当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Use of copper(I) catalyzed azide alkyne cycloaddition (CuAAC) for the preparation of conjugated pyrrolo[2,3-a]carbazole Pim kinase inhibitors.

Use of copper(I) catalyzed azide alkyne cycloaddition (CuAAC) for the preparation of conjugated pyrrolo[2,3-a]carbazole Pim kinase inhibitors.

Abstract：

:We have previously demonstrated that pyrrolo[2,3-a]carbazole-3-carbaldehydes are potent Pim kinase inhibitors with in vitro antiproliferative activities. In the present study, we report the synthesis of new pyrrolocarbazoles substituted at the N-10 position. When their ability to inhibit Pim kinase activities were evaluated in in vitro assays, we observed that this nitrogen atom can be substituted without loss of Pim-1 and Pim-3 inhibitory potencies. Moreover, when we added a fluorescent dansyl group (compound 13), we were able to show that 13 penetrates the plasma membrane and enters the cytoplasm.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Letribot B,Akué-Gédu R,Santio NM,El-Ghozzi M,Avignant D,Cisnetti F,Koskinen PJ,Gautier A,Anizon F,Moreau P

doi

10.1016/j.ejmech.2012.02.009

subject

Has Abstract

pub_date

2012-04-01 00:00:00

pages

304-10

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00085-2

journal_volume

50

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Design, synthesis and potential 6 Hz psychomotor seizure test activity of some novel 2-(substituted)-3-{[substituted]amino}quinazolin-4(3H)-one.

    abstract：:Thirty new 2-(substituted)-3-{[substituted]amino}quinazolin-4(3H)-one were designed and synthesized keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and neurotoxicity. The anticonvulsant activity of the titled compounds was assessed using the 6 Hz psychomotor seizur...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.01.009

    authors： Kumar P,Shrivastava B,Pandeya SN,Stables JP

    更新日期：2011-04-01 00:00:00

  • New dimeric cyclodiphosph(V)azane complexes of Cr(III), Co(II), Ni(II), Cu(II), and Zn(II): preparation, characterization and biological activity studies.

    abstract：:The complexes of type [CrLCl](2).3.5H(2)O and [ML(H(2)O)](2).nH(2)O in which M = Co(II); n = 1, Ni(II); n = 4, Cu(II); n = 0.5 and Zn(II); n = 2 ions and L is 1,3-dimethyl-2,4-dioxo-2',4'-bis(2iminothiophene)cyclodiphosph(V)azane, were prepared and their structures characterized by elemental analysis, IR, (1)H NMR, (3...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.12.008

    authors： Alaghaz AN,Ammar RA

    更新日期：2010-04-01 00:00:00

  • Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.

    abstract：:Small molecules that can restore biological function to the p53 mutants found in human cancers have been highly sought to increase the anticancer efficacy. In efforts to generate hybrid anticancer drugs that can impact two or more targets simultaneously, we designed and developed piperlongumine (PL) derivatives with a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.10.052

    authors： Punganuru SR,Madala HR,Venugopal SN,Samala R,Mikelis C,Srivenugopal KS

    更新日期：2016-01-01 00:00:00

  • Heparin-polynitroxides: synthesis and preliminary evaluation as cardiovascular EPR/MR imaging probes and extracellular space-targeted antioxidants.

    abstract：:We report here the synthesis of heparin-polynitroxide derivatives (HPNs) in which nitroxide moieties are linked either to uronic acid or glycosamine residues of the heparin macromolecule. HPNs have low anticoagulant activity, possess superoxide scavenging properties, bind to the vascular endothelium/extra-cellular mat...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.09.028

    authors： Kleschyov AL,Sen' V,Golubev V,Münnemann K,Hinderberger D,Lackner KJ,Weber S,Terekhov M,Schreiber LM,Münzel T

    更新日期：2012-12-01 00:00:00

  • Synthesis and in vitro cytostatic activity of new beta-D-arabino furan[1',2':4,5]oxazolo- and arabino-pyrimidinone derivatives.

