当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Benzofuran derivatives as anticancer inhibitors of mTOR signaling.

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, suggesting insensitivity to the resistance associated to Akt overactivation observed with rapamycin derivatives currently used in clinic.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

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

doi

10.1016/j.ejmech.2014.05.014

subject

Has Abstract

pub_date

2014-06-23 00:00:00

pages

181-91

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00428-0

journal_volume

81

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Synthesis, characterization and anticancer screening of some novel piperonyl-tetrazole derivatives.

    abstract：:A series of new 1,2-substituted tetrazole derivatives were synthesized and evaluated on MCF-7 (ER positive), MDA-MB-231 and ZR-75 (ER negative) breast cancer cell lines. Out of the fourteen compounds, three compounds 10, 12 and 14 showed higher inhibitory effects on MCF-7 cells. Whereas, compound 8 exhibited higher in...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.11.008

    authors： Arshad M,Bhat AR,Pokharel S,Kim JE,Lee EJ,Athar F,Choi I

    更新日期：2014-01-01 00:00:00

  • Recent insights into synthetic β-carbolines with anti-cancer activities.

    abstract：:Cancer, an uncontrolled and rapid proliferation of abnormal cells, has become one of the leading cause of death worldwide. The development of resistance among the numerous drugs in clinical use has provided strong impetus for the identification and development of novel cancer therapeutics. β-carbolines constitute an i...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.05.059

    authors： Kumar S,Singh A,Kumar K,Kumar V

    更新日期：2017-12-15 00:00:00

  • Synthesis and biological evaluation of novel aniline-derived asiatic acid derivatives as potential anticancer agents.

    abstract：:Asiatic acid (AA) derivatives 4 and 5 modified at the C-11 and C-28 positions were designed and synthesized, their structures were confirmed using HRMS, (1)H NMR and (13)C NMR. In vitro antitumor activities of all compounds against MGC-803, NCI-H460, HepG2, Hela and 7404 cancer cell lines were evaluated and compared w...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.08.003

    authors： Li JF,Huang RZ,Yao GY,Ye MY,Wang HS,Pan YM,Xiao JT

    更新日期：2014-10-30 00:00:00

  • Synthesis of 1-[3-(4-benzotriazol-1/2-yl-3-fluoro-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-3-substituted-thiourea derivatives as antituberculosis agents.

    abstract：:In continuation of our research program for new antituberculosis drugs, we have designed, synthesized and evaluated antimycobacterial activity of new series of 1-[3-(4-benzotriazol-1/2-yl-3-fluoro-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-3-substituted-thiourea derivatives against different Mycobacterium species i.e. M. tu...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.12.005

    authors： Dixit PP,Patil VJ,Nair PS,Jain S,Sinha N,Arora SK

    更新日期：2006-03-01 00:00:00

  • Synthesis, in vitro β-glucuronidase inhibitory potential and molecular docking studies of quinolines.

    abstract：:In this study synthesis and β-glucuronidase inhibitory potential of 3/5/8 sulfonamide and 8-sulfonate derivatives of quinoline (1-40) are discussed. Studies reveal that all the synthetic compounds were found to have good inhibitory activity against β-glucuronidase. Nonetheless, compounds 1, 2, 5, 13, and 22-24 having ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.08.052

    authors： Bano B,Arshia,Khan KM,Kanwal,Fatima B,Taha M,Ismail NH,Wadood A,Ghufran M,Perveen S

    更新日期：2017-10-20 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

  • Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors.

    abstract：:The c-Met kinase has emerged as an attractive target for developing antitumor agents because of its close relationship with the development of many human cancers, poor clinical outcomes and even drug resistance. A series of novel c-Met kinase inhibitors have been identified with multiple workflow in this work, includi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.11.073

    authors： Yuan H,Liu Q,Zhang L,Hu S,Chen T,Li H,Chen Y,Xu Y,Lu T

    更新日期：2018-01-01 00:00:00

  • Synthesis and anticancer evaluation of some new hydrazone derivatives of 2,6-dimethylimidazo[2,1-b][1,3,4]thiadiazole-5-carbohydrazide.

