摘要:

Abstracto‐Aminophenyl‐substituierte Ketoxime und Amidoxime3reagieren mit Aldehyden und Ketonen zu cyclischen Amidin‐ bzw. Chinazolin‐N‐oxiden5, mit Diethylcarbonat ergibt Anthranilsäureamidoxim (3c) das Oxadiazolon12. Dieses erfährt bei der Thermolyse eine Ringtransformation zu dem Aminoindazol14, mit Ketonen erfolgt der Ringschluß zu den anellierten Chinazolinderivaten22. Zur Erklärung des Reaktionsverlaufs werden semiempirische Molekülorbitalverfahren und die Störungstheor

ISSN:0365-6233    

DOI:10.1002/ardp.19953280502

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractA new class of heteroaromatic analogs of lignans, called heterolignanolides, have been tested against several tumor cell lines. These compounds carry diverse heterocyclic rings, instead of the trimethoxyphenyl ring found in the natural lignans yatein and podorhizol. They have moderate antineoplastic activity (P‐388, A‐549, HT‐29) compared with that of yatein. None of the tested compounds has discernible antiviral (HSV‐1, VSV) or enzyme inhibitor (ADA, DHFR, GST) a

ISSN:0365-6233    

DOI:10.1002/ardp.19953280503

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractThe Pt(II) complexes of 1,3‐diphenylpropane‐1,3‐diamines (part IV2)) were tested for DNA interaction (UV‐difference spectroscopy, Tables 1 and 2), for affinity to the estrogen receptor (calf uterus cytosol; scarcely any affinity), and for cytostatic activity at estrogen independent MDA‐MB 231 cells (Tables 3 and 4) and estrogen dependent MCF‐7 cells (Tables 5 and 6). The data are compared with those reported for the analogous 1,2‐diphenylethane‐1,2‐diamine‐Pt(II) complexes: most probably, the cytostatic activity is not mediated by th

ISSN:0365-6233    

DOI:10.1002/ardp.19953280504

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractSome new oximinoalkanoic (n = 2,3,4) esters and acids derived from methoxyphenylthienyl ketones have been synthesized and evaluatedin vitrofor their inhibitory effects on arachidonic acid‐induced human platelet aggregation. Of the eighteen oximinoethers tested the most active derivatives, which were four times more active as aspirin, belonged to theparamethoxy series with Z configuration and n = 2 or

ISSN:0365-6233    

DOI:10.1002/ardp.19953280505

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractA series of 22 benzimidazoles, having several substituents on the azole and benzene nuclei, were prepared and evaluatedin vitrofor antimicrobial activity. At first 2‐chloro or 2‐chloromethyl‐5(6)‐substituted‐1H‐benzimidazoles were synthesized, which were then substituted at C‐2 with several piperazine or piperidine derivatives. The antibacterial activity of these compounds againstStaphylococcus aureus, Bacillus subtilis, Escherichia coli, andPseudomonas aeruginosa, and the antifungal activity againstCandida albicans, Candida stellatoidea, Candida parapsilosis, andCandida pseudotropicaliswere determined as the MIC values. Since compound12exhibits good activity, in order to clarify the effect of substituents at C‐1 on the activity, benzimidazole derivatives having ethyl, allyl, benzyl, andp‐fluorobenzyl substituents at C‐1 were prepared, and slightly increase

ISSN:0365-6233    

DOI:10.1002/ardp.19953280506

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractCyclische Salze des Dithiokohlensäure‐diester‐imidium Typs (3, 5) wurden mit NH2‐Nucleophilen zu den cyclischen Isothioharnstoffen6–8umgesetzt. Einige dieser Verbindungen konnten zu cyclischen Isothioharnstoff‐S,S‐dioxiden (9, 10) oxi