    abstract：:A series of nucleoside derivatives was obtained via heteroatom annulation of the amino oxazoline of D-(-)-arabinose. Unequivocal proofs for the stereostructure of some new arabinosyl pyrimidinone derivatives were obtained by X-ray structure analysis. These newly synthesized compounds were then evaluated for their cyto...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.10.032

    authors： Bosc JJ,Latxague L,Léger JM,Balzarini J,Forfar I,Jarry C,Guillon J

    更新日期：2010-02-01 00:00:00

  • Design, synthesis and preliminary bioactivity evaluations of 8-hydroxyquinoline derivatives as matrix metalloproteinase (MMP) inhibitors.

    abstract：:Matrix metalloproteinases (MMPs) play important roles in many diseases including cancer. With moderate metal-binding affinity, 8-hydroxyquinoline has gained much interest in current drug design and development. Specially, it has been reported that 8-hydroxyquinoline derivatives serve as MMP-2 inhibitors with micromola...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111563

    authors： Chen C,Yang X,Fang H,Hou X

    更新日期：2019-11-01 00:00:00

  • 5-Ene-4-thiazolidinones induce apoptosis in mammalian leukemia cells.

    abstract：:The article presents the synthesis of 5-ene-4-thiazolidinone derivatives with pyrazole core linked by enamine group. The structure and purity of compounds were confirmed by analytical and spectral data including X-ray analysis. Target compounds were screened for their anticancer activity and selective antileukemic act...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.03.089

    authors： Senkiv J,Finiuk N,Kaminskyy D,Havrylyuk D,Wojtyra M,Kril I,Gzella A,Stoika R,Lesyk R

    更新日期：2016-07-19 00:00:00

  • Synthesis, analgesic and anti-inflammatory activities evaluation of some bi-, tri- and tetracyclic condensed pyrimidines.

    abstract：:Novel series of bicyclic pyrrolo[1,2-c]pyrimidines 3a-g, 5, 6a, b, and 7a, b, tricyclic pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines 8a-c, 9a-g, 13a-c, 17, 18a, b, 19, 20a,b and 21 and tetracyclic condensed pyrimidines 14, 22 and 23 were synthesized through different chemical reactions. Structures of all synthesized pyrim...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.06.028

    authors： Amin KM,Hanna MM,Abo-Youssef HE,George RF

    更新日期：2009-11-01 00:00:00

  • Design, synthesis, biological evaluation, and comparative docking study of 1,2,4-triazolones as CB1 receptor selective antagonists.

    abstract：:Cannabinoids are potentially useful for the treatment of several diseases. In the present work, we report the syntheses and biological evaluations of 1,2,4-triazolone derivatives designed using a combined approach of scaffold hopping and pharmacophore-oriented method. These compounds exhibited interesting antagonistic...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.12.018

    authors： Han S,Zhang FF,Xie X,Chen JZ

    更新日期：2014-03-03 00:00:00

  • Synthesis, biological evaluation and molecular docking studies of some pyrimidine derivatives.

    abstract：:Some novel pyrimidine-5-carbonitrile derivatives bearing various substituent have been synthesized. The structures of target compounds were confirmed by elemental analysis and spectral data. Some selected members of the newly synthesized compounds were investigated for their cytotoxic potency against certain human tum...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.05.028

    authors： Fargualy AM,Habib NS,Ismail KA,Hassan AM,Sarg MT

    更新日期：2013-08-01 00:00:00

  • Design, synthesis, and structure-activity relationships of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety as potent antitumor agents.

    abstract：:A series of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety were designed and synthesized and their cytotoxic activities against five cancer cell lines (NCI-H226, SK-N-SH, HT29, MKN45, and MDA-MB-231) were screened in vitro. Most of them showed moderate to excellent activity again...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.08.058

    authors： Ma J,Chen D,Lu K,Wang L,Han X,Zhao Y,Gong P

    更新日期：2014-10-30 00:00:00

  • 3,5-Diaryl-1H-pyrazolo[3,4-b]pyridines as potent tubulin polymerization inhibitors: Rational design, synthesis and biological evaluation.

    abstract：:A series of novel 3,5-diaryl-1H-pyrazolo[3,4-b]pyridines as tubulin polymerization inhibitors targeting the colchicine site were designed via ring tethering strategy, which was supported by conformational analysis. The general, chemically unstable and rotational linker, carbanyl group, was locked by 1H-pyrazolo[3,4-b]...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.12.053

    authors： Zhai M,Liu S,Gao M,Wang L,Sun J,Du J,Guan Q,Bao K,Zuo D,Wu Y,Zhang W

    更新日期：2019-04-15 00:00:00

  • Indole based antimalarial compounds targeting the melatonin pathway: Their design, synthesis and biological evaluation.

    abstract：:Malaria, one of the most severe global diseases, infects nearly 300 million people causing death of about a million population annually. Herein we have reported design, synthesis and biological evaluation of potent antimalarial compounds that target melatonin hormone as a potential pathway for the inhibition of the pa...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.02.019

    authors： Luthra T,Nayak AK,Bose S,Chakrabarti S,Gupta A,Sen S

    更新日期：2019-04-15 00:00:00

  • Discovery of colon tumor cell growth inhibitory agents through a combinatorial approach.

    abstract：:Two series with the general formula of 4,6-diaryl-2-oxo-1,2 dihydropyridine-3-carbonitriles and their isosteric 4,6-diaryl-2-imino-1,2-dihydropyridine-3-carbonitrile were synthesized through one pot reaction of the appropriate acetophenone, aldehyde, ammonium acetate with ethyl cyanoacetate or malononitrile, respectiv...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.09.029

    authors： Abadi AH,Abouel-Ella DA,Lehmann J,Tinsley HN,Gary BD,Piazza GA,Abdel-Fattah MA

    更新日期：2010-01-01 00:00:00

  • Discovery of a benzenesulfonamide-based dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase that favorably modulates lipid mediator biosynthesis in inflammation.

    abstract：:Leukotrienes (LTs) and prostaglandin (PG)E2, produced by 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1), respectively, are key players in inflammation, and pharmacological suppression of these lipid mediators (LM) represents a strategy to intervene with inflammatory disorders. Previous stud...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.07.031

    authors： Cheung SY,Werner M,Esposito L,Troisi F,Cantone V,Liening S,König S,Gerstmeier J,Koeberle A,Bilancia R,Rizza R,Rossi A,Roviezzo F,Temml V,Schuster D,Stuppner H,Schubert-Zsilavecz M,Werz O,Hanke T,Pace S

    更新日期：2018-08-05 00:00:00

  • Structure-based drug design: Synthesis and biological evaluation of quinazolin-4-amine derivatives as selective Aurora A kinase inhibitors.

    abstract：:Aurora kinases play critical roles in the regulation of the cell cycle and mitotic spindle assembly. Aurora A kinase, a member of the Aurora protein family, is frequently highly expressed in tumors, and selective Aurora A inhibition serves as a significant component of anticancer therapy. However, designing highly sel...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.08.053

    authors： Long L,Wang YH,Zhuo JX,Tu ZC,Wu R,Yan M,Liu Q,Lu G

    更新日期：2018-09-05 00:00:00

  • Chemotherapy of leishmaniasis part-VIII: synthesis and bioevaluation of novel chalcones.

    abstract：:Some novel dihydro-alpha-ionone based chalcones have been synthesized and evaluated for their in vitro antileishmanial activity in promastigote and amastigote model. Some of the compounds showed 100% inhibition at 5 and 2 microm/ml concentration. ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.12.014

    authors： Suryawanshi SN,Chandra N,Kumar P,Porwal J,Gupta S

    更新日期：2008-11-01 00:00:00

  • Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.

