Abstract:
:Reaction of K2PtCl4 with the substituted 2-aminomethylpyridines 9, 14, and 22 affords the corresponding dichloroplatinum(II) complexes 3-5. Compounds 3 and 22 show remarkable relative binding affinities for the estrogen receptor. Towards the hormone-independent P388-tumor of the CD2F1-mouse the platinum(II) complexes 4 and 5 are weakly active, complex 3 is inactive. Towards the hormone-independent MDA-MB 231-cell line, compounds 3-5, 9, 14, and 22 exhibit no significant antitumor activity. Towards the hormone-dependent MCF-7 cell line, compounds 3-5, 9, 14 show weak antitumor activity, whereas compound 22 exhibits strong inhibition.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Brunner H,Nerl G,von Angerer E,Knebel Nsubject
Has Abstractpub_date
1991-10-01 00:00:00pages
779-84issue
10eissn
0365-6233issn
1521-4184journal_volume
324pub_type
杂志文章abstract::A series of oximes deriving from 5-arylidene-pyrrolidine-2,3,4-triones and pyridine-2,3,4-triones has been prepared. The presence of the tautomeric nitrosoenol was proven in solutions of alpha-ketooxime 7a. The binding affinity of the new oximes toward the N-methyl-D-aspartate (glycine site) receptor has been measured...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/(sici)1521-4184(19999)332:9<309::aid-ardp3
更新日期:1999-09-01 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
pub_type: 杂志文章
doi:10.1002/ardp.200700001
更新日期:2007-05-01 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
pub_type: 杂志文章
doi:10.1002/ardp.201500342
更新日期:2016-03-01 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
pub_type: 杂志文章
doi:10.1002/ardp.200800233
更新日期:2009-07-01 00:00:00
abstract::The synthesis and preliminary assays as hypocholesterolemic agents of five N-diphenylmethylpiperazines are described. The evaluations were carried out in hypercholesterolemic mice and two of these compounds were more effective than bezafibrate in the test employed. The di-p-chlorosubstituted compounds showed higher ac...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.2503240907
更新日期:1991-09-01 00:00:00
abstract::In continuation of our effort aimed towards the development of novel aldose reductase inhibitors, several phenylacetic acids bearing an alkoxy substituent in position 3 or 4, respectively, were prepared and screened. The latter represent formal ring opening products of the cyclohexylmethyloxyphenylacetic acids IIa and...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200600054
更新日期:2006-10-01 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
pub_type: 杂志文章
doi:10.1002/(sici)1521-4184(199802)331:2<59::aid-ardp5
更新日期:1998-02-01 00:00:00
abstract::The plant pentacyclic alkaloid camptothecin and its structural analogs were extensively studied. These compounds are interesting due to the antitumor activity associated with their ability to inhibit topoisomerase I in tumor cells. During the last decades of the 20th century, a large number of the silicon-containing c...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章,评审
doi:10.1002/ardp.201700297
更新日期:2018-01-01 00:00:00
abstract::A series of hydantoin prostaglandin analogues, in which the hexamethylene moiety of the acid side chain was replaced by other spacing groups possessing either ether, sulphide and/or olefin functionality, were prepared and evaluated for platelet aggregation inhibiting activity. The 4-thia analogue 13*) proved to be the...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19933260206
更新日期:1993-02-01 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
pub_type: 杂志文章
doi:10.1002/ardp.201600332
更新日期:2017-02-01 00:00:00
abstract::Rapamycin is an mTOR allosteric inhibitor with multiple functions such as immunosuppressive, anticancer, and lifespan prolonging activities. Its C-43 semi-synthetic derivatives temsirolimus and everolimus have been used as mTOR targeting anticancer drugs in the clinic. Following our previous research on antitumor rapa...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201800123
更新日期:2018-11-01 00:00:00
abstract::Several 2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-benzimidazole-5-carboxamidine analogues were synthesized for their antibacterial and antifungal activities against S. aureus, Methicillin-resistant S. aureus (MRSA), C. albicans, and C. krusei. MIC values of the targeted compounds 43-58 are comparabl...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200500168
更新日期:2006-02-01 00:00:00
abstract::In this study, the synthesis of a new series of 3,6-disubstituted-7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazine 1a-4c compounds derived from 4-amino-3-substituted-1,2,4-triazole-5-thiones 1-4 is described. All of the synthesized compounds were screened for their possible analgesic / anti-inflammatory, antioxidant activit...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200800188
更新日期:2009-05-01 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
pub_type: 杂志文章,评审
doi:10.1002/ardp.201900272
更新日期:2020-01-01 00:00:00
abstract::A series of 5-alkyl-5-phenylbarbituric acid analogues were shown to be potent hypolipidemic agents in rats and mice at 20 mg/kg/day. This dose is lower than that required for hypolipidemic activity for clofibrate and nicotinic acid derivatives in rodents and man. These new derivatives reduced both serum cholesterol an...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19903230905