ISSN:0365-6233    

DOI:10.1002/ardp.19953280507

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractThe regioselective synthesis of isomeric 5(3)‐aminomethyl‐3(5)‐phenyl isoxazoles using different methods is described. Spectroscopic data, especially mass spectrometric fragmentation, were used to identify and characterize the regioisomers. The muscarinic activity of these isoxazoles was assayed on isolated guinea‐pig ileum and atria as well as on isolated rabbit vas d

ISSN:0365-6233    

DOI:10.1002/ardp.19953280508

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractIn search of structure‐activity relationships among histamine H3‐receptor antagonists the imidazole ring of known H3‐receptor antagonists was replaced by different heteroaromatic ring systems. Thus, azines and diazines with ether (6–13) and carbamate (15–24) moieties as functional groups were synthesized. The obtained compounds did not show significant H3‐receptor antagonist activityin vitro(rat brain cortex) orin vivo(mice brain). The new compounds were also screened for H1‐receptor antagonist activity on the isolated guinea‐pig ileum and for H2‐receptor antagonist activity on the isolated spontaneously beating guinea‐pig right atrium. The substances showed only weak antagonistic activity at both histamine

ISSN:0365-6233    

DOI:10.1002/ardp.19953280509

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractDer 5‐Lipoxygenase‐Inhibitor 2‐(3,5‐Di‐tert‐butyl‐4‐hydroxyphenyl)‐3‐hydroxy‐1,4‐naphthochinon (2), sein Deoxygenierungsprodukt1sowie die oxygenierte Spezies3sind O2•−‐ Quencher unterschiedlicher Potenz in wäßriger Lösung. In alkoholischer Lösung ändert sich die antioxidative Aktivität von1nicht,2allerdings ist nur noch ein schwacher O2•−‐ Quencher und3zeigt prooxidative Eigenschaften. Dieses Phänomen wurde in dem O2•−‐generierenden Oxygenierungssystem (OS)DMSO‐CO32‐O2mit präparativer Technik untersucht. Dabei konnte folgende Reaktionssequenz bewiesen werden:3⇒2⇒4(2,6‐Di‐tert‐butyl‐1,4‐benzochinon). Während der Schritt3⇒2|O2•−abhängig sein sollte, erfolgt der Übergang2⇒4in zwei Stufen. Die 1. Stufe ist eine Retro‐Michaelreaktion unter Freisetzung von 2,6‐Di‐tert‐butylphenol (5), die 2. Stufe (5⇒4) beinhaltet die basenkatalysierte Oxygenierung mit3O2. Das als Nebenprodukt anfallende Diphenochinon6kann – i

ISSN:0365-6233    

DOI:10.1002/ardp.19953280510

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

Abstract[1,2‐Bis(4‐methoxy/4‐hydroxyphenyl)ethylenediamine]dichloroplatinum‐(II) complexes with Cl‐, CH3‐, or OCH3‐substituents in theortho‐positions of the aromatic rings (meso‐1‐PtCl2,D,L‐1‐PtCl2,meso‐2‐PtCl2,D,L‐2‐PtCl2,meso‐3‐PtCl2,meso‐4‐PtCl2,meso‐5‐PtCl2) were tested on the MDA‐MB 231 breast cancer cell line, the lymphocytic leukemia P388, and the estrogen receptor‐positive and ‐negative MXT mammary carcinoma of the mouse (MXT,ER(+)‐MC, MXT,ER(−)‐MC). The comparison of the effects of methoxy‐substituted complexes (meso‐1‐PtCl2,D,L‐1‐PtCl2,meso‐3‐PtCl2) with those of the respective hydroxy‐substituted ones (meso‐2‐PtCl2,D,L‐2‐PtCl2,meso‐4‐PtCl2) shows that a reduction of estrogenic effects as well as a total loss of the mammary tumor‐inhibiting activity takes place on methylation of the 4‐OH group. The exchange of the 2,6‐standing chlorine atoms by methyl groups inmeso‐2‐PtCl2led to the non‐estrogenic, but on the MXT,ER(+)‐MC highly effective derivativemeso‐4

ISSN:0365-6233    

DOI:10.1002/ardp.19953280511

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY