Synthesis and neuromuscular blocking activity of 16beta-piperidinosteroidal derivatives.

abstract：:As a part of the research on the improvement of an alternative to conventional photodynamic therapy by light-induced formation of intercalators, we synthesized a series of novel heterocyclic compounds and their acyclic precursors. We now report details about their synthesis/characterization in respect to their potenti...

journal_title：European journal of medicinal chemistry

authors： Starcević K,Kralj M,Piantanida I,Suman L,Pavelić K,Karminski-Zamola G

更新日期：2006-08-01 00:00:00

abstract：:Emulsions have shown great potential in the delivery of various types of cargoes such as nucleic acids and proteins. In this study, fluorinated polymer emulsions (PFx@PFD-n) were prepared using fluorinated polymers with different structures as surfactant in PFD emulsions under ultrasound. These polymer emulsions gave ...

journal_title：European journal of medicinal chemistry

authors： Xiao YP,Zhang J,Liu YH,Huang Z,Yu XQ

更新日期：2020-12-01 00:00:00

abstract：:Survival of the human malaria parasite Plasmodium falciparum is dependent on pantothenate (vitamin B5), a precursor of the fundamental enzyme cofactor coenzyme A. CJ-15,801, an enamide analogue of pantothenate isolated from the fungus Seimatosporium sp. CL28611, was previously shown to inhibit P. falciparum proliferat...

journal_title：European journal of medicinal chemistry

authors： Spry C,Sewell AL,Hering Y,Villa MVJ,Weber J,Hobson SJ,Harnor SJ,Gul S,Marquez R,Saliba KJ

更新日期：2018-01-01 00:00:00

abstract：:Taking the rising interest in jasmone structure based fragrant compounds into account it has been decided to take up an attempt to synthesize the new heterocyclic derivatives of this 2,3-disubstituted cyclopentenone, which could be characterized by the ability of interaction with the same receptors with which jasmone ...

journal_title：European journal of medicinal chemistry

authors： Pawełczyk A,Zaprutko L

更新日期：2009-07-01 00:00:00

abstract：:Succinate dehydrogenase inhibitors (SDHIs) are efficient fungicides that are widely used to control plant diseases caused by phytopathogenic fungi, although their effectiveness is undermined by the development of resistance across a range of different fungi. One of the most common structural features of SDHIs is their...

journal_title：European journal of medicinal chemistry

authors： Wang ZJ,Gao Y,Hou YL,Zhang C,Yu SJ,Bian Q,Li ZM,Zhao WG

更新日期：2014-10-30 00:00:00

abstract：:PDT is a well-established therapeutic modality for many types of cancer. Photoluminescent cyclometalated iridium(III) complexes are one of the most commonly used classes of organometallic compounds with potential beneficial applications in bioimaging and as promising anticancer agents. In the present study, three new ...

journal_title：European journal of medicinal chemistry

authors： Song XD,Chen BB,He SF,Pan NL,Liao JX,Chen JX,Wang GH,Sun J

更新日期：2019-10-01 00:00:00

abstract：:EGFR and VEGFR-2 are involved in pathological disorders and the progression of different kinds of tumors, the combined blockade of EGFR and VEGFR signaling pathways appears to be an attractive approach to cancer therapy. In this work, a series of 4-anilinoquinazoline derivatives containing substituted diaryl urea or g...

journal_title：European journal of medicinal chemistry

authors： Zhang HQ,Gong FH,Ye JQ,Zhang C,Yue XH,Li CG,Xu YG,Sun LP

更新日期：2017-01-05 00:00:00

abstract：:A series of sixteen novel thiazolidinone derivatives were synthesized from the efficient one-pot reaction of 2-(piperidin-1-yl)ethylamine, arenealdehydes and mercaptoacetic acid in good yields. Identification and characterization of products were achieved by NMR and GC-MS techniques. The in vitro antifungal activities...

journal_title：European journal of medicinal chemistry

authors： Kunzler A,Neuenfeldt PD,das Neves AM,Pereira CM,Marques GH,Nascente PS,Fernandes MH,Hübner SO,Cunico W

