Breast cancer, estrogen receptor and ligands.

abstract：:Novel 6,11-dioxo-6,11-dihydro-benzo[f]pyrido[1,2-a]indole-12-carboxamide derivatives and the corresponding 7,10-dihydroxy analogues were designed in accordance with Moore's and Pindur's theory and synthesized based on the structural similarity with known antitumour agents such as ellipticine, daunorubicin, mitoxantron...

journal_title：Archiv der Pharmazie

authors： Defant A,Guella G,Mancini I

更新日期：2007-03-01 00:00:00

abstract：:Structural feature analysis of chlorogenic acid derivatives made up of varying lengths of alkyl groups as α-glucosidases inhibitors were performed by QSAR techniques. The statistically significant models derived from the study were validated by leave one out, Y-randomization and test set methods. The predictive capaci...

journal_title：Archiv der Pharmazie

authors： Narayana Moorthy NS,Ramos MJ,Fernandes PA

更新日期：2012-04-01 00:00:00

abstract：:Isatin and azole moieties, which have the ability to form various noncovalent interactions with different therapeutic targets, are common pharmacophores in drug development. Isatin and azole derivatives possess promising in vitro and in vivo anticancer activity, and many of them, such as semaxanib, sunitinib, and carb...

journal_title：Archiv der Pharmazie

authors： Hou Y,Shang C,Wang H,Yun J

更新日期：2020-01-01 00:00:00

abstract：:A novel series of N-(2-(piperazin-1-yl)phenyl)aryl carboxamide derivatives were simply synthesized by Ugi-multicomponent reaction as β-secretase (BACE1) inhibitors. The BACE1 inhibitory activity of the synthesized compounds was examined using a Forester resonance energy transfer (FRET)-based assay. Among the tested co...

journal_title：Archiv der Pharmazie

authors： Edraki N,Firuzi O,Fatahi Y,Mahdavi M,Asadi M,Emami S,Divsalar K,Miri R,Iraji A,Khoshneviszadeh M,Firoozpour L,Shafiee A,Foroumadi A

更新日期：2015-05-01 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：: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：: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：: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：:Pyrrolo[3,4-c]-beta-carbolinedione dimers 5-14 were synthesized from furo[3,4-c]-beta-carbolinediones and diamines by solvent-free TaCl5/silica catalyzed reaction under microwave irradiation. The inhibitory property of these target compounds, the starting materials 2, 31, 32, and the N-alkylated pyrrolo[3,4-c]-beta-ca...

journal_title：Archiv der Pharmazie

authors： Mahboobi S,Eluwa S,Kumar S,Koller M,Störl K

更新日期：1999-07-01 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：: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：:Cancer can invade or spread to almost all parts of the body. The increasing morbidity and high mortality of cancer create a great demand for the development of novel anticancer drugs. Coumarin derivatives are ubiquitous in nature and can readily interact with diverse enzymes and receptors in cancer cells via weak bond...

journal_title：Archiv der Pharmazie

authors： Song XF,Fan J,Liu L,Liu XF,Gao F

更新日期：2020-08-01 00:00:00

abstract：:A new series of 4-hydroxycoumarin derivatives 3a-d was synthesized by the reaction of 3-bromo-4-hydroxy coumarin 1 with various heteroaldehydes 2a-d in good yields. The synthesized compounds were characterized on the basis of their elemental and spectral (IR, (1)H-NMR and mass spectrometry) analysis. All target compou...

journal_title：Archiv der Pharmazie

authors： Siddiqui ZN,N MM,Ahmad A,Khan AU

更新日期：2011-06-01 00:00:00

abstract：:Cathepsin B and plasmin are intra- or extracellular proteases that are overexpressed by several solid tumors. In order to exploit both proteases as molecular targets for tumor-specific cleavage of prodrugs, an albumin-binding formulation of methotrexate was developed that incorporated the peptide sequence D-Ala-Phe-Ly...

journal_title：Archiv der Pharmazie

authors： Warnecke A,Fichtner I,Sass G,Kratz F

更新日期：2007-08-01 00:00:00

abstract：:A series of 1-¿omega-(4-aryl-1-piperazinyl)alkyl]indolin-2(1H)-one derivatives 2-14 was synthesized in order to obtain ligands with a dual 5-HT1A/5-HT2A activity. The majority of those compounds (2-5, 7, 10-13) exhibited a high 5-HT1A (Ki = 2-44 nM) and/or 5-HT2A affinity (Ki = 51 and 39 for 5 and 7, respectively). In...

journal_title：Archiv der Pharmazie

authors： Mokrosz MJ,Duszyńska B,Misztal S,Kłodzińska A,Tatarczyńska E,Chojnacka-Wójcik E,Dziedzicka-Wasylewska M

更新日期：1998-10-01 00:00:00

abstract：:A novel dimer of 2-(4-pyridylmethyl)-1-indanone (2) was obtained while carrying out aldol condensation of 1-indanone with pyridine-4-carboxaldehyde in potassium hydroxide. The structure of dimer 3 has been established using various spectral techniques and was screened for its ability to inhibit the cytochrome P(450) e...

