Novel ametantrone-amsacrine related hybrids as topoisomerase IIβ poisons and cytotoxic agents.

abstract：:Mono-Mannich bases, 1-aryl-3-phenethylamino-1-propanone hydrochlorides, 1a, 2a, 3a, 4a, 5a, 6a, 7a, 8a, 9a, and semi-cyclic mono-Mannich bases, 3-aroyl-4-aryl-1-phenethyl-4-piperidinols, 1b, 2b, 3b, 4b, 5b, 6b, 7b, 8b, 9b, were synthesized by a non-classical Mannich reaction. The aryl part was: C(6)H(5 )for 1a, 1b; 4-...

journal_title：Archiv der Pharmazie

authors： Mete E,Ozelgul C,Kazaz C,Yurdakul D,Sahin F,Inci Gul H

更新日期：2010-05-01 00:00:00

abstract：:Cycloaddition reactions of the nitrilimines 4-6 with N-arylmaleimides 7 and acrylamide (11) yield the pyrrolopyrazole derivatives 8-10 and 2-pyrazolines 12, respectively, in excellent yield. The regioselectivity and biological activities of some of the new compounds were investigated. ...

journal_title：Archiv der Pharmazie

authors： Ead HA,Hassaneen HM,Abdallah MA,Mousa HA

更新日期：1991-01-01 00:00:00

abstract：:A series of cis-restricted 4,5-diaryl-3-aminopyrazole derivatives were synthesized and tested for their cytotoxic activity in vitro against five human cancer cell lines (K562, ECA-109, A549, SMMC-7721, and PC-3). Compounds 5a, 5b, 5d, and 6b showed potent cytotoxicity against all tested cell lines. Primary mechanism r...

journal_title：Archiv der Pharmazie

authors： Liu T,Cui R,Chen J,Zhang J,He Q,Yang B,Hu Y

更新日期：2011-05-01 00:00:00

abstract：:Stress is implicated in the pathogenesis of numerous disorders such as cardiovascular diseases or neurodegeneration. The extensive overlap between diseases attributed to stress and oxidative damage is indicative of their potential relationship. We hereby study the influence of alpha-tocopherol (alpha-toc) on the devel...

journal_title：Archiv der Pharmazie

authors： Tsiakitzis K,Kourounakis AP,Tani E,Rekka EA,Kourounakis PN

更新日期：2005-07-01 00:00:00

abstract：:A series of 5-amino-3-methylisoxazole-4-carboxylic acid amides has been prepared by condensation of 5-amino-3-methylisoxazole-4-carboxylic acid with ethyl chloroformate. The resulting mixed anhydride undergoes condensation with appropriate phenylamides to form the corresponding amides 6-16. The compounds obtained were...

journal_title：Archiv der Pharmazie

authors： Ryng S,Zimecki M,Sonnenberg Z,Mokrosz MJ

更新日期：1999-05-01 00:00:00

abstract：:Although a large number of pharmaceutical therapies are available to treat cardiovascular diseases like heart failure, in many medical conditions treatment is still not optimal and, therefore, the need for innovative, safe and efficacious drugs is still very high in this indication. Biomarkers are an important tool in...

journal_title：Archiv der Pharmazie

authors： Kramer F,Dinh W

更新日期：2016-06-01 00:00:00

abstract：:In this study, some novel cyanine dyes, 1, 3, and 5-15, were synthesized by a one-pot step reaction of pyridinium salts 2 and/or 4 with benzenaminium salt 1. N-{[1-Chloro-3,4-dihydronaphthalen-2-yl)methylene]benzenaminium} chloride 1 was obtained by the reaction of α-tetralone with Vilsmeier-Haack reagent, followed by...