    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

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(03)00138-7

    authors： Terzioglu N,Gürsoy A

    更新日期：2003-07-01 00:00:00

  • Structure-activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme.

    abstract：:Insulin degrading enzyme (IDE) is a zinc metalloprotease that degrades small amyloid peptides such as amyloid-â and insulin. So far the dearth of IDE-specific pharmacological inhibitors impacts the understanding of its role in the physiopathology of Alzheimer's disease, amyloid-â clearance, and its validation as a pot...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.12.005

    authors： Charton J,Gauriot M,Totobenazara J,Hennuyer N,Dumont J,Bosc D,Marechal X,Elbakali J,Herledan A,Wen X,Ronco C,Gras-Masse H,Heninot A,Pottiez V,Landry V,Staels B,Liang WG,Leroux F,Tang WJ,Deprez B,Deprez-Poulain R

    更新日期：2015-01-27 00:00:00

  • Tetrazole hybrids and their antifungal activities.

    abstract：:Fungi, which can cause serious infections, results in more than 1.35 million deaths annually throughout the world. Azole antifungal drugs which could inhibit the enzyme lanosterol 14α-demethylase, occupy an important position in the treatment of fungal infections. Tetrazoles, practically non-metabolized bioisosteric a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2019.03.023

    authors： Wang SQ,Wang YF,Xu Z

    更新日期：2019-05-15 00:00:00

  • Novel antiacanthamoebic compounds belonging to quinazolinones.

    abstract：:We report one-pot synthesis of a series of new 3-aryl-8-methylquinazolin-4(3H)-ones (QNZ) and their antimicrobial activity against Acanthamoeba castellanii belonging to T4 genotype. A library of fifteen synthetic derivatives of QNZs was synthesized, and their structural elucidation was performed by using nuclear magne...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111575

    authors： Anwar A,Shahbaz MS,Saad SM,Kanwal,Khan KM,Siddiqui R,Khan NA

    更新日期：2019-11-15 00:00:00

  • Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents.

    abstract：:A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure-activity relationships (SARs). Most of the synthesized compounds possessed potent anti-HBV activity, of whi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.11.019

    authors： Guo RH,Zhang Q,Ma YB,Luo J,Geng CA,Wang LJ,Zhang XM,Zhou J,Jiang ZY,Chen JJ

    更新日期：2011-01-01 00:00:00

  • 5,10b-Ethanophenanthridine amaryllidaceae alkaloids inspire the discovery of novel bicyclic ring systems with activity against drug resistant cancer cells.

    abstract：:Plants of the Amaryllidaceae family produce a large variety of alkaloids and non-basic secondary metabolites, many of which are investigated for their promising anticancer activities. Of these, crinine-type alkaloids based on the 5,10b-ethanophenanthridine ring system were recently shown to be effective at inhibiting ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.004

    authors： Henry S,Kidner R,Reisenauer MR,Magedov IV,Kiss R,Mathieu V,Lefranc F,Dasari R,Evidente A,Yu X,Ma X,Pertsemlidis A,Cencic R,Pelletier J,Cavazos DA,Brenner AJ,Aksenov AV,Rogelj S,Kornienko A,Frolova LV

    更新日期：2016-09-14 00:00:00

  • Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues.

    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

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.046

    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

  • Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.

    abstract：:In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4'-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new deriv...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.11.010

    authors： Thaler F,Moretti L,Amici R,Abate A,Colombo A,Carenzi G,Fulco MC,Boggio R,Dondio G,Gagliardi S,Minucci S,Sartori L,Varasi M,Mercurio C

    更新日期：2016-01-27 00:00:00

  • Activation of anti-oxidant Nrf2 signaling by enone analogues of curcumin.

    abstract：:Inflammation and oxidative stress are common in many chronic diseases. Targeting signaling pathways that contribute to these conditions may have therapeutic potential. The transcription factor Nrf2 is a major regulator of phase II detoxification and anti-oxidant genes as well as anti-inflammatory and neuroprotective g...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.11.048

    authors： Deck LM,Hunsaker LA,Vander Jagt TA,Whalen LJ,Royer RE,Vander Jagt DL

    更新日期：2018-01-01 00:00:00

  • Polypharmacological drug actions of recently FDA approved antibiotics.

    abstract：:The current epidemic of antibiotic resistant bacterial infections has fueled the demand for novel antibiotics exhibiting both antibacterial efficacy and anti-drug resistance. This need has not been fully satisfied by the conventional "one target-one molecule" approach. Consequently, there has been rising interest in t...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.112931

    authors： Wetzel C,Lonneman M,Wu C

    更新日期：2021-01-01 00:00:00

  • Highly potent non-steroidal FXR agonists protostane-type triterpenoids: Structure-activity relationship and mechanism.

    abstract：:Farnesoid X receptor (FXR) is a key regulator in charge of bile acid synthesis, transport, and metabolism. Activation of FXR represses bile acid synthesis and increases its excretion and transport, consequently protecting the liver functions. Thus, FXR is considered as a critical therapeutic target of cholestasis and ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111652

    authors： Luan ZL,Huo XK,Dong PP,Tian XG,Sun CP,Lv X,Feng L,Ning J,Wang C,Zhang BJ,Ma XC

    更新日期：2019-11-15 00:00:00

  • Design and synthesis of some new pyrazolyl-pyrazolines as potential anti-inflammatory, analgesic and antibacterial agents.

    abstract：:In the present study, an efficient synthesis of some new substituted pyrazoline derivatives linked to a substituted pyrazole scaffold was performed by a multistep reaction sequences and compounds were screened for their anti-inflammatory, analgesic and antibacterial activities. The preliminary results revealed that th...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.07.002

    authors： Viveka S,Dinesha,Shama P,Nagaraja GK,Ballav S,Kerkar S

    更新日期：2015-08-28 00:00:00

  • In situ and in silico evaluation of amine- and folate-terminated dendrimers as nanocarriers of anesthetics.

    abstract：:The search for new nano-systems for targeted biomedical applications and controlled drug release has attracted significant attention in polymer chemistry, pharmaceutics, and biomaterial science. Controlled drug delivery has many advantages over conventional drug administration, such as reduction of side effects, maint...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.11.040

    authors： Carrasco-Sánchez V,Vergara-Jaque A,Zuñiga M,Comer J,John A,Nachtigall FM,Valdes O,Duran-Lara EF,Sandoval C,Santos LS

    更新日期：2014-02-12 00:00:00

  • Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2.

    abstract：:The antimalarial acitivity of hydroxyethylamines, synthesized from the reaction of intermediated hydroxyethypiperazines with benzenesulfonyl chlorides or benzoyl chlorides, has been evaluated in vitro against a W2 Plasmodium falciparum clone. Some of the nineteen tested derivatives showed a significant activity in vit...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.03.041

    authors： Cunico W,Gomes CR,Facchinetti V,Moreth M,Penido C,Henriques MG,Varotti FP,Krettli LG,Krettli AU,da Silva FS,Caffarena ER,de Magalhães CS

    更新日期：2009-09-01 00:00:00

  • Vocational training for medicinal chemists: views from industry.

    abstract：:The Medicinal Chemistry Section of IUPAC sent a questionnaire regarding academic training for medicinal chemists to major research pharmaceutical companies in various countries in July 1992 and again in July 1993. A total of 102 replies were received from 65 companies, mainly from Germany, Italy, Japan, the UK and the...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/0223-5234(96)83968-7

    authors： Busse W,Ganellin C,Mitscher L

    更新日期：1996-01-01 00:00:00

  • Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent.

    abstract：:A series of 4-pyridylpiperazine derivatives with varying regulatory region substituents proved to be potent histamine H3 receptor (H3R) ligands in the nanomolar concentration range. The most influential modification that affected the affinity toward the H3R appeared by introducing electron-withdrawing moieties into th...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.113041

    authors： Szczepańska K,Pockes S,Podlewska S,Höring C,Mika K,Latacz G,Bednarski M,Siwek A,Karcz T,Nagl M,Bresinsky M,Mönnich D,Seibel U,Kuder KJ,Kotańska M,Stark H,Elz S,Kieć-Kononowicz K

    更新日期：2020-11-24 00:00:00

  • Site-directed mutagenesis provides insights into the selective binding of trityl derivatives to Plasmodium falciparum dUTPase.

    abstract：:We have previously identified a series of triphenylmethane derivatives of deoxyuridine with antimalarial activity in vitro which selectively inhibit Plasmodium falciparum deoxyuridine triphosphate nucleotidohydrolase (PfdUTPase) compared to the human enzyme. The crystal structure of PfdUTPase in complex with one of th...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.04.052

    authors： Recio E,Musso-Buendía A,Vidal AE,Ruda GF,Kasinathan G,Nguyen C,Ruiz-Pérez LM,Gilbert IH,González-Pacanowska D

    更新日期：2011-08-01 00:00:00

  • Syntheses of tetrahydroisoquinoline derivatives that inhibit NO production in activated BV-2 microglial cells.

    abstract：:Seventeen tetrahydroisoquinoline derivatives were designed, synthesized and evaluated for inhibition of NO production in lipopolysaccharide-stimulated BV-2 microglial cells. Compounds 5a, 9c and 11a potently attenuated NO production by >60%, and 5a and 11a inhibited BH4 production by >48% at 100 microM. In particular,...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.09.009

    authors： Seo JW,Srisook E,Son HJ,Hwang O,Cha YN,Chi DY

    更新日期：2008-06-01 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

  • Design, synthesis and biological evaluation of new quinoline derivatives as potential antitumor agents.

    abstract：:A series of new quinoline derivatives was designed, synthesized and evaluated for their antiproliferative activity. The results demonstrated that compounds 11p, 11s, 11v, 11x and 11y exhibited potent antiproliferative activity with IC50 value of lower than 10 μM against seven human tumor cell lines, and N-(3-methoxyph...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.05.088

    authors： Su T,Zhu J,Sun R,Zhang H,Huang Q,Zhang X,Du R,Qiu L,Cao R

    更新日期：2019-09-15 00:00:00

  • Synthesis, anticancer activity and QSAR study of 1,4-naphthoquinone derivatives.

    abstract：:A series of 2-substituted amino-3-chloro-1,4-naphthoquinone derivatives (3-12) were synthesized as anticancer agents and tested against four cancer cell lines including HepG2, HuCCA-1, A549 and MOLT-3. The most potent cytotoxic activity against the HepG2, HuCCA-1 and A549 cell lines was found to be m-acetylphenylamino...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.07.024

    authors： Prachayasittikul V,Pingaew R,Worachartcheewan A,Nantasenamat C,Prachayasittikul S,Ruchirawat S,Prachayasittikul V

    更新日期：2014-09-12 00:00:00

  • Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia.

    abstract：:Fms-like tyrosine kinase 3 (FLT3) is a well-known and important target for the treatment of acute myeloid leukemia (AML). A series of thieno[2,3-d]pyrimidine derivatives from a modification at the 6-position were synthesized to identify effective FLT3 inhibitors. Although compounds 1 and 2 emerged as promising FLT3 in...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.022

    authors： Kim H,Lee C,Yang JS,Choi S,Park CH,Kang JS,Oh SJ,Yun J,Kim MH,Han G

    更新日期：2016-09-14 00:00:00

  • QSAR study of 4-phenylpiperidine derivatives as mu opioid agonists by neural network method.

    abstract：:A nonlinear QSAR study was conducted on a series of 4-phenylpiperidine derivatives (4PPs) acting as mu opioid agonists by three-layer back-propagation neural network (NN) method. At first a variety of molecular descriptors were calculated and then selected with two-stage least squares combining partial least squares (...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.10.017

    authors： Wang XH,Tang Y,Xie Q,Qiu ZB

    更新日期：2006-02-01 00:00:00