_title：Archiv der Pharmazie

authors： Eiden F,Kainz A,Gebhard R

更新日期：1992-02-01 00:00:00

abstract：:The syntheses, conformational studies, and investigations on the estrogen receptor binding of [R/S-1-(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]platinum(II) complexes (1-PtL2, 2L = leaving groups) are described. A Strecker synthesis using the 2,6-dichloro-4-methoxybenzaldehyde, NaCN, and NH4Cl afforded the cyanoami...

journal_title：Archiv der Pharmazie

authors： Gust R,Lubczyk V,Schmidt K,Shihada U

更新日期：2001-03-01 00:00:00

abstract：:New resveratrol (trans-3,4',5-trihydroxystilbene) analogs were synthesized and screened for their in vitro cancer chemopreventive potential using various bioassays relevant for the prevention of carcinogenesis in humans: two assays to detect modulators of carcinogen metabolism (Cyp1A inhibition; determination of NAD(P...

journal_title：Archiv der Pharmazie

authors： Orsini F,Verotta L,Klimo K,Gerhäuser C

更新日期：2016-06-01 00:00:00

abstract：:Ten pyrazole derivatives were synthesized and evaluated for their ability to inhibit the replication of influenza virions. All the compounds were synthesized in good-to-excellent yield, and the structures were ascertained with the help of (1) H NMR, (13) C NMR, mass, and elemental analysis. Among the tested series, co...

journal_title：Archiv der Pharmazie

authors： Meng FJ,Sun T,Dong WZ,Li MH,Tuo ZZ

更新日期：2016-03-01 00:00:00

abstract：:Design, synthesis, and cytotoxic activity of amidine derivatives of melphalan are described and structure-activity relationships are discussed. Evaluation of the cytotoxicity of these compounds employing a MTT assay and inhibition of [(3)H]thymidine incorporation into DNA in both MDA-MB-231 and MCF-7 human breast canc...

journal_title：Archiv der Pharmazie

authors： Bielawska A,Bielawski K,Anchim T

更新日期：2007-05-01 00:00:00

abstract：:The synthesis of 4-Methoxyphenyl-[5-methyl-6-(2-(4-morpholinyl)-ethyl)-6H-thieno[2,3- b]pyrrol-4-yl)phenylmethanone (1), a thiophene analogue of the analgesic Pravadoline B, is described. Starting with the acetylprotected thienylhydrazine 2b compound 7 was obtained in a Fischer-analogue cyclication in two steps. Use o...

journal_title：Archiv der Pharmazie

authors： Binder D,Schnait H,Rovenszky F,Enzenhofer R,Stroissnig H

更新日期：1991-04-01 00:00:00

abstract：:A new series of 1,4-disubstituted phthalazinylpiperazine derivatives 7a-f, 12a-f and 20a-f were designed and synthesized in order to develop potent and selective antitumor agents. The target compounds were screened for their cytotoxic activities against A549, HT-29 and MDA-MB-231 cancer cell lines in vitro. Among them...

journal_title：Archiv der Pharmazie

authors： Liu Y,Zhang S,Li Y,Wang J,Song Y,Gong P

更新日期：2012-04-01 00:00:00

abstract：:Inhibition of 5-lipoxygenase by anthralin (1) and 41 derivatives is determined: the acids 38 and 39, the lactones 40-42 and 9-anthrone (8) are the most potent inhibitors, the lactone 41 reaching the efficacy of nordihydroguaiaretic acid (NDGA). The results were correlated with the hydrophilic/lipophilic balance of the...

journal_title：Archiv der Pharmazie

authors： Tanzer H,Braun C,Seidel M,Wiegrebe W

更新日期：1991-11-01 00:00:00

abstract：:A new series of 16 6-chloro-1,1-dioxo-7-{4-[(4-R(1)-phenyl)imino]-4H-3,1-benzoxazin-2-yl}-3-(substituted amino)-1,4,2-benzodithiazines 7-22 was prepared in order to evaluate the cytotoxic activity against six human cancer cell lines. The structures of the new compounds were confirmed by IR, (1)H-, and (13)C-NMR, eleme...