更新日期：2013-06-01 00:00:00

abstract：:Curcumin (CU), an edible natural pigment from Curcuma Longa, has demonstrated extensive anti-tumor effect in vivo and in vitro. With the property of reversing drug resistance and low toxicity, CU has been considered to develop a new adjuvant chemotherapy protocol of cancer. However, the poor stability, solubility, in ...

journal_title：European journal of medicinal chemistry

authors： Zhao S,Pi C,Ye Y,Zhao L,Wei Y

更新日期：2019-10-15 00:00:00

abstract：:A series of 1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives were synthesized by the cyclization of novel 2-(quinolin-8-yloxy) acetohydrazones. In vitro antiamoebic activity was performed against HM1: IMSS strain of Entamoeba histolytica. The results showed that all the 2-(quinolin-8-yloxy) acetohydrazones were m...

journal_title：European journal of medicinal chemistry

authors： Hayat F,Salahuddin A,Zargan J,Azam A

更新日期：2010-12-01 00:00:00

abstract：:Identification and investigation of novel classes and compounds for the treatment of tuberculosis remains of utmost importance in the fight against the disease. Despite many efforts, the weakly gram positive Mycobacterium tuberculosis keeps demanding its toll in human lives. For this reason a small library of substitu...

journal_title：European journal of medicinal chemistry

authors： Claes P,Cappoen D,Mbala BM,Jacobs J,Mertens B,Mathys V,Verschaeve L,Huygen K,De Kimpe N

更新日期：2013-09-01 00:00:00

abstract：:1,4-Dihydropyridine-3,5-dicarboxylate derivatives (1-25) were synthesized in high yields via Hantzsch reaction and evaluated for their α-glucosidase inhibitory activity. Compounds 1, 2, 6-8, 11, 13-15, and 23-25 showed a potent inhibitory activity against yeast α-glucosidase with IC50 values in the range of 35.0-273.7...

journal_title：European journal of medicinal chemistry

authors： Niaz H,Kashtoh H,Khan JA,Khan A,Wahab AT,Alam MT,Khan KM,Perveen S,Choudhary MI

更新日期：2015-05-05 00:00:00

abstract：:Oxindole has emerged as a valuable scaffold in medicinal chemistry possessing diverse range of pharmacological activities. Its value has further been increased by its natural occurrence as alkaloids in variety of plants. It was first extracted from the cat claw's plant Uncaria tomentosa found in the Amazon rainforest ...

journal_title：European journal of medicinal chemistry

authors： Kaur M,Singh M,Chadha N,Silakari O

更新日期：2016-11-10 00:00:00

abstract：:To evaluate N-hydroxyurea as zinc binding group in the design of MMP inhibitors, two peptidyl 1-hydroxyureas were prepared by N-hydroxycarbamoylation of the diastereomeric dipeptides H-Leu-Phe-NHMe and H-D-Leu-Phe-NHMe. Peptidyl 1-hydroxyureas were more potent than the parent peptides, but dramatically weaker (4-5 ord...

journal_title：European journal of medicinal chemistry

authors： Campestre C,Tortorella P,Agamennone M,Preziuso S,Biasone A,Nuti E,Rossello A,Gallina C

更新日期：2008-05-01 00:00:00

abstract：:A series of 2-(benzylthio)-5-aryloxadiazole derivatives have been designed and synthesized, and their biological activities are also evaluated for EGFR inhibitory activity. Fourteen compounds among the twenty compounds are reported for the first time. Their chemical structures are characterized by (1)H NMR, MS, and el...

journal_title：European journal of medicinal chemistry

authors： Liu K,Lu X,Zhang HJ,Sun J,Zhu HL

更新日期：2012-01-01 00:00:00

abstract：:The present work involves design and synthesis of new substituted 1,4-dihydropyridin-4-yl-phenoxyacetohydrazones (4a-s, 5a-h), starting from 4-hydroxybenzaldehyde. The final compounds were screened for their in vivo anticonvulsant activity by MES, scPTZ and 6 Hz methods, while their anti-inflammatory screening was per...

