abstract：:A series of 1,8-diazaanthraquinone derivatives carrying a 3-dialkylaminomethyl or a 3-(N-alkyl or aryl)carbamoyloxymethyl substituent was synthesised and their in vitro cytotoxic activities were evaluated against eight human cancer cell lines (HOP62, SK-OV-3, HCT-15, SF295, MCF7, SNU-354, KB-3-1 and KB-V-1). A number ...

journal_title：European journal of medicinal chemistry

authors： Lee H,Lee SI,Cho J,Choi SU,Yang SI

更新日期：2003-07-01 00:00:00

abstract：:In this study, some novel 2,6-dimethyl-N'-substituted phenylmethylene-imidazo[2,1-b][1,3,4]thiadiazole-5-carbohydrazides (3a-3h) were synthesized from 2,6-dimethylimidazo-[2,1-b][1,3,4]thiadiazole-5-carbohydrazide (2). The newly synthesized compounds (3a-3h) were evaluated in the National Cancer Institute's 3-cell lin...

journal_title：European journal of medicinal chemistry

authors： Terzioglu N,Gürsoy A

更新日期：2003-07-01 00:00:00

abstract：:Boron neutron capture therapy (BNCT) is an experimental treatment modality which depends on a sufficient cellular uptake of Boron ((10)B) followed by an exposure to a thermal neutron beam from a nuclear reactor. High energetic particles (4He and 7Li) are created during the neutron capture reaction and produce DNA dama...

journal_title：European journal of medicinal chemistry

authors： Braun K,Wolber G,Waldeck W,Pipkorn R,Jenne J,Rastert R,Ehemann V,Eisenmenger A,Corban-Wilhelm H,Braun I,Heckl S,Debus J

更新日期：2003-06-01 00:00:00

abstract：:We have synthetised a series of oxidised apomorphine derivatives (orto and para quinones 2-5), in order to analyse their vascular activity. We have performed radioligand binding assays on rat cortical membranes and functional studies on rat aortic rings. Instead the relaxant activity exhibited by (R)-apomorphine, o-qu...

journal_title：European journal of medicinal chemistry

authors： Abarca B,Ballesteros R,Bielsa P,Moragues J,D'Ocon P,García-Zaragozá E,Noguera MA

更新日期：2003-05-01 00:00:00

abstract：:Phosphopantetheine adenylyltransferase (PPAT) is an essential enzyme in Coenzyme A biosynthesis. Because bacterial PPAT and mammalian PPAT are dissimilar, this enzyme is an attractive antibacterial target. Based on the structure of the substrate, 4-phosphopantetheine, a dipeptide library was designed, synthesised and ...

journal_title：European journal of medicinal chemistry

authors： Zhao L,Allanson NM,Thomson SP,Maclean JK,Barker JJ,Primrose WU,Tyler PD,Lewendon A

更新日期：2003-04-01 00:00:00

abstract：:Human leukocyte elastase (HLE) is a serine proteinase, capable of degrading a variety of structural matrix proteins. SSR69071 2-[(4-isopropyl-6-methoxy-1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methoxy]-9-(2-piperidin-1-ylethoxy)-4H-pyrido[1,2-a]pyrimidin-4-one was selected as a novel orally active HLE inhibitor f...

journal_title：European journal of medicinal chemistry

authors： Varga M,Kapui Z,Bátori S,Nagy LT,Vasvári-Debreczy L,Mikus E,Urbán-Szabó K,Arányi P

更新日期：2003-04-01 00:00:00

abstract：:The absorption of 111 drug and drug-like compounds was evaluated from 111 references based on the ratio of urinary excretion of drugs following oral and intravenous administration to intact rats and biliary excretion of bile duct-cannulated rats. Ninety-eight drug compounds for which both human and rat absorption data...

journal_title：European journal of medicinal chemistry

authors： Zhao YH,Abraham MH,Le J,Hersey A,Luscombe CN,Beck G,Sherborne B,Cooper I

更新日期：2003-03-01 00:00:00

abstract：:Several heteroaromatic analogues of (2-aryl-1-cyclopentenyl-1-alkylidene)-(arylmethyloxy)amine COX-2 inhibitors, in which the cyclopentene moiety was replaced by pyrazole, thiophene or isoxazole ring, were synthesized, in order to verify the influence of the different nature of the central core on the COX inhibitory p...