journal_title：Archiv der Pharmazie

authors： Fadda AA,Tawfik EH,Abdel-Motaal M,Selim YA

更新日期：2020-11-10 00:00:00

abstract：:Synthesis of some new derivatives of 2-aryl-4-oxo-1-(4-quinazolyl)quinazolines is described. Methyl N-(4-quinazolyl)anthranilate was allowed to react with phenyl iso(thio)cyanate to give 3-phenyl-1-(4-quinazolyl)-1, 2, 3, 4-tetrahydro-2, 4-dioxo- and 4-oxo-2-thioxoquinazolines (3a and 3b respectively) Alternatively, a...

journal_title：Archiv der Pharmazie

authors： Gineinah MM,El-Sherbeny MA,Nasr MN,Maarouf AR

更新日期：2002-01-01 00:00:00

abstract：:Polyketide-derived macrolactones like zearalenone (1), zearalane (2) or curvularin (3) display a wide range of interesting pharmacological activities. Here, we present a short and efficient approach towards this class of natural products by a combination of the Sonogashira and Mitsunobu reactions. The resulting lacton...

journal_title：Archiv der Pharmazie

authors： Krauss J,Unterreitmeier D,Neudert C,Bracher F

更新日期：2005-12-01 00:00:00

abstract：:A series of 7, 7'-alkylene-bridged dimers(7a-e) of the benz [d]indolo[3, 2-f]azecine derivative LE300 was synthesized. Affinity and functional activity at dopamine D(1) and D(2) receptors were estimated by radioligand binding and a functional Ca(2+) assay. All the new bivalent ligands showed significant binding affini...

journal_title：Archiv der Pharmazie

authors： Abadi AH,Lankow S,Hoefgen B,Decker M,Kassack MU,Lehmann J

更新日期：2002-08-01 00:00:00

abstract：:Three novel series of quinoline derivatives have been prepared by cyclization of the intermediate 3-(1,3-dioxolan-2-yl)-2-substituted thiocarbamoyl-hydrazinoquinolines with different alpha-halocarbonyl compounds. These series are: 3-(1,3-dioxolan-2-yl)-2-(3-substituted-4-phenylthiazolin-2-y lidene) hydrazinoquinolines...

journal_title：Archiv der Pharmazie

authors： Farghaly AM,Habib NS,Khalil MA,el-Sayed OA,Bistawroos AE

更新日期：1990-04-01 00:00:00

abstract：:A series of novel N-(4,5-dihydroimidazol-2-yl)-1,3-dihydrobenzimidazole derivatives 2a-d, 3a-d and 4a-p were prepared and their structure was determined by IR and NMR spectroscopic data as well as X-ray analysis of carbonitrile 2a. The compounds were studied as potential inhibitors of the human blood platelet aggregat...

journal_title：Archiv der Pharmazie

authors： Saczewski F,Debowski T,Petrusewicz J,Trzeciak H,Krzystanek E,Krzystanek M,Gdaniec M,Nowakowska E

更新日期：1998-07-01 00:00:00

abstract：:Synthesis of 2-chloro-1,1-dimethylethyl and 2-chloro-2,2-dimethylethyl analogues of ifosfamide was performed via aziridine intermediate. In vitro metabolic activation showed that both compounds are metabolised at a rate similar to the parent drug. However, their anticancer activity against L1210 leukaemia in mice was ...

journal_title：Archiv der Pharmazie

authors： Misiura K,Kardacka K,Kusnierczyk H

更新日期：2001-09-01 00:00:00

abstract：:A series of eperezolid analogs with glycinyl substitutions were prepared and their antibacterial activities were studied against a panel of susceptible and resistant Gram-positive bacteria. The compounds with N-arylacyl or N-heteroarylacyl glycinyl structural units showed good antibacterial activities. The compounds 1...

journal_title：Archiv der Pharmazie

authors： Wang XJ,Wu N,Du GJ,Zhao SQ,Yan M,Gu LQ

更新日期：2009-07-01 00:00:00

abstract：:The complex of lanthanum (III) was synthesized reacting the respective inorganic salt with 5-aminoorotic acid in amounts equal to the metal:ligand molar ratio of 1:3. The complex was prepared by adding an aqueous solution of lanthanum (III) nitrate to an aqueous solution of the ligand, subsequently raising the pH of t...