journal_title：European journal of medicinal chemistry

authors： Ulloora S,Shabaraya R,Ranganathan R,Adhikari AV

更新日期：2013-01-01 00:00:00

abstract：:A series of novel indole-chalcone fibrates were synthesized and their hypolipidemic activity was evaluated in triton WR-1339 induced hyperlipidemic rat model. Preliminary studies indicated that the hybrids 19, 24 and 29 exhibited potent in vitro antioxidant and significant in vivo antidyslipidemic effects. Our results...

journal_title：European journal of medicinal chemistry

authors： Sashidhara KV,Dodda RP,Sonkar R,Palnati GR,Bhatia G

更新日期：2014-06-23 00:00:00

abstract：:The synthesis of some novel Ospemifene derived analogs and their evaluation as anti-breast cancer agents against MCF-7 (ER-positive) and MDA-MB-231 (ER-negative) human breast cancer cell lines are described. Few of these analogs for instance, compounds 6, 7 and 8 are shown to be more effective than recent Selective Es...

journal_title：European journal of medicinal chemistry

authors： Kaur G,Mahajan MP,Pandey MK,Singh P,Ramisetti SR,Sharma AK

更新日期：2014-10-30 00:00:00

abstract：:Two series of novel pyrazolobenzothiazine-based hybrid compounds were efficiently synthesized starting from saccharin sodium salt. Pyrazolo[4,3-c][1,2]benzothiazine scaffolds were N-arylated by using p-fluorobenzaldehyde, followed by the incorporation of a benzimidazole or similar ring systems by treatment with arylen...

journal_title：European journal of medicinal chemistry

authors： Aslam S,Zaib S,Ahmad M,Gardiner JM,Ahmad A,Hameed A,Furtmann N,Gütschow M,Bajorath J,Iqbal J

更新日期：2014-05-06 00:00:00

abstract：:The activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6 kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most active compounds indica...

journal_title：European journal of medicinal chemistry

authors： Andreani A,Granaiola M,Leoni A,Locatelli A,Morigi R,Rambaldi M,Varoli L,Lannigan D,Smith J,Scudiero D,Kondapaka S,Shoemaker RH

更新日期：2011-09-01 00:00:00

abstract：:The use of nitroreductases (NTR) that catalyze the reduction of nitro compounds by using NAD(P)H in GDEPT (Gene-directed enzyme prodrug therapy) studies which minimize toxicity at healthy cells and increases concentration of drugs at cancer cells is remarkable. Discovery of new prodrug/NTR combinations is necessary to...

journal_title：European journal of medicinal chemistry

authors： Güngör T,Önder FC,Tokay E,Gülhan ÜG,Hacıoğlu N,Tok TT,Çelik A,Köçkar F,Ay M

更新日期：2019-06-01 00:00:00

abstract：:A series of novel triptolide/furoxans hybrids were designed and synthesized as analogues of triptolide, which is a naturally derived compound isolated from the thunder god vine (Tripterygium wilfordii Hook. F). Some of these synthesized compounds exhibited antiproliferative activities in the nanomolar range. Among the...

journal_title：European journal of medicinal chemistry

authors： Zang Y,Lai F,Fu J,Li C,Ma J,Chen C,Liu K,Zhang T,Chen X,Zhang D

更新日期：2020-03-15 00:00:00

abstract：:Thirty-five 3-aryl-4-arylaminofuran-2(5H)-one derivatives were designed, prepared and tested for their inhibitory activity against tyrosyl-tRNA synthetase. Out of these compounds, 3-(3-bromophenyl)-4-(3,5-dichlorophenylamino)furan-2(5H)-one (35) was the most active with IC(50) of 0.09 ± 0.02 μM. The structure-activity...

journal_title：European journal of medicinal chemistry

authors： Xiao ZP,Ma TW,Liao ML,Feng YT,Peng XC,Li JL,Li ZP,Wu Y,Luo Q,Deng Y,Liang X,Zhu HL