更新日期:1990-09-01 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
pub_type: 杂志文章
doi:10.1002/ardp.201100005
更新日期:2011-10-01 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
pub_type: 杂志文章
doi:10.1002/ardp.201500063
更新日期:2015-07-01 00:00:00
abstract::A short series of arylhydrazones of 4-[(2-methylimidazo[1,2-a]pyridine-3-yl)azo]benzoic acid hydrazide was synthesized and tested for antimicrobial activity. All of the compounds show antimicrobial activity against Escherichia coli. A few members were also active against Klebsiella pneumoniae, Staphylococcus aureus an...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19903230304
更新日期:1990-03-01 00:00:00
abstract::The 2-(2-Bromophenyl)-acetaldehyde acetals 8 are treated with n-BuLi and the aldehydes 7 and 11 to form the hydroxyacetales 9 and 12, respectively. 9 is cyclized under acidic conditions to the epoxybenzoxocine 2; analogously 12 yields the epoxydibenzoxocine 14. ...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19903231111
更新日期:1990-11-01 00:00:00
abstract::A synthesis of two new active substances, DOMCl (1-(4-chloromethyl-2, 5-dimethoxyphenyl)-2-propanamine; 2) and DOMOM (1-(2, 5-dimethoxy-4-methoxymethylphenyl)-2-propanamine; 3), was developed. Unexpectedly, the Blanc reaction permitted successful synthesis of 2, 5-dimethoxyphenylpropylamine derivatives having a substi...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200390014
更新日期:2003-06-01 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
pub_type: 杂志文章
doi:10.1002/ardp.200300841
更新日期:2004-04-01 00:00:00
abstract::[4-(Adamantane-1-carboxamido)-3-oxo-1-thia-4-azaspiro[4.4]nonan-2-yl]acetic acid (4a) and [4-(adamantane-1-carboxamido)-8-nonsubstituted/substituted-3-oxo-1-thia-4-azas-piro[4.5]decane-2-yl]acetic acid (4b-g) derivatives were synthesized; their structures were verified by elemental analysis, infrared spectroscopy, 1 H...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.202000256
更新日期:2021-01-06 00:00:00
abstract::This review emphasizes the relationship of breast cancer, estrogen receptor and ligands, especially the centrality of the estrogen receptor, which mediates on one hand the hormone-induced gene transcription and on the other hand the anti-estrogen action against breast cancer. The characterization of the estrogen recep...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章,评审
doi:10.1002/ardp.200800174
更新日期:2009-03-01 00:00:00
abstract::Several derivatives of 1H-benzimidazole-2-carboxylic acid (BICA, 2a) were tested in vitro in comparison to 1H-indole-2-carboxylic acid (ICA, 1e) for their ability to displace [3H]glycine from rat hippocampal membranes. Compound 2a was 8 times more potent than 1e (Ki 5.3 microM, as compared to 42 microM). However, intr...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19963290303
更新日期:1996-03-01 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
pub_type: 杂志文章,评审
doi:10.1002/ardp.200400991
更新日期:2005-06-01 00:00:00
abstract::Alzheimer's disease (AD) is a neurodegenerative disorder characterized by dementia, memory impairment, cognitive dysfunction, and speech impairment. The utility of cholinergic replacement by acetylcholinesterase (AChE) inhibitors in AD treatment has been well documented so far. Recently, studies have also evidenced th...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.202000282
更新日期:2020-11-06 00:00:00
abstract::Copper and zinc have been found to contribute to the burden of amyloid-β (Aβ) aggregations in neurodegenerative Alzheimer's disease (AD). Dysregulation of these metals leads to the generation of reactive oxygen species (ROS) and eventually results in oxidative damage and accumulation of the Aβ peptide, which are the k...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.201500453
更新日期:2016-05-01 00:00:00
abstract::A series of new benzofuran/oxadiazole hybrids (8a-n) was synthesized from 2H-chromene-3-carbonitriles (3a-c) through the multistep synthetic methodology, and these hybrids are known to exhibit anticancer activities. All the compounds were evaluated for their in vitro cytotoxicity against the HCT116 and MIA PaCa2 cell ...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.202000006
更新日期:2020-06-01 00:00:00
abstract::The effect of triterpenes and flavonoids on the activity of several hyaluronic acid-splitting enzymes was investigated. Studies showed that the inhibitory effect of the triterpenes glycyrrhizin and glycyrrhetinic acid is dependent on the source of hyaluronate lyase. Hyaluronate lyase from Streptococcus agalactiae (Hya...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.200500216
更新日期:2006-06-01 00:00:00
abstract::The biotransformation of the positively inotropically active compound N-methyl-N-(2-hydroxy-3-phenoxy-propyl)-11-(2-aminoethyl)-6,11- dihydrodibenz[b,e]-oxepine, neutral fumarate, (Doxaminol, racemic mixture of diastereomeres) in dogs is examined. The metabolits M1-M7 were isolated and their chemical structures identi...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19903230503
更新日期:1990-05-01 00:00:00