journal_title：European journal of medicinal chemistry

authors： Balsamo A,Coletta I,Guglielmotti A,Landolfi C,Mancini F,Martinelli A,Milanese C,Minutolo F,Nencetti S,Orlandini E,Pinza M,Rapposelli S,Rossello A

更新日期：2003-02-01 00:00:00

abstract：:Designed as a new group of planar molecule containing the proposed 2-phenylnaphthalene-type structure, a number of 11H-indolo[3.2-c]quinoline derivatives were synthesized and evaluated biologically. Several compounds were found to possess cytotoxic activity against the growth of human promyelocytic leukemia cells (HL-...

journal_title：European journal of medicinal chemistry

authors： He L,Chang HX,Chou TC,Savaraj N,Cheng CC

更新日期：2003-01-01 00:00:00

abstract：:A series of 6,7-diaryl-2,3-1H-dihydropyrrolizines was prepared as COX-1/COX-2 and 5-LOX inhibitors. The inhibition of COX-1 was evaluated using intact bovine platelets as the enzyme source, whereas LPS-stimulated human monocytes served as the enzyme source for inducible COX-2. The determination of arachidonic metaboli...

journal_title：European journal of medicinal chemistry

authors： Ulbrich H,Fiebich B,Dannhardt G

更新日期：2002-12-01 00:00:00

abstract：:A new series of 5-nitro-1H-indole-2,3-dione-3-thiosemicarbazones (3a-k) obtained by condensation of 5-nitro-1H-indole-2,3-dione (1) with N-substituted-thiosemicarbazides (2a-k) were treated with morpholine or piperidine and formaldehyde to yield 1-morpholino/piperidinomethyl-5-nitroindole-2,3-dione-3-thiosemicarbazone...

journal_title：European journal of medicinal chemistry

authors： Karali N

更新日期：2002-11-01 00:00:00

abstract：:5,6-Dimethylxanthenone-4-acetic acid (DMXAA) is a novel anticancer agent with a number of unique activities, and is in clinical trial. The current synthesis of DMXAA involves six steps, beginning with a heterogeneous reaction to form an isonitrosoacetanilide, and gives an overall yield of 11% from 2,3-dimethylaniline....

journal_title：European journal of medicinal chemistry

authors： Atwell GJ,Yang S,Denny WA

更新日期：2002-10-01 00:00:00

abstract：:The synthesis of S-(-)-1-(4-(2-ethoxyethoxy)phenoxy)-2-hydroxy-3-(2-(3,4-dimethoxyphenyl)ethylamino)propane hydrochloride (D140S.HCl 6), a novel short acting beta(1)-specific adrenoceptor antagonist, has been described. The antagonist potency for D140S.HCl 6 has been compared with esmolol, another short acting agent, ...

journal_title：European journal of medicinal chemistry

authors： Jackman GP,Iakovidis D,Nero TL,Anavekar NS,Rezmann-Vitti LA,Louis SN,Mori M,Drummer OH,Louis WJ

更新日期：2002-09-01 00:00:00

abstract：:While nonsteroidal androgen receptor (AR) antagonists have been known for many years, and used in the clinic for the treatment of hormone dependent prostate cancer, very little is known about nonsteroidal AR agonists. We designed and synthesized a series of chiral bicalutamide analogs, which bear electron-withdrawing ...

journal_title：European journal of medicinal chemistry

authors： He Y,Yin D,Perera M,Kirkovsky L,Stourman N,Li W,Dalton JT,Miller DD

更新日期：2002-08-01 00:00:00

abstract：:Thirty-six 6(7)-substituted-3-methyl- or 3-halogenomethyl-2-phenylthio-phenylsulphonyl-chloro-quinoxaline 1,4-dioxides belonging to series 3-6 were synthesised and submitted to a preliminary in vitro evaluation for antimycobacterial, anticandida and antibacterial activities. Antitubercular screening showed a generally...

journal_title：European journal of medicinal chemistry

authors： Carta A,Paglietti G,Rahbar Nikookar ME,Sanna P,Sechi L,Zanetti S

更新日期：2002-05-01 00:00:00

abstract：:7-(5'-Biotinylamidopropanoyl)paclitaxel was synthesised by chemical methods; its immunofluorescence assay and the cell uptake experiments were performed by use of human leukemia U937 cells. The results indicate that paclitaxel is arresting cell cycle at the G(2)M phase only. ...

