Does [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]- dichloro-platinum(II) act as an immune response modifier? Part III: Progressively growing MXT-M-3,2 breast cancer stimulates the proliferation of phagocytes in B6D2F1 mice.

abstract：:2-Acetyl-(6-picolyl)-4N-substituted thiosemicarbazones and their copper(II) complexes were shown to be potent antineoplastic and cytotoxic agents against murine and human cultured cells. Numerous derivatives were as active against solid tumor growth as clinically useful agents. The agents inhibited L1210 DNA and RNA s...

journal_title：Archiv der Pharmazie

authors： Miller MC 3rd,Bastow KF,Stineman CN,Vance JR,Song SC,West DX,Hall IH

更新日期：1998-04-01 00:00:00

abstract：:Permeability glycoprotein (P-gp) is involved in the pathology of various diseases including cancer and epilepsy, mainly through the translocation of some medicines across the cell membrane. Here, we employed image-based quantitative structure-activity relationship (QSAR) models to predict the P-gp inhibitory activity ...

journal_title：Archiv der Pharmazie

authors： Shayanfar S,Shayanfar A,Ghandadi M

更新日期：2016-02-01 00:00:00

abstract：:Salicylamide amino acid conjugates were prepared utilizing 5-formyl-, 5-dicyanoethenyl-, and 5-nitroethenylsalicylic acid. 5-Substituted salicylanilides were treated with glycine and formaldehyde in a Mannich type reaction affording the corresponding 3-(N-glycino)salicylanilides. The reactions of anilines with pyrans ...

journal_title：Archiv der Pharmazie

authors： Nawwar GA

更新日期：1994-04-01 00:00:00

abstract：:The combined effects of amino acid antagonists with proven or potential inhibitory activities on aminoacyl-tRNA synthetases were investigated on the murine leukemic cell line P388 D1. As the best result a summation of the antiproliferative effects was observed. Combinations with established cytostatic agents like plat...

journal_title：Archiv der Pharmazie

authors： Laske R,Schönenberger H,Holler E

更新日期：1991-03-01 00:00:00

abstract：:A new class of acetamidomethylsulfonyl bis heterocycles-oxazolyl-1,3,4-oxadiazoles, -thiazolyl-1,3,4-oxadiazoles, and -imidazolyl-1,3,4-oxadiazoles were synthesized from the synthetic intermediates, methyl 2-((4-aryloxazol-2-ylcarbamoyl)methylsulfonyl)acetate, methyl 2-((4-arylthiazol-2-ylcarbamoyl)methylsulfonyl)acet...

journal_title：Archiv der Pharmazie

authors： Mahaboob Basha N,Lavanya G,Padmaja A,Padmavathi V

更新日期：2013-07-01 00:00:00

abstract：:JL 13 (5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b]- [1,5]benzoxazepine fumarate) and JL 3 (10-(4-methylpiperazin-1- yl)pyrido[4,3-b][1,4]benzothiazepine), two pyridobenzazepine derivatives structurally related to clozapine, were selected for further development. Due to their structural similarity to clozapine, t...

journal_title：Archiv der Pharmazie

authors： Liégeois JF,Zahid N,Bruhwyler J,Uetrecht J

更新日期：2000-03-01 00:00:00

abstract：:A number of novel pyridazinomorphinans have been synthesized by the inverse electron demand Diels-Alder reaction of various 3,6-disubstituted 1,2,4,5-tetrazines with enamines derived from dihydrocodeinone and with codeinone. Reduction of some of the pyridazinomorphinans did not furnish the expected pyrroloepoxymorphin...

journal_title：Archiv der Pharmazie

authors： Klindert T,Stroetmann I,Seitz G,Höfner G,Wanner KT,Frenzen G,Eckhoff B

更新日期：1997-06-01 00:00:00

abstract：:The histone deacetylase (HDAC) enzyme plays an important role in gene transcription. Inhibitors of histone deacetylases induce cell differentiation and suppress cell proliferation in tumor cells. Hydroxamates with rigid linker have displayed better inhibition profiles than those with linear and flexible aliphatic link...

journal_title：Archiv der Pharmazie

authors： Chakrabarty S,Jasmine,Bhadaliya C,Sinha BN,Mahesh A,Bai H,Blond SY,Jayaprakash V

更新日期：2010-03-01 00:00:00

abstract：:A series of 5-(o-tolyl)-1H-tetrazole derivatives were synthesized and evaluated for their anticonvulsant activities. 1-(2-Methylbenzyl)-5-(o-tolyl)-1H-tetrazole (3h) showed important anticonvulsant activity against the MES-induced seizures, as well as lower neurotoxicity with an ED50 value of 12.7 mg/kg and a TD50 val...

journal_title：Archiv der Pharmazie

authors： Dong S,Wang T,Wang H,Qian K,Zhang Z,Zuo Y,Luo G,Jin Y,Wang Z

更新日期：2017-05-01 00:00:00

abstract：:Paullones 3 and 4 with aminoalkyl side chains in 2- or 3-position were synthesized as derivatives of kenpaullone 1. Both 3 and 4 showed the characteristic CDK1-inhibitory activity of the paullones and a modest antiproliferative activity on cultured human tumor cell lines. Hence, 3 and 4 appear to be suitable tools for...

journal_title：Archiv der Pharmazie

authors： Wieking K,Knockaert M,Leost M,Zaharevitz DW,Meijer L,Kunick C

更新日期：2002-07-01 00:00:00

abstract：:The synthesis and odour properties of the new santalol analogue, methyl-beta-santalol, are described. The additional methyl group adjacent to the hydroxyl function of the standard molecule, beta-santalol, deprives the new compound of the sandalwood note. The synthesis and the odour evaluation of this compound supports...

journal_title：Archiv der Pharmazie

authors： Buchbauer G,Zechmeister-Machhart F,Weiss-Greiler P,Wolschann P

更新日期：1997-04-01 00:00:00

abstract：:Two new arylnaphthalide lignans, procumphthalide A (1) and 4-O-beta-D-glucopyranosyl-(1"'-->2")-beta-D-apiofuranosyldiphyllin, named procumbenoside B (2), along with cilinaphthalide B (3) and several other known compounds were isolated from the methanolic extracts of Justicia procumbens. By using NMR and other spectra...

journal_title：Archiv der Pharmazie

authors： Weng JR,Ko HH,Yeh TL,Lin HC,Lin CN

更新日期：2004-04-01 00:00:00

abstract：:The objective of this work was to develop a liver-specific antihepato carcinoma agent. A series of 5-fluorouracil / cholic acid conjugates (5-FU-cholic acid conjugates) were prepared and tested for their chemical characteristics and bio-distribution properties. The in-vitro stability trial showed 5-FU-cholic acid conj...

journal_title：Archiv der Pharmazie

authors： Qian S,Wu JB,Wu XC,Li J,Wu Y

更新日期：2009-09-01 00:00:00

abstract：:3'-Azidonucleosides 4 have been synthesized by condensation of silylated (Z)-5-ethylidenehydantoin and (Z)-5-benzylidenehydantoin with methyl 3-azido-5-O-tert-butyldiphenylsilyl-2,3-dideoxy-D-erythro-pento furanoside (3). The nucleosides 4 were deblocked on treatment with tetrabutylammonium fluoride. The ethylidene gr...

journal_title：Archiv der Pharmazie

authors： el-Barbary AA,Khodair AI,Pedersen EB

更新日期：1994-10-01 00:00:00

abstract：:A screening study was conducted to examine the effect of a series of synthesized pyrazoloquinoline derivatives on the growth of Leishmania donovani promastigotes. Sixteen compounds were tested, ten of which showed an inhibitory effect on the growth of promastigotes. Compound 1 demonstrated potent antileishmanial activ...

journal_title：Archiv der Pharmazie

authors： Al-Qahtani A,Siddiqui YM,Bekhit AA,El-Sayed OA,Aboul-Enein HY,Al-Ahdalb MN

更新日期：2005-10-01 00:00:00

abstract：:Gypsogenin (1) was obtained by acidic hydrolysis from its saponin. While the parent compound 1 acted as a selective inhibitor for butyrylcholinesterase (from equus) possessing a moderate mixed-type inhibition of the enzyme, Ki values as low as 2.67 ± 0.59 μM were determined for (3β,4α) 3-O-acetyl-olean-12-ene-23,28-di...

journal_title：Archiv der Pharmazie

authors： Heller L,Schwarz S,Weber BA,Csuk R

更新日期：2014-10-01 00:00:00

abstract：:Two series of amino-1,4-benzoquinones (AQ1-18) based on the structural analogs of plastoquinones were synthesized and the structure-activity relationship against chronic myelogenous leukemia activity was examined. All of the synthesized compounds were tested for their cytotoxic effects on different leukemic cell lines...

journal_title：Archiv der Pharmazie

authors： Ciftci HI,Bayrak N,Yıldırım H,Yıldız M,Radwan MO,Otsuka M,Fujita M,Tuyun AF

更新日期：2019-12-01 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：:The newly synthesized analogs of NAN-190 containing m-Cl and m-CF(3) substituents in the arylpiperazine moiety and their conformationally restricted counterparts showed a very high 5-HT(1A )receptor affinity. In the LLR test, the flexible compounds 4a and 5a displayed features of a partial agonist and agonist, respect...

journal_title：Archiv der Pharmazie

authors： Paluchowska MH,Bugno R,Charakchieva-Minol S,Bojarski AJ,Tatarczyńska E,Chojnacka-Wójcik E