    abstract：:Inspired by the traditional Chinese herbal pair of Polygala tenuifolia-Acori Tatarinowii for treating epilepsy, 33 novel substituted cinnamic α-asaronol esters and analogues were designed by Combination of Traditional Chinese Medicine Molecular Chemistry (CTCMMC) strategy, synthesized and tested systematically not onl...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111650

    authors： Bai Y,He X,Bai Y,Sun Y,Zhao Z,Chen X,Li B,Xie J,Li Y,Jia P,Meng X,Zhao Y,Ding Y,Xiao C,Wang S,Yu J,Liao S,Zhang Y,Zhu Z,Zhang Q,Zhao Y,Qin F,Zhang Y,Wei X,Zeng M,Liang J,Cuan Y,Shan G,Fan TP,Wu B

    更新日期：2019-12-01 00:00:00

  • Attenuation of Mycobacterium species through direct and macrophage mediated pathway by unsymmetrical diaryl urea.

    abstract：:Tuberculosis is a major threat for mankind and the emergence of resistance strain of Mycobacterium tuberculosis (Mtb) against first line antibiotics makes it lethal for human civilization. In this study, we have synthesized different diaryl urea derivatives targeting the inhibition of mycolic acid biosynthesis. Among ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.09.083

    authors： Velappan AB,Charan Raja MR,Datta D,Tsai YT,Halloum I,Wan B,Kremer L,Gramajo H,Franzblau SG,Kar Mahapatra S,Debnath J

    更新日期：2017-01-05 00:00:00

  • Benzofuran derivatives as anticancer inhibitors of mTOR signaling.

    abstract：:A series of 32 derivatives and isosteres of the mTOR inhibitor 2 were synthesized and compared for their cytotoxicity in radioresistant SQ20B cancer cell line. Several of these compounds, in particular 30b, were significantly more cytotoxic than 2. Importantly, 30b was shown to block both mTORC1 and Akt signaling, sug...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.05.014

    authors： Salomé C,Ribeiro N,Chavagnan T,Thuaud F,Serova M,de Gramont A,Faivre S,Raymond E,Désaubry L

    更新日期：2014-06-23 00:00:00

  • Design, synthesis and biological evaluation of chalconyl blended triazole allied organosilatranes as giardicidal and trichomonacidal agents.

    abstract：:A series of chalconyl blended triazole allied silatranes (7a-g/8a-g/9a-g) were synthesized in good yields using a simple, economical and biocompatible synthetic route. The blend of three different pharmacologically active moieties into a single scaffold resulted into synergistic effect in their bio-activity. Various s...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.11.029

    authors： Singh G,Arora A,Mangat SS,Rani S,Kaur H,Goyal K,Sehgal R,Maurya IK,Tewari R,Choquesillo-Lazarte D,Sahoo S,Kaur N

    更新日期：2016-01-27 00:00:00

  • Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors.

    abstract：:Shikonin exhibits powerful anticancer activities for various cancer cells, but its poor solubility and strong toxicity hinder its development as clinical anticancer agent. We previously confirmed that shikonin and its derivatives can disturb mitosis through targeting tubulin. In this study, α-lipoic acid, the naturall...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.12.019

    authors： Lin HY,Han HW,Sun WX,Yang YS,Tang CY,Lu GH,Qi JL,Wang XM,Yang YH

    更新日期：2018-01-20 00:00:00

  • Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents.

    abstract：:A series of triazin-3(2H)-one derivatives bearing 1,3,4-oxadiazole (4a-4o) were synthesized, characterized and evaluated for anti-inflammatory and analgesic activities. Preliminary in vitro anti-inflammatory activity was assessed using an albumin denaturation assay. The promising compounds were further evaluated in ac...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.06.020

    authors： Banerjee AG,Das N,Shengule SA,Srivastava RS,Shrivastava SK

    更新日期：2015-08-28 00:00:00

  • Development of resveratrol-curcumin hybrids as potential therapeutic agents for inflammatory lung diseases.