journal_title：European journal of medicinal chemistry

authors： Sambaiah T,King KY,Tsay SC,Mei NW,Hakimclahi S,Lai YK,Lieu CH,Hwu JR

更新日期：2002-04-01 00:00:00

abstract：:The synthesis of pyrrolo[2,3-e]indole derivatives with the structural characteristics of DNA bis- and mono-intercalators are described. A dihydro benzoindol analogue was also synthesised to elucidate the major structural requirements for cytotoxic activity. A biological evaluation of the test compounds was carried out...

journal_title：European journal of medicinal chemistry

authors： Chacón-García L,Martínez R

更新日期：2002-03-01 00:00:00

abstract：:Several myrcenylhydroquinone derivatives have been evaluated for their cytotoxic activity against three neoplastic cell line cultures and compared with the activity previously observed on other neoplastic systems. Also a new series of this type of compounds has been prepared and the compounds synthesised have been eva...

journal_title：European journal of medicinal chemistry

authors： Molinari A,Oliva A,Reinoso P,del Corral JM,Castro MA,Gordaliza M,Gupta MP,Solís P,San Feliciano A

更新日期：2002-02-01 00:00:00

abstract：:The pyrrolo[1,2-f]phenanthridines 8-22 and the corresponding non-rigid analogues 23-41 were synthesised and their ability to inhibit the replication of HIV-1 was tested. Only the polycyclic derivatives 10, 11, and 13 showed a weak anti-HIV activity, whereas several pyrrolo-phenanthridines (8, 10, 16-18) were found to ...

journal_title：European journal of medicinal chemistry

authors： Almerico AM,Mingoia F,Diana P,Barraja P,Montalbano A,Lauria A,Loddo R,Sanna L,Delpiano D,Setzu MG,Musiu C

更新日期：2002-01-01 00:00:00

abstract：:This work reports the synthesis by microwave irradiation and the binding tests on the 5-HT(1A), 5-HT(2A) and 5-HT(2C) receptors of new substituted piperazines in order to identify selective ligands for 5-HT(1A) subtype receptor. Conventional heating and microwave irradiation of the reactions was compared. Synthesis by...

journal_title：European journal of medicinal chemistry

authors： Caliendo G,Fiorino F,Perissutti E,Severino B,Gessi S,Cattabriga E,Borea PA,Santagada V

更新日期：2001-11-01 00:00:00

abstract：:Two series of three trioxanes and 18 disubstituted peroxides were synthesised and evaluated for their in vitro trichomonacidal activity against Trichomonas vaginalis. The most active compound, 2-methylprop-2-yl 2-methoxyeth-1-yl peroxide exhibited an IC(50) value of 1.0+/-0.2 microM whereas other dialkyl peroxides had...

journal_title：European journal of medicinal chemistry

authors： Camuzat-Dedenis B,Provot O,Cointeaux L,Peyrou V,Berrien JF,Bories C,Loiseau PM,Mayrargue J

更新日期：2001-10-01 00:00:00

abstract：:Several Mannich ketones of 2-arylmethylenecycloalkanones were synthesised using the classical acid-catalysed Mannich reaction. Antibacterial activity of these new water-soluble compounds was reported against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Staphylococcus saprophyticus, Micrococcus lute...

journal_title：European journal of medicinal chemistry

authors： Lóránd T,Kocsis B,Sohár P,Nagy G,Kispál G,Krane HG,Schmitt H,Weckert E

更新日期：2001-09-01 00:00:00

abstract：:A series of N-guanidino substituted 2,4-diamino-5-carbonylguanidine molecules related to amiloride were synthesised and evaluated for their ability to inhibit the sodium-calcium exchanger in rat insulinoma cells (RINm5F) and human platelets. Specific chemical pathways were used to prepare the benzene derivatives desig...

journal_title：European journal of medicinal chemistry

authors： Rogister F,Laeckmann D,Plasman P,Van Eylen F,Ghyoot M,Maggetto C,Liégeois J,Géczy J,Herchuelz A,Delarge J,Masereel B

更新日期：2001-07-01 00:00:00

abstract：:Ambasilide, a representative of Class III antiarrhythmics, was reported to prolong the cardiac action potential duration in the dog, with little or no effect on Ca and Na currents. We synthesised a series of ambasilide analogues, having the 3,8-diazabicyclo-[3.2.1]-octane moiety instead of the 3,7-diazabicyclo-[3.3.1]...