更新日期：2011-10-01 00:00:00

abstract：:A series of novel diastereoisomeric σ ligands 3 was designed, synthesized and pharmacologically evaluated. The highly rigid [4.3.3]propellane scaffold was used to fix the three dimensional orientation of the pharmacophoric moieties required for σ affinity. The syn,syn-configured aminocarbamate syn,syn-3a reveals the m...

journal_title：European journal of medicinal chemistry

authors： Torres-Gómez H,Lehmkuhl K,Schepmann D,Wünsch B

更新日期：2013-01-01 00:00:00

abstract：:QSAR analysis for modeling the antileishmanial activity screening of a series of 49 nitro derivatives of Hydrazides were carried out using different Chemometrics methods. First, a large number of descriptors were calculated using Hyperchem, Mopac and Dragon softwares. Then, a suitable number of these descriptors were ...

journal_title：European journal of medicinal chemistry

authors： Garkani-Nejad Z,Ahmadi-Roudi B

更新日期：2010-02-01 00:00:00

abstract：:In the search of structure-activity relationship studies and to explore the antitumor effect associated with the pyrimidoisoquinolinequinone scaffold, several diversily substituted 8-aminopyrimido[4,5-c]isoquinolinequinones were regioselectively synthesized. Variation in the structure of the nitrogen substituent bonde...

journal_title：European journal of medicinal chemistry

authors： Vásquez D,Rodríguez JA,Theoduloz C,Calderon PB,Valderrama JA

更新日期：2010-11-01 00:00:00

abstract：:Four mexiletine analogues have been tested for their antiarrhythmic, inotropic, and chronotropic effects on isolated guinea pig heart tissues and to assess calcium antagonist activity, in comparison with the parent compound mexiletine. All analogues showed from moderate to high antiarrhythmic activity. In particular, ...

journal_title：European journal of medicinal chemistry

authors： Roselli M,Carocci A,Budriesi R,Micucci M,Toma M,Di Cesare Mannelli L,Lovece A,Catalano A,Cavalluzzi MM,Bruno C,De Palma A,Contino M,Perrone MG,Colabufo NA,Chiarini A,Franchini C,Ghelardini C,Habtemariam S,Lentini G

更新日期：2016-10-04 00:00:00

abstract：:For the optimization of the plakortin pharmacophore, we recently proposed a straightforward synthesis of 4-carbomethoxy-3-methoxy-1,2-dioxanes as potential antimalarial drug candidates. Herein we report the chemoselective reduction of the 4-carbomethoxy group which has allowed us to prepare in good yields twenty-four ...

journal_title：European journal of medicinal chemistry

authors： Persico M,Parapini S,Chianese G,Fattorusso C,Lombardo M,Petrizza L,Quintavalla A,Rondinelli F,Basilico N,Taramelli D,Trombini C,Fattorusso E,Taglialatela-Scafati O

更新日期：2013-01-01 00:00:00

abstract：:Mono- and diacylated derivatives of galactopyranosyl amines were obtained from d-galactose, via aminated intermediates prepared by reaction of 6-deoxy-6-iodo-1,2:3,4-di-O-isopropylidene-alpha-d-galactopyranose with 1,3-propanediamine, 1,2-ethanediamine or ethanolamine. Monoacylated derivatives displayed antitubercular...

journal_title：European journal of medicinal chemistry

authors： de Almeida MV,Le Hyaric M,Amarante GW,Silva Lourenço MC,Lima Brandão ML

更新日期：2007-08-01 00:00:00

abstract：:2-methoxyestradiol is a novel agent showing both anti-angiogenic and vascular disrupting properties. In this study, a series of 11α-substituted 2-methoxyestradiol analogs have been designed and synthesized targeting dual ERα and microtubulin. Biological evaluation was performed on their anti-proliferative activities a...

journal_title：European journal of medicinal chemistry

authors： Lao K,Wang Y,Chen M,Zhang J,You Q,Xiang H

更新日期：2017-10-20 00:00:00