journal_title：Archiv der Pharmazie

authors： Gupta R,Jindal DP,Jit B,Narang G,Palusczak A,Hartmann RW

更新日期：2004-07-01 00:00:00

abstract：:A general procedure for the preparation of 1,2,3-triazole analogs of nucleosides from diethyl 2-azidoethoxymethyl- and 2-azidoethoxyethylphosphonates was elaborated. The application of microwave irradiation shortened the reaction time to 10 min in comparison to ca. 48 h when 1,3-dipolar cycloadditions were performed u...

journal_title：Archiv der Pharmazie

authors： Głowacka IE,Balzarini J,Wróblewski AE

更新日期：2013-04-01 00:00:00

abstract：:Marine organisms play an important role in natural product-based drug research due to accumulation of structurally unique and bioactive metabolites. The exploration of marine-derived compounds may significantly extend the scientific knowledge of potential scaffolds for antibiotic drug discovery. Development of novel a...

journal_title：Archiv der Pharmazie

authors： Daletos G,Ancheeva E,Chaidir C,Kalscheuer R,Proksch P

更新日期：2016-10-01 00:00:00

abstract：:In this study, a number of 2,5-disubstituted 1,3,4-thiadiazoles were synthesized using an appropriate synthetic route, and their anticonvulsant activity was determined by the maximal electroshock seizure (MES) test and their neurotoxicity was evaluated by the rotarod test. Additionally, their hypnotic activity was tes...

journal_title：Archiv der Pharmazie

authors： Toolabi M,Khoramjouy M,Aghcheli A,Ayati A,Moghimi S,Firoozpour L,Shahhosseini S,Shojaei R,Asadipour A,Divsalar K,Faizi M,Foroumadi A

更新日期：2020-12-01 00:00:00

abstract：:A series of hydroxy-substituted chalcone oxime derivatives were synthesized. These compounds were then evaluated for their inhibitory activities on tyrosinase and melanogenesis in murine B16F10 melanoma cells. The structures of the synthesized compounds were confirmed by (1) H NMR, (13) C NMR, FTIR, and HRMS. Two of t...

journal_title：Archiv der Pharmazie

authors： Radhakrishnan SK,Shimmon RG,Conn C,Baker AT

更新日期：2016-01-01 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

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：:Schiff base transition metal complexes are an important class of compounds with great potential for therapeutic interventions. However, data on antileukemic and antilymphoma effects of these complexes are limited. The activity of N,N'-bis(salicylidene)-1,2-phenylenediamine (salophene, 1), its iron(II/III) and manganes...

journal_title：Archiv der Pharmazie

authors： Hille A,Wolf T,Schumacher P,Ott I,Gust R,Kircher B

更新日期：2011-04-01 00:00:00

abstract：:A rapid and efficient one-pot condensation reaction of long-chain alkyl and alkenyl acid hydrazides and nitriles was carried out to afford 3,5-disubstituted-1H-1,2,4-triazoles. The compounds 5a-o were screened for in-vitro antibacterial activity against the representative panel of two Gram-positive and two Gram-negati...

journal_title：Archiv der Pharmazie

authors： Sharma S,Gangal S,Rauf A,Zahin M

更新日期：2008-11-01 00:00:00

abstract：:Alzheimer's disease (AD) is the most common type of dementia and related to the degeneration of hippocampal cholinergic neurons, which dramatically affects cognitive ability. Acetylcholinesterase (AChE) inhibitors are employed as drugs for AD therapy. Three series of sulfonylhydrazone compounds were designed, and thei...

journal_title：Archiv der Pharmazie

authors： Fernandes TB,Cunha MR,Sakata RP,Candido TM,Baby AR,Tavares MT,Barbosa EG,Almeida WP,Parise-Filho R

更新日期：2017-11-01 00:00:00

abstract：:The oncoprotein cytotoxic associated gene A (CagA) of Helicobacter pylori plays a pivotal role in the development of gastric cancer, so it has been an important target for anti-H. pylori drugs. Conventional drugs are currently being implemented against H. pylori. The inhibitory role of plant metabolites like curcumin ...

journal_title：Archiv der Pharmazie

authors： Srivastava AK,Tewari M,Shukla HS,Roy BK

更新日期：2015-08-01 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：: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：: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：:CXC chemokine receptor-3 (CXCR3) is a G-protein coupled receptor (GPCR) predominantly expressed on activated T lymphocytes that promote Th1 responses. Previously, we described the 3H-quinazolin-4-one containing VUF 5834 (decanoic acid {1-[3-(4-cyano-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-yl]-ethyl}-(2-dimethylamino-et...

journal_title：Archiv der Pharmazie

authors： Storelli S,Verzijl D,Al-Badie J,Elders N,Bosch L,Timmerman H,Smit MJ,De Esch IJ,Leurs R

更新日期：2007-06-01 00:00:00