journal_title：Archiv der Pharmazie

authors： Pomarnacka E,Kornicka A,Kuchnio A,Heinrichs M,Grünert R,Gdaniec M,Bednarski PJ

更新日期：2011-07-01 00:00:00

abstract：:N-Methoxyquinolinium salts 3 are prepared as potential cardiotonic agents by alkylation of the corresponding N-oxides 2 synthesized by two different methods. 1. Oxidation of some quinoline derivatives 1 using 30% H2O2 or 3-chloroperbenzoic acid. 2. Nitration of the quinoline-N-oxides 2a, 2c, and 2m. Preparation of 2h ...

journal_title：Archiv der Pharmazie

authors： Bünz C,Heber D,Ravens U

更新日期：1993-04-01 00:00:00

abstract：:The pyrrolidino enaminones, with the carboxylic acid chain fixed at the nitrogen, inhibit cyclooxygenase more potently or selectively than 5-lipoxygenase. According to the structure-activity relationships discussed the potency depends significantly on the chain length of the carboxylic acid, the substitution pattern o...

journal_title：Archiv der Pharmazie

authors： Dannhardt G,Bauer A,Nowe U

更新日期：1997-03-01 00:00:00

abstract：:A series of novel N(1)-[5-(4-substituted phenyl)-1,3,4-thiadiazol-2-yl]-N(4)-(4-substituted benzaldehyde)-semicarbazone 1-12, N(1)-[5-(4-substituted phenyl)-1,3,4-thiadiazol-2-yl]-N(4)-[1-(4-substituted phenyl)ethanone]-semicarbazone 13-16, and N(1)-[5-(4-substituted phenyl)-1,3,4-thiadiazol-2-yl]-N(4)-[1-(4-substitut...

journal_title：Archiv der Pharmazie

authors： Rajak H,Deshmukh R,Aggarwal N,Kashaw S,Kharya MD,Mishra P

更新日期：2009-08-01 00:00:00

abstract：:Albumin binding for the enantiomers of four closely related N-methyl-5-phenyl-5-alkyl-barbiturates 1-4 was investigated for three different mammalian species by means of equilibrium dialysis. Lipid solubility (n-heptane/phosphate buffer distribution coefficient) increased stepwise by a factor of 56 from 1 to 4. Bovine...

journal_title：Archiv der Pharmazie

authors： Büch HP,Krug R,Knabe J

更新日期：1996-08-01 00:00:00

abstract：:The key step in the synthesis of the pharmacologically interesting 1-phenyltetrahydro-3-benzazepine skeleton is the Michael addition of (2-lithiophenyl)acetaldehyde acetals, which are generated in situ upon treatment of the bromo acetals 5a,b with n-butyllithium, to beta-nitrostyrene (6). The reductive ring closure of...

journal_title：Archiv der Pharmazie

authors： Wünsch B,Nerdinger S,Bauschke G,Höfner G

更新日期：1997-07-01 00:00:00

abstract：:Viral gastroenteritis is a serious viral infection which affects a large number of individuals around the world, most of them being children. The infection may occur due to different viruses, for example, coxsackievirus, adenovirus, and rotavirus. There is no available cure for such infections, and the treatment mainl...

journal_title：Archiv der Pharmazie

authors： Mohamed MS,Abd El-Hameed RH,Sayed AI,Soror SH

更新日期：2015-03-01 00:00:00

abstract：:Series of N-(4-substitutedphenyl)-4-(1-methyl (or 1,2-dimethyl)-4-oxo-1,2-dihydroquinazolin-3(4H)-yl)-alkanamides (5a-j) and 4-chloro-N'-((1-methyl (or 1,2-dimethyl)-4-oxo-1,2-dihydroquinazolin-3(4H)-yl)-alkaloyl)benzohydrazides (6a-f) were designed based on the previously reported essential structural features for an...

journal_title：Archiv der Pharmazie

authors： Noureldin NA,Kothayer H,Lashine EM,Baraka MM,El-Eraky W,Awdan SA

更新日期：2017-02-01 00:00:00

abstract：:A 3D pharmacophore model predicting anticonvulsant activity was obtained for a series of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives recently disclosed as a new class of noncompetitive AMPA receptor antagonists. The training set included 17 compounds with varying potency against audiogenic seizures in DBA...