journal_title：European journal of medicinal chemistry

authors： Villa S,Barlocco D,Cignarella G,Papp GJ,Baláti B,Takács J,Varró A,Borosy A,Keserû K,Mátyus P

更新日期：2001-06-01 00:00:00

abstract：:In our search for new compounds acting on benzodiazepine receptors among the fused 2-thiohydantoin derivatives, a series of arylidene imidazo[2,1-b]thiazines was synthesized. The 1,2- and 2,3- cyclized derivatives of mono- and di-substituted Z-5-arylidene-2-thiohydantoins were examined (the X-ray crystal structure of ...

journal_title：European journal of medicinal chemistry

authors： Kieć-Kononowicz K,Karolak-Wojciechowska J,Müller CE,Schumacher B,Pekala E,Szymańska E

更新日期：2001-05-01 00:00:00

abstract：:A data set of 389 compounds, active in the central nervous system (CNS) and divided into eight classes according to the receptor type, was extracted from the RBI database and analyzed by Self-Organizing Maps (SOM), also known as Kohonen Artificial Neural Networks. This method gives a 2D representation of the distribut...

journal_title：European journal of medicinal chemistry

authors： Pintore M,Taboureau O,Ros F,Chrétien JR

更新日期：2001-04-01 00:00:00

abstract：:Eleven derivatives of 1,1'-[1,2-ethylenebis(benzene-1,4-diylmethylene)]bis(4-pyridinium) dibromides bearing various groups at C-4 of the pyridinium moiety were synthesized and examined for their inhibition of choline kinase (ChoK) and antiproliferative activities. The C-4 substituents include electron-releasing, neutr...

journal_title：European journal of medicinal chemistry

authors： Campos J,del Carmen Núñez M,Rodríguez V,Entrena A,Hernández-Alcoceba R,Fernández F,Lacal JC,Gallo MA,Espinosa A

更新日期：2001-03-01 00:00:00

abstract：:The synthesis and pharmacological profiles of some new steroidal mono- and bisquaternary ammonium derivatives have been described. The compounds featured have been conceptually derived structurally from two lead structures: pancuronium bromide 1 and chandonium iodide 2. In vitro and in vivo neuromuscular blocking stud...

journal_title：European journal of medicinal chemistry

authors： Jindal DP,Piplani P,Fajrak H,Prior C,Marshall IG

更新日期：2001-02-01 00:00:00

abstract：:The synthesis and biological activities of acidic, basic and neutral types of butyric acid (BA) prodrugs possessing increased aqueous solubility are described. The compounds are butyroyloxyalkyl derivatives of carboxylic acids, which possess functionalities suitable for aqueous solubilization. The anticancer activity ...

journal_title：European journal of medicinal chemistry

authors： Nudelman A,Gnizi E,Katz Y,Azulai R,Cohen-Ohana M,Zhuk R,Sampson SR,Langzam L,Fibach E,Prus E,Pugach V,Rephaeli A

更新日期：2001-01-01 00:00:00

abstract：:A series of 1H,3H-thiazolo[4,3-b]quinazolines (2a-i) were synthesized and evaluated for their in vitro antitumour activity against ca. 60 human tumour cell lines. They exhibited moderate (2c, 2d, 2f and 2g) to strong (2a, 2b, 2e, 2h and 2i) cell-growth inhibition at a concentration of 10(-4) M, but weak activity at lo...

journal_title：European journal of medicinal chemistry

authors： Grasso S,Micale N,Monforte AM,Monforte P,Polimeni S,Zappalà M

更新日期：2000-12-01 00:00:00

abstract：:The title compounds (8) were synthesized through the cyclocondensation of the corresponding N-substituted 4-amino-2-chloro-1,8-naphthyridine-3-carboxamides (4) with the proper hydrazides, in order to evaluate their anti-inflammatory and anti-aggressive properties. Several compounds 8 exhibited high anti-inflammatory a...

journal_title：European journal of medicinal chemistry

authors： Roma G,Di Braccio M,Grossi G,Mattioli F,Ghia M

更新日期：2000-11-01 00:00:00

abstract：:Five newly synthesised original compounds were investigated for acute toxicity, influence on hexobarbital sleeping time, effect on the locomotor activity, and brain antihypoxic activity. Two of the compounds were tested in a model of glutamate induced neurotoxicity in the brain cell culture using a cell viability test...