journal_title：Archiv der Pharmazie

authors： Kostova I,Rastogi VK,Kiefer W,Kostovski A

更新日期：2006-11-01 00:00:00

abstract：:Chemical modification of cinnoxacin was studied with the aim of improving its antibacterial activity and spectrum. A series of 4-imino-1, 4-dihydrocinnoline-3-carboxylic acid derivatives was synthesized and their in vitro antibacterial activity was evaluated. These derivatives were designed as isosteric analogues of f...

journal_title：Archiv der Pharmazie

authors： Stańczak A,Ochocki Z,Martynowski D,Główka M,Nawrot E

更新日期：2003-03-01 00:00:00

abstract：:A series of 4-amino-7,8-dimethoxy-5H-pyrimido[5,4-b]indole derivatives has been synthesized. These compounds resemble carbazeram and other pyridazino compounds with activity in the cardiovascular system. Some of these new compounds possess inotropic activity (Table 2), with a complementary effect on the inhibition of ...

journal_title：Archiv der Pharmazie

authors： Monge A,Martínez-Crespo FJ,Villanueva MA,Font M,Santiago E,Martínez de Irujo JJ,Alberdi E,López-Unzu MJ,Cenarruzabeitia E,Castiella E

更新日期：1993-11-01 00:00:00

abstract：:The present work describes the synthesis and antifungal evaluation of new 5-arylidene-(Z)-2-dimethylamino-1,3-thiazol-4-ones 4a-f, obtained by the reaction of aromatic aldehydes 1 and rhodanine 2 followed by treatment with DMF. All compounds were tested against a panel of yeasts, hialohyphomycetes, and dermatophytes u...

journal_title：Archiv der Pharmazie

authors： Insuasty B,Gutiérrez A,Quiroga J,Abonia R,Nogueras M,Cobo J,Svetaz L,Raimondi M,Zacchino S

更新日期：2010-01-01 00:00:00

abstract：:Michael-type reaction of compounds of type 9 were studied. Addition reactions with acrolein and methyl vinyl ketone, respectively, lead--depending on the conditions--to pyridoindoles of type 16 and 14 and/or to tetrahydrocarbazoles of type 17 and 15. With Triton B compounds 15 undergo retro-Michael-type elimination of...

journal_title：Archiv der Pharmazie

authors： Mahboobi S,Burgemeister T,Kastner F

更新日期：1995-01-01 00:00:00

abstract：:Synthesis of a new series of 1beta-methylcarbapenems with a substituted oxadiazolopyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of the substituent on the oxadiazole ring investigated. In particular, compounds 13...

journal_title：Archiv der Pharmazie

authors： Oh CH,Dong HG,Lee JS,Lee SC,Hong JH,Cho JH

更新日期：2003-12-01 00:00:00

abstract：:Based upon molecular modeling, the pharmacophore of potential inhibitors of p38 MAPK (mitogen-activated protein kinases) is discussed and the predictive binding affinities are calculated. Syntheses of original diarylimidazo[2,1-a]phthalazines obtained by Suzuki coupling are described. ...

journal_title：Archiv der Pharmazie

authors： Mavel S,Thery I,Gueiffier A

更新日期：2002-01-01 00:00:00

abstract：:A series of bis(benzo[g]indoles) bridged by CX-(CH2)nN(Me)(CH2)n-CX (X = O, S, H2; n = 2,3) was synthesized as bifunctional antitumor agents and evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. The parent compounds 2a,b exhibited a good level of activity and de...

journal_title：Archiv der Pharmazie

authors： Pinna GA,Pirisi MA,Grella GE,Gherardini L,Mussinu JM,Paglietti G,Ferrari AM,Rastelli G

更新日期：2001-11-01 00:00:00

abstract：:New 5-(2-arylethenyl)-1, 2, 4-triazine N-oxide and N, N'-dioxide derivatives were synthesized in order to obtain compounds as selective hypoxic cell cytotoxins. The desired products were obtained when the 5-methyl heterocycle reacted with the corresponding iminium electrophiles. The new compounds were tested for their...