journal_title：Archiv der Pharmazie

authors： De Luca L,Gitto R,Barreca ML,Caruso R,Quartarone S,Citraro R,De Sarro G,Chimirri A

更新日期：2006-07-01 00:00:00

abstract：:This paper describes the use of the multivariate image analysis-quantitative structure-activity relationship (MIA-QSAR) methodology, which is a method capable of relating chemical structures with their biological activities. This in silico method has been shown to be extremely reliable and provides excellent results, ...

journal_title：Archiv der Pharmazie

authors： Bitencourt M,Freitas MP,Rittner R

更新日期：2012-09-01 00:00:00

abstract：:The ongoing interest in very efficient systems for the imitation of cytochrome P-450-dependent monooxygenase reactions, consisting of metalloporphyrin and oxygen donor, prompted us to develop a method to compare the catalytic activity of soluble metalloporphyrins with those which have been immobilised on different sil...

journal_title：Archiv der Pharmazie

authors： Lübbe AN,Rickerts B,Duchstein HJ

更新日期：2006-12-01 00:00:00

abstract：:In an attempt to find a new class of antibacterial agents, we have synthesized thirty new coumarin (2H-benzopyran-2-one) analogues. These derivatives include substituted azetidin-2-ones (beta-lactam) 3a-f, pyrrolidin-2-ones 4a-f, 2H-1,3,4-oxadiazoles 5a-f, and thiazolidin-4-ones 6a-f attached to 4-phenyl-2H-benzopyran...

journal_title：Archiv der Pharmazie

authors： Hassan GS,Farag NA,Hegazy GH,Arafa RK

更新日期：2008-11-01 00:00:00

abstract：:A series of benzamide derivatives possessing potent dopamine D2 , serotonin 5-HT1A , and 5-HT2A receptor properties were synthesized and evaluated as potential antipsychotics. Among them, 5-(4-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)butoxy)-N-cyclopropyl-2-fluorobenzamide (4k) held the best pharmacological profile....

journal_title：Archiv der Pharmazie

authors： Xu M,Guo S,Yang F,Wang Y,Wu C,Jiang X,Zhao Q,Chen W,Tian G,Zhu F,Xie Y,Hu T,Wang Z,He Y,Shen J

更新日期：2019-04-01 00:00:00

abstract：:Three ketomethylene pseudodideptide analogues [(S)Lys psi(COCH2)(R and S)Phe (14 or 15 and 15 or 14) and (S)Lys psi(COCH2)(xi Trp (19)] of natural arphamenine A [(S)Arg psi(COCH2(R,S)Phe (1)] were easily prepared by a route involving two successive main reactions: a malonic ester alkylation with Z-protected lysine iod...

journal_title：Archiv der Pharmazie

authors： García-López MT,González-Muñiz R,Hartoa JR,Gómez-Monterrey I,Pérez C,De Ceballos ML,López E,Del Río J

更新日期：1992-01-01 00:00:00

abstract：:We report in this work the synthesis, cytotoxicity, and antimicrobial activity of ([1,2,4]triazolo[1,5-c]quinazolin-2-ylthio)carboxylic acid amides 4-7 in connection with our previous research in the preparation of triazoloquinazoline derivatives. Due to simplicity, general availability of starting materials, and high...

journal_title：Archiv der Pharmazie

authors： Antipenko LN,Karpenko AV,Kovalenko SI,Katsev AM,Komarovska-Porokhnyavets EZ,Novikov VP

更新日期：2009-11-01 00:00:00

abstract：:The influence of RE 1492 on the storage of red blood cells (RBCs) was investigated. RE 1492 (c > or = 50 mumol/L) induces the formation of cup cells and hence delays the appearance of echinocytes and crenated spheres in the blood. A concentration of 50 mumol/L RE 1492 drops hemolysis by 50%. At this concentration afte...

journal_title：Archiv der Pharmazie

authors： Rehse K,Müller S

更新日期：1995-04-01 00:00:00