当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues.

Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues.

Abstract：

:Two series of 2-aroyltrimethoxyindoles were designed to investigate the effects of the replacement of the trimethoxyphenyl ring of phenstatin with a trimethoxyindole moiety. These compounds were efficiently prepared through a domino palladium-catalyzed sequence from 2-gem-dibromovinylanilines substituted by three methoxy groups and arylboronic acids under carbon monoxide atmosphere. These novel heterocyclic combretastatin A4 analogues were evaluated for their cell growth inhibitory properties and their ability to inhibit the tubulin polymerization.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Arthuis M,Pontikis R,Chabot GG,Quentin L,Scherman D,Florent JC

doi

10.1016/j.ejmech.2010.10.018

subject

Has Abstract

pub_date

2011-01-01 00:00:00

pages

95-100

issue

1

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(10)00758-0

journal_volume

46

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.

    abstract：:Six series of semisynthetic lipophilic glycopeptide antibiotic derivatives were evaluated for in vitro activity against influenza A and B viruses. The new teicoplanin pseudoaglycon-derived lipoglycopeptides were prepared by coupling one or two side chains to the N-terminus of the glycopeptide core, using various conju...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.08.058

    authors： Szűcs Z,Kelemen V,Le Thai S,Csávás M,Rőth E,Batta G,Stevaert A,Vanderlinden E,Naesens L,Herczegh P,Borbás A

    更新日期：2018-09-05 00:00:00

  • Design, synthesis and antitubercular evaluation of novel series of N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives.

    abstract：:The analogs of N-[4-(piperazin-1-yl)phenyl]cinnamamide were designed and synthesized by molecular hybridization approach in which part C of the designed molecule was linked through amide and carbamate functionality that improves the physicochemical properties and govern the pharmacokinetic and pharmacodynamic behavior...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.01.024

    authors： Patel KN,Telvekar VN

    更新日期：2014-03-21 00:00:00

  • Novel series of 6-(2-substitutedacetamido)-4-anilinoquinazolines as EGFR-ERK signal transduction inhibitors in MCF-7 breast cancer cells.

    abstract：:Epidermal growth factor receptor (EGFR) signaling pathway has been previously investigated for its significant role in the progression of different types of malignant tumors, where development of small molecules targeting EGFR is well known strategy for design of antitumor agents. Herein, we report the design and synt...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.06.024

    authors： Ismail RSM,Abou-Seri SM,Eldehna WM,Ismail NSM,Elgazwi SM,Ghabbour HA,Ahmed MS,Halaweish FT,Abou El Ella DA

    更新日期：2018-07-15 00:00:00

  • Synthesis, brain antihypoxic activity and cell neuroprotection of 1-substituted-3,7-dimethylxanthines.

    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

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)01172-7

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

    更新日期：2000-10-01 00:00:00

  • 3,8-diazabicyclo--[3.2.1]-octane derivatives as analogues of ambasilide, a Class III antiarrhythmic agent.

    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

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(01)01246-6

    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

  • Synthesis, characterization and cytotoxicity of ammine/ethylamine platinum(II) complexes with carboxylates.

    abstract：:Six new mixed ammine/ethylamine platinum(II) complexes with carboxylates [Pt(II)(NH(3))(C(2)H(5)NH(2))X(2)] (a-f) (X = CH(3)COO(-), CH(2)ClCOO(-), C(6)H(5)-COO(-), p-CH(3)-C(6)H(4)-COO(-), p-CH(3)O-C(6)H(4)-COO(-), p-NO(2)-C(6)H(4)-COO(-)) (a-f) have been synthesized and characterized by elemental analysis, conductivi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.10.035

    authors： Zhang J,Li Y,Sun J

    更新日期：2009-06-01 00:00:00

  • Optimisation of correlation weights of SMILES invariants for modelling oral quail toxicity.

    abstract：:The SMILES (simplified molecular input line entry system) nomenclature was used to elucidate the molecular structure in constructing the quantitative structure-property/activity relationships (QSPR/QSAR) for predicting quail toxicity after oral exposure. The presence of chemical elements in different electronic states...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.11.018

    authors： Toropov AA,Benfenati E

    更新日期：2007-05-01 00:00:00

  • Discovery of a new selective inhibitor of A Disintegrin And Metalloprotease 10 (ADAM-10) able to reduce the shedding of NKG2D ligands in Hodgkin's lymphoma cell models.

    abstract：:Hodgkin's lymphoma (HL) is the most common malignant lymphoma in young adults in the western world. This disease is characterized by an overexpression of ADAM-10 with increased release of NKG2D ligands, involved in an impaired immune response against tumor cells. We designed and synthesized two new ADAM-10 selective i...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.01.053

    authors： Camodeca C,Nuti E,Tepshi L,Boero S,Tuccinardi T,Stura EA,Poggi A,Zocchi MR,Rossello A

    更新日期：2016-03-23 00:00:00

  • Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation.

    abstract：:We report the design of hetero-bifunctional small molecules that selectively target p38α and p38β for degradation. These proteolysis targeted chimeras (PROTACs) are based on an ATP competitive inhibitor of p38α and p38β, which is linked to thalidomide analogues to recruit the Cereblon E3 ubiquitin ligase complex. Comp...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112451

    authors： Donoghue C,Cubillos-Rojas M,Gutierrez-Prat N,Sanchez-Zarzalejo C,Verdaguer X,Riera A,Nebreda AR

    更新日期：2020-09-01 00:00:00

  • Structure-based discovery of selective BRPF1 bromodomain inhibitors.

    abstract：:Bromodomain and plant homeodomain (PHD) finger containing protein 1 (BRPF1) is a member of subfamily IV of the human bromodomains. Experimental evidence suggests that BRPF1 is involved in leukemia. In a previous high-throughput docking campaign we identified several chemotypes targeting the BRPF1 bromodomain. Here, ph...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.05.037

    authors： Zhu J,Zhou C,Caflisch A

    更新日期：2018-07-15 00:00:00

  • Synthesis and evaluation of xanthine oxidase inhibitory and antioxidant activities of 2-arylbenzo[b]furan derivatives based on salvianolic acid C.

    abstract：:Xanthine oxidase (XO) is the key enzyme in humans which is related to a variety of diseases such as gout, hyperuricemia and cardiovascular diseases. In this work, a series of 2-arylbenzo[b]furan derivatives were synthesized based on salvianolic acid C, and they were evaluated for xanthine oxidase inhibitory and antiox...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.08.019

    authors： Tang HJ,Zhang XW,Yang L,Li W,Li JH,Wang JX,Chen J

    更新日期：2016-11-29 00:00:00

  • Synthesis and antioxidant properties of some novel 5H-dibenz[b,f]azepine derivatives in different in vitro model systems.

    abstract：:A series of 5H-dibenz[b,f]azepine containing different aminophenols and substituted aminophenols were synthesized. 3-chloro-1-(5H-dibenz[b,f]azepine-5yl)propan-1-one (2) was obtained by N-acylation of 5H-dibenz[b,f]azepine (1) with 3-chloro propionyl chloride. Further base condensation with different aminophenols and ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.09.016

    authors： Vijay Kumar H,Naik N

    更新日期：2010-01-01 00:00:00

  • Structure activity relationship studies of natural product chemokine receptor CCR5 antagonist anibamine toward the development of novel anti prostate cancer agents.

    abstract：:Recent studies have indicated that the CCR5 chemokine receptor may be a potential target for treating prostate cancer. Thus, development of CCR5 antagonists may provide novel prostate cancer therapy. Anibamine, a novel pyridine quaternary alkaloid isolated from Aniba sp., was found to effectively compete with (125)I-g...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.07.049

    authors： Zhang F,Arnatt CK,Haney KM,Fang HC,Bajacan JE,Richardson AC,Ware JL,Zhang Y

    更新日期：2012-09-01 00:00:00

  • Discovery of benzothiazole derivatives as novel non-sulfamide NEDD8 activating enzyme inhibitors by target-based virtual screening.

    abstract：:NEDD8 activating enzyme (NAE) plays a critical role in various cellular functions in cancers. In this study, a target-based virtual screening was applied to discover benzothiazoles to be potent non-covalent NAE inhibitors. Further two round optimizations concluded a preliminary structure-activity relationship (SAR) of...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.03.076

    authors： Ma H,Zhuang C,Xu X,Li J,Wang J,Min X,Zhang W,Zhang H,Miao Z

    更新日期：2017-06-16 00:00:00

  • Scaffold hopping strategy toward original pyrazolines as selective CB₂ receptor ligands.

    abstract：:In line of a scaffold hopping strategy of pyrazole structures, especially known as potent CB(2) receptor antagonists, we exploited an original and convergent synthesis of a new class of C4-benzyl pyrazolines and derivatives from readily available hydrazones and enones (two or three steps). Making use of a mixture of r...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.10.031

    authors： Gembus V,Furman C,Millet R,Mansouri R,Chavatte P,Levacher V,Brière JF

    更新日期：2012-12-01 00:00:00

  • 2-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.

    abstract：:Microtubules are recognized as crucial components of the mitotic spindle during cell division, and, for this reason, the microtubule system is an attractive target for the development of anticancer agents. Continuing our search strategy for novel tubulin targeting-compounds, a new series of 2-alkoxycarbonyl-3-(3',4',5...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.11.096

    authors： Romagnoli R,Kimatrai Salvador M,Schiaffino Ortega S,Baraldi PG,Oliva P,Baraldi S,Lopez-Cara LC,Brancale A,Ferla S,Hamel E,Balzarini J,Liekens S,Mattiuzzo E,Basso G,Viola G

    更新日期：2018-01-01 00:00:00

  • Simultaneous tritium labelling of two potent 5-HT4 ligands.

    abstract：:Two potent and selective 5-HT(4) ligands, [(3)H]-5-[(N-propylpiperidin-4-yl)methoxy]-1,2,3,4-tetrahydrobenzo[h][1,6] naphthyridine (1a) and [(3)H]-1-methyl-5-[(N-propylpiperidin-4-yl)methoxy]pyrrolo[1,2-a]thieno[2,3-e]pyrazine (2a) were radiolabelled with tritium. Radioactive labelling was achieved by simultaneous tri...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.12.012

    authors： Sobrio F,Lemaitre S,Hinsberger A,Barré L,Rousseau B,Rault S

    更新日期：2010-03-01 00:00:00

  • Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.

    abstract：:A possible ability of twelve new derivatives of known antioxidants trolox (TroH), trolox succinate (TroS), α-tocopheryl succinate (α-TOS) containing nitroxyl radicals (1-12) to protect bacterial cells from spontaneous and peroxide-induced mutagenesis and their cytotoxicity against six different tumor cells as well as ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.051

    authors： Zakharova OD,Frolova TS,Yushkova YV,Chernyak EI,Pokrovsky AG,Pokrovsky MA,Morozov SV,Sinitsina OI,Grigor'ev IA,Nevinsky GA

    更新日期：2016-10-21 00:00:00

  • Novel benzylidenephenylpyrrolizinones with pleiotropic activities potentially useful in Alzheimer's disease treatment.

    abstract：:This work describes the synthesis and the biological evaluation of novel benzylidenephenylpyrrolizinones as potential antioxidant, metal chelating or amyloid β (βA) aggregation inhibitors. Some derivatives exhibited interesting results in regard to several of the performed evaluations and appear as valuable Multi-Targ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.03.023

    authors： Jourdan JP,Since M,El Kihel L,Lecoutey C,Corvaisier S,Legay R,Sopkova-de Oliveira Santos J,Cresteil T,Malzert-Fréon A,Rochais C,Dallemagne P

    更新日期：2016-05-23 00:00:00

  • Synthesis and in vitro evaluation of novel spiroketopyrazoles as acetyl-CoA carboxylase inhibitors and potential antitumor agents.

    abstract：:Acetyl-CoA carboxylase (ACC) is a rate-limiting enzyme in de novo fatty acid synthesis, which plays a critical role in the growth and survival of cancer cells. In this study, a series of spiroketopyrazole derivatives bearing quinoline moieties were synthesized, and in vitro anticancer activities of these compounds as ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.113036

    authors： Huang T,Wu X,Yan S,Liu T,Yin X

    更新日期：2020-11-27 00:00:00

  • Synthesis and biological evaluation of novel ferrocene-naphthoquinones as antiplasmodial agents.

    abstract：:This work deals with the synthesis and evaluation of new compounds designed by combination of 1,4-naphthoquinone and ferrocene fragments in a 3-ferrocenylmethyl-2-hydroxy-1,4-naphthoquinone arrangement. A practical coupling reaction between 2-hydroxy-1,4-naphthoquinone and ferrocenemethanol derivatives has been develo...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.10.011

    authors： García-Barrantes PM,Lamoureux GV,Pérez AL,García-Sánchez RN,Martínez AR,San Feliciano A

    更新日期：2013-01-01 00:00:00

  • Affinity-based small fluorescent probe for NAD(P)H:quinone oxidoreductase 1 (NQO1). Design, synthesis and pharmacological evaluation.

    abstract：:NQO1 is a dimeric flavoprotein which intimately associated with cancer and overexpressed in the cytosol of numerous human tumor cells. Given that the cellular environment is quite dynamic and versatile, further investigation of the function of NQO1 depends on tools for specific detection of it. Currently, several acti...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.10.062

    authors： Bian J,Li X,Xu L,Wang N,Qian X,You Q,Zhang X

    更新日期：2017-02-15 00:00:00

  • Symmetry-based inhibitors of HIV-1 protease. Design, synthesis and preliminary structure-activity studies of acylated 2,3-diamino-1-hydroxypropanes and 2,4 diamino-1-hydroxybutanes.

    abstract：:Two series of peptidomimetics containing a novel C(2) pseudosymmetrical hydroxyalkyldiamino core structure were prepared from amino acid starting materials and tested for inhibitory activity against the HIV-1 protease (HIV-1 Pr) and the virus in cell culture. In the 2,3-diamino-1-hydroxypropane series, compound 6a, co...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)80034-3

    authors： Marastoni M,Bazzaro M,Bortolotti F,Salvadori S,Tomatis R

    更新日期：1999-07-01 00:00:00

  • The one-pot synthesis of butyl-1H-indol-3-alkylcarboxylic acid derivatives in ionic liquid as potent dual-acting agent for management of BPH.

    abstract：:Based on the SAR of both α1-AR antagonists and 5α-reductase (5AR) inhibitors, the dual-acting agent 4-(1-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-1H-indol-3-yl)butanoic acid 4aaa was designed against BPH and synthesized by two steps of N-alkylation. One-pot protocol towards 4aaa was newly developed. With IL [C6min...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112616

    authors： Zeng LY,Yang F,Chen K,Zeng Y,Jiang Z,Liu S,Xi B

    更新日期：2020-11-01 00:00:00

  • Synthesis and antimicrobial activities of a new series of 4-S-[4(1)-amino-5(1)-oxo-6(1)-substituted benzyl-4(1),5(1)-dihydro-1(1),2(1),4(1)-triazin-3-yl]mercaptoacetyl-3-arylsydnones.

    abstract：:The synthesis of some 4-S-(4(1)-amino-5(1)-oxo-6(1)-substituted benzyl-4(1),5(1)-dihydro-1(1),2(1),4(1)-triazin-3-yl)mercaptoacetyl-3-arylsydnones by the reaction of 3-aryl-4-bromoacetylsydnones with 6-substituted-4-amino-3-mercapto-1,2,4-triazin-5-ones is described. The IR, (1)H NMR, mass spectra and elemental analys...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.02.003

    authors： Hegde JC,Girisha KS,Adhikari A,Kalluraya B

    更新日期：2008-12-01 00:00:00

  • Bismuth heterocycles based on a diphenyl sulfone scaffold: synthesis and substituent effect on the antifungal activity against Saccharomyces cerevisiae.

    abstract：:A series of heterocyclic organobismuth(III) compounds 2 [ClBi(5-R-C6H(3)-2-SO2C6H(4)-1'-): R=Me, Ph, MeO, Cl, H, t-Bu, CF3, F, Me2N] was synthesized in order to study the relative importance of structure and specific substitutions in relation to their lipophilicity and antifungal activity against the yeast Saccharomyc...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.11.031

    authors： Murafuji T,Fujiwara Y,Yoshimatsu D,Miyakawa I,Migita K,Mikata Y

    更新日期：2011-02-01 00:00:00

  • Synthesis and evaluation of novel rutaecarpine derivatives and related alkaloids derivatives as selective acetylcholinesterase inhibitors.

    abstract：:A series of novel rutaecarpine derivatives and related alkaloid derivatives 3-aminoalkanamido-substituted rutaecarpine 4a-f and 7,8-dehydrorutaecarpine 5a-c, and 6-aminoalkanamido-substituted 3-[2-(3-Indolyl)ethyl]-4(3a)-quinazolinones 8a-c, were synthesized and subjected to pharmacological evaluation as acetylcholine...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.12.044

    authors： Wang B,Mai YC,Li Y,Hou JQ,Huang SL,Ou TM,Tan JH,An LK,Li D,Gu LQ,Huang ZS

    更新日期：2010-04-01 00:00:00

  • Progress of the synthesis of condensed pyrazole derivatives (from 2010 to mid-2013).

    abstract：:Condensed pyrazole derivatives are important heterocyclic compounds due to their excellent biological activities and have been widely applied in pharmaceutical and agromedical fields. In recent years, numerous condensed pyrazole derivatives have been synthesized and advanced to clinic studies with various biological a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2014.07.102

    authors： Li M,Zhao BX

    更新日期：2014-10-06 00:00:00

  • Structure-based virtual screening of novel inhibitors of the uridyltransferase activity of Xanthomonas oryzae pv. oryzae GlmU.

    abstract：:N-Acetylglucosamine-1-phosphate uridyltransferase (GlmU) catalyzes the formation of UDP-GlcNAc, a fundamental precursor in cell wall biosynthesis. GlmU represents an attractive target for new antibacterial agents. In this study, a theoretical three-dimensional (3D) structure of GlmU from Xanthomonas oryzae pv. oryzae ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.03.051

    authors： Min J,Lin D,Zhang Q,Zhang J,Yu Z

    更新日期：2012-07-01 00:00:00

  • Design, synthesis and bioevaluation of novel 6-(4-Hydroxypiperidino)naphthalen-2-ol-based potential Selective Estrogen Receptor Modulators for breast cancer.

    abstract：:In a study directed towards development of novel Selective Estrogen Receptor Modulators (SERMs), 1-(4-(2-(dialkylamino)ethoxy)benzyl)-6-(4-hydroxypiperidin-1-yl)-2-naphthol and corresponding aryl methyl ethers were synthesized and bioevaluated against the estrogen-responsive human MCF-7 breast cancer cell line. The ph...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.12.037

    authors： Jha A,Yadav Y,Naidu AB,Rao VK,Kumar A,Parmar VS,MacDonald WJ,Too CK,Balzarini J,Barden CJ,Cameron TS

    更新日期：2015-03-06 00:00:00