journal_title：Archiv der Pharmazie

authors： Cerecetto H,González M,Risso M,Saenz P,Olea-Azar C,Bruno AM,Azqueta A,De Ceráin AL,Monge A

更新日期：2004-05-01 00:00:00

abstract：:New analogues of nifedipine, in which the 2-nitrophenyl group at position 4 is replaced by a 1-methyl-5-nitro-2-imidazolyl substituent, were synthesized. The symmetrical dialkyl 1, 4-dihydro-2, 6-dimethyl-4-(1-methyl-5-nitro-2-imidazolyl)-3, 5-pyridinedicarboxylates were prepared by a classical Hantzsch condensation. ...

journal_title：Archiv der Pharmazie

authors： Miri R,Javidnia K,Kebriaie-Zadeh A,Niknahad H,Shaygani N,Semnanian S,Shafiee A

更新日期：2003-09-01 00:00:00

abstract：:Fourteen new 1-[(N, N-disubstituted thiocarbamoylthio)acetyl]-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives (7a-n) were synthesised by reacting 1-(chloroacetyl)-3-(2-thienyl)-5-aryl-2-pyrazolines (5a-g) and appropriate sodium salts of N, N-disubstituted dithiocarbamoic acids (6a, b). The structures of the synthesised ...

journal_title：Archiv der Pharmazie

authors： Turan-Zitouni G,Ozdemir A,Güven K

更新日期：2005-03-01 00:00:00

abstract：:Novel sulfur-containing glutethimide derivatives, substituted with either thiol or methylsulfide groups in the ortho/para positions of the aromatic ring, were synthesized and tested for both human placental aromatase and bovine adrenocortical desmolase inhibitory activities. The synthesis was achieved by the chlorosul...

journal_title：Archiv der Pharmazie

authors： Bednarski PJ,Hartmann RW

更新日期：1993-07-01 00:00:00

abstract：:Several chloro- and iodo-lignanolides have been obtained by direct halogenation of aromatic rings from yatein and 4'-O-demethylyatein. They were assayed as antineoplastics, in order to check the influence in the activity of substitution in both aromatic rings. Although these compounds show a modest antineoplastic acti...

journal_title：Archiv der Pharmazie

authors： Medarde M,Peláez-Lamamié de Clairac R,López JL,Grávalos DG,San Feliciano S

更新日期：1995-09-01 00:00:00

abstract：:The marine fatty acid (+/-)-2-methoxytetradecanoic acid was synthesized in two steps (71% overall yield) starting from commercially available methyl-2-hydroxy-tetradecanoate. The title compound was antifungal against Candida albicans (ATCC 14053) in RPMI medium and Aspergillus niger (ATCC 16404) and Cryptococcus neofo...

journal_title：Archiv der Pharmazie

authors： Carballeira NM,Ortiz D,Parang K,Sardari S

更新日期：2004-03-01 00:00:00

abstract：:36 Novel heterocyclic chalcone derivatives were synthesized and tested for their anti-bacterial activity. Some compounds presented good anti-microbial activities against Gram-positive bacteria (including the multidrug-resistant clinical isolates). This class of compounds presented high potency against Streptococcus mu...

journal_title：Archiv der Pharmazie

authors： Zheng CJ,Jiang SM,Chen ZH,Ye BJ,Piao HR

更新日期：2011-10-01 00:00:00

abstract：:To identify new agents for the treatment of American cutaneous leishmaniasis, a series of eight 1,4-bis(substituted benzalhydrazino)phthalazines was evaluated against Leishmania braziliensis and Leishmania mexicana parasites. These compounds represent a disubstituted version of the 1-chloro-4-(monoaryl/heteroarylhydra...

journal_title：Archiv der Pharmazie

authors： Romero AH,Rodríguez N,Oviedo H,Lopez SE

更新日期：2019-06-01 00:00:00