journal_title：European journal of medicinal chemistry

authors： Zlatkov A,Peikov P,Rodriguez-Alvarez J,Danchev N,Nikolova I,Mitkov J

更新日期：2000-10-01 00:00:00

abstract：:Progestagens are drugs, which are widely used in hormonal contraception and in hormone-replacement therapy. Since the natural hormone, progesterone, lacks oral activity, much effort has been devoted to finding analogues with improved oral activity and, preferably, higher potency and selectivity. A crystal structure of...

journal_title：European journal of medicinal chemistry

authors： Bursi R,Groen MB

更新日期：2000-09-01 00:00:00

abstract：:A series of 6-chloro-3-phenyl-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones 3 and a series of 6-chloro-3-phenyl-2H-1,3-benzoxazine-2, 4(3H)-dithiones 4 were synthesized by melting 6-chloro-3-phenyl-2H-1, 3-benzoxazine-2,4(3H)-dione and its derivatives substituted on the phenyl ring 2 with tetraphosphorus decasulfide. Compoun...

journal_title：European journal of medicinal chemistry

authors： Waisser K,Gregor J,Kubicová L,Klimesová V,Kunes J,Machácek M,Kaustová J

更新日期：2000-07-01 00:00:00

abstract：:A naphthalene compound was chosen as lead compound to develop a new series of fibrinogen receptor antagonists. Eight new compounds with different condensed heterocyclic parts were prepared and their in vitro activities were evaluated. 5-Amidinobenzofuran compound 2, 6-amidinobenzothiophene 7, and 5-amidinofuro[2,3-b]p...

journal_title：European journal of medicinal chemistry

authors： Ono S,Inoue Y,Yoshida T,Kosaka K,Maeda K,Imada T,Fukaya C,Nakamura N

更新日期：2000-06-01 00:00:00

abstract：:Naturally occurring saponins 3 and 4 have a normal type F ring and alpha-arranged CH(3)-21 group. Treatments of pseudosaponin peracetates 18 and 19 derived from 3 and 4, respectively, with alcoholic KOH, followed by acidification with acetic acid, gave spirostanols 20 and 22 having iso type F rings as major products. ...

journal_title：European journal of medicinal chemistry

authors： Tobari A,Teshima M,Koyanagi J,Kawase M,Miyamae H,Yoza K,Takasaki A,Nagamura Y,Saito S

更新日期：2000-05-01 00:00:00

abstract：:The quantitative dependencies of in vitro fungistatic action on the physico-chemical parameters connected with the structure of 2, 4-dihydroxythiobenzanilides were investigated. It was stated that the action of these compounds depends on lipophilicity determined by substitution of the N-aryl moiety and on electron pro...

journal_title：European journal of medicinal chemistry

authors： Matysiak J,Niewiadomy A,Macik-Niewiadomy G,Kornillowicz T

更新日期：2000-04-01 00:00:00

abstract：:Several novel semicarbazone derivatives were prepared from 5-nitro-2-furaldehyde or 5-nitrothiophene-2-carboxaldehyde and semicarbazides bearing a spermidine-mimetic moiety. All derivatives presented the E-configuration, as determined by NMR-NOE experiments. These compounds were tested in vitro as potential antitrypan...

journal_title：European journal of medicinal chemistry

authors： Cerecetto H,Di Maio R,González M,Risso M,Sagrera G,Seoane G,Denicola A,Peluffo G,Quijano C,Stoppani AO,Paulino M,Olea-Azar C,Basombrío MA

更新日期：2000-03-01 00:00:00

abstract：:Strokes (intracranial thomboses or haemorrhaging) cause death and disability, but effective treatments are lacking. The metabolism of tryptophan leads to the generation of quinolinic acid, an agonist potentially neurotoxic at glutamate receptors, and kynurenic acid, an antagonist at the same population of receptors. T...

journal_title：European journal of medicinal chemistry

authors： Stone TW

更新日期：2000-02-01 00:00:00

abstract：:We report the synthesis and biological in vitro activities of 16 new 2-quinoxalinecarbonitrile 1,4-di-N-oxides. These compounds present new basic lateral chains (piperazines and anilines) in the 3 position as well as different substituents in the 6 and/or 7 positions of the quinoxaline ring. Among piperazine derivativ...

journal_title：European journal of medicinal chemistry

authors： Ortega MA,Morancho MJ,Martínez-Crespo FJ,Sainz Y,Montoya ME,López de Ceráin A,Monge A

更新日期：2000-01-01 00:00:00