    abstract：:Acute lung injury (ALI) is a major cause of acute respiratory failure in critically-ill patients. Resveratrol and curcumin are proven to have potent anti-inflammatory efficacy, but their clinical application is limited by their metabolic instability. Here, a series of resveratrol and the Mono-carbonyl analogs of curcu...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.09.033

    authors： Pan J,Xu T,Xu F,Zhang Y,Liu Z,Chen W,Fu W,Dai Y,Zhao Y,Feng J,Liang G

    更新日期：2017-01-05 00:00:00

  • Synthesis and primary cytotoxicity evaluation of new imidazo[2,1-b]thiazole derivatives.

    abstract：:A series of arylidenehydrazides (3a-3i) were synthesized from [6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetic acid hydrazide. The structures of new compounds were determined by analytical and spectral (IR, (1)H NMR, (13)C NMR, EIMS) methods. The synthesized compounds (3a-3i) were evaluated in the National Cancer I...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.10.012

    authors： Gürsoy E,Güzeldemirci NU

    更新日期：2007-03-01 00:00:00

  • Discovery and optimization of phthalazinone derivatives as a new class of potent dengue virus inhibitors.

    abstract：:Using a dengue replicon cell line-based screening, we identified 3-(dimethylamino)propyl(3-((4-(4-fluorophenyl)-1-oxophthalazin-2(1H)-yl)methyl)phenyl)carbamate (10a) as a potent DENV-2 inhibitor, with an IC50 value of 0.64 μM. A series of novel phthalazinone derivatives based on hit 10a were synthesized and evaluated...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.01.008

    authors： Lu D,Liu J,Zhang Y,Liu F,Zeng L,Peng R,Yang L,Ying H,Tang W,Chen W,Zuo J,Tong X,Liu T,Hu Y

    更新日期：2018-02-10 00:00:00

  • Synthesis, properties, and perspectives of gem-diphosphono substituted-thiazoles.

    abstract：:A series of substituted arylidene thiazoles were allowed to react with Wittig-Horner (WH) reagent, tetraethyl methyl-1,1-bisphosphonate, to produce via Michael addition reaction the corresponding heteroarylmethylenebisphosphonates (BPs) in different yields according to the experimental conditions. Acid hydrolysis of t...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.07.005

    authors： Abdou WM,Ganoub NA,Geronikaki A,Sabry E

    更新日期：2008-05-01 00:00:00

  • Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype.

    abstract：:We report the design, synthesis and pharmacological screening of a group of analogues of anabaseine 2, a naturally occurring unselective nicotinic agonist. The novel nAChR ligands 5-15 were planned following a molecular modeling analysis which suggested the replacement of the pyridine ring of 2 with a 3-substituted be...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.11.045

    authors： Matera C,Quadri M,Sciaccaluga M,Pomè DY,Fasoli F,De Amici M,Fucile S,Gotti C,Dallanoce C,Grazioso G

    更新日期：2016-01-27 00:00:00

  • Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.

    abstract：:A series of Lapatinib derivatives were designed and prepared by changing the straight alkyl side chain of Lapatinib into a branched one. ELISA assay and western blot analysis showed that these derivatives can significantly inhibit HER1/HER2 as well as their downstream signal transduction proteins. In vitro cytotoxicit...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.10.006

    authors： Lyu A,Fang L,Gou S

    更新日期：2014-11-24 00:00:00

  • Synthesis and anticancer activity of γ-(triazolyl ethylidene)butenolides and polyfunctional pyrrolinones.

    abstract：:A series of novel γ-(triazolyl ethylidene)butenolides (4-23) were prepared from commercially available l-ascorbic acid in good yields. These butenolides on reaction with ethanolic ammonia/amines led to formation of respective 5-hydroxy pyrrolinones (24-33). The two of these pyrrolinones on dehydration with p-toluenesu...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.05.042

    authors： Devender N,Ramakrishna KK,Hamidullah,Shukla SK,Konwar R,Tripathi RP

    更新日期：2014-07-23 00:00:00