更新日期：2006-09-01 00:00:00

abstract：:1-Acetylcarbazoles are readily converted to 3-desazacanthin-4-ones upon treatment with Bredereck's reagent, but in contrast to canthin-4-ones, these do not undergo ring transformation reactions with guanidine. Only after N-protection (methyl or 2-(trimethylsilyl)ethoxymethyl group), 2-desaza analogues of the alkaloid ...

journal_title：Archiv der Pharmazie

authors： Strödke B,Gehring AP,Bracher F

更新日期：2015-02-01 00:00:00

abstract：:6-Amino-5-imino-pyrazolo[4',3':5,6]pyrano[2,3-d]pyrimidine derivative 4 and pyrazolo-[4',3':5,6]pyrano[2,3-d]pyrimidin-5-ylhydrazine derivative 5 were prepared starting from 6-amino-3-methyl-4-(p-nitrophenyl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile 1. The synthesis and structure characterization of 9,11-dihydr...

journal_title：Archiv der Pharmazie

authors： Shamroukh AH,Zaki ME,Morsy EM,Abdel-Motti FM,Abdel-Megeid FM

更新日期：2007-07-01 00:00:00

abstract：:Synthesis and biological assays of a series of 2-phenylpteridine derivatives are described to compare their affinities to adenosine receptors with those of the corresponding adenines, purposely prepared, and 8-azaadenines previously described. This study demonstrates that the enlargement of the five-membered ring of t...

journal_title：Archiv der Pharmazie

authors： Giorgi I,Biagi G,Livi O,Leonardi M,Scartoni V,Pietra D

更新日期：2007-02-01 00:00:00

abstract：:The photochemical stability of 2, 6, 6-trimethyl-3-carbmethoxy-4-phenyl-5-oxo-1, 4, 5, 6, 7, 8-hexahydroquinoline (HHQ) derivatives with different substituents on the phenyl ring (-Cl, -NO(2), -CF(3), -CH(3), -OCH(3)) has been studied.The process of photodegradation was studied by UV spectrophotometry. The rate of pho...

journal_title：Archiv der Pharmazie

authors： Mielcarek J,Safak C,Simsek R,Matloka A

更新日期：2002-05-01 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：:Antibiotic-resistant bacteria continue to play an important role in human health and disease. Inventive strategies are necessary to develop new therapeutic leads to challenge drug-resistance problems. From this perception, new quinoline hybrids bearing bioactive pharmacophores were synthesized. The newly synthesized c...

journal_title：Archiv der Pharmazie

authors： Rizk OH,Bekhit MG,Hazzaa AAB,El-Khawass EM,Abdelwahab IA

更新日期：2019-10-01 00:00:00

abstract：:With the purpose of expanding the structural variety of chemical compounds available as pharmacological tools for the treatment of Alzheimer's disease, we synthesized and evaluated a novel series of indole-benzoxazinones (Family I) and benzoxazine-arylpiperazine derivatives (Family II) for potential human acetylcholin...

journal_title：Archiv der Pharmazie

authors： Méndez-Rojas C,Quiroz G,Faúndez M,Gallardo-Garrido C,Pessoa-Mahana CD,Chung H,Gallardo-Toledo E,Saitz-Barría C,Araya-Maturana R,Kogan MJ,Zúñiga-López MC,Iturriaga-Vásquez P,Valenzuela-Gutiérrez C,Pessoa-Mahana H

更新日期：2018-05-01 00:00:00

abstract：:Solid-state Nuclear Magnetic Resonance (NMR) provides a general method to study molecular structure and dynamics in a non-crystalline and insoluble environment. We discuss the latest methodological progress to construct 3D molecular structures from solid-state NMR data obtained under magic-angle-spinning conditions. A...

journal_title：Archiv der Pharmazie

authors： Luca S,Heise H,Lange A,Baldus M

更新日期：2005-06-01 00:00:00

abstract：:2- or 6-(1-Hydroxyiminoalkyl)-5,8-dimethoxy-1,4-naphthoquin-one (DMNQ) and 6-(1-propyloxyimino- alkyl)-DMNQ derivatives were synthesized, and their inhibitory effects on DNA topoisomerase-I (TOPO-I) and antiproliferative activities against L1210 cells were examined. In a comparison, it was found that 6-(1-hydroxyimino...

journal_title：Archiv der Pharmazie

authors： Song GY,Kim Y,You YJ,Cho H,Kim SH,Sok DE,Ahn BZ

更新日期：2000-04-01 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 novel series of dithiocarbamic acid 6,11-dioxo-6,11-dihydro-1H-anthra[1,2-d]imidazol-2-yl methyl esters were synthesized and their cytotoxic and apoptotic activities were evaluated on HeLa cells. Some of these compounds showed potent cytotoxic activities and are able to induce the apoptosis mechanism in this cell li...

journal_title：Archiv der Pharmazie

authors： Onder Nİ,İncesu Z,Özkay Y

更新日期：2015-07-01 00:00:00