当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents.

Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents.

Abstract：

:By using fragment-based design strategies, a series of 2-thio-substituted anthra[1,2-d]imidazole-6,11-diones were synthesized and evaluated for hTERT repressing activities, cell proliferations, and NCI 60-cell panel assay. Compounds 2, 3, 4, 11, 15 and 35 were selected by the NCI and 3, 4, 11 and 15 represent the GI₅₀, TGI and LC₅₀, respectively. Among them, all were moderate selectivity toward leukemia cancer except for 4 exhibited distinctive selectivity of CNS and renal cancer with 7.403 and 6.475. The overall of test compounds exhibited different cytostatic and cytotoxic activities for further developing potential application as anticancer drugs.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Chen TC,Yu DS,Huang KF,Fu YC,Lee CC,Chen CL,Huang FC,Hsieh HH,Lin JJ,Huang HS

doi

10.1016/j.ejmech.2013.06.058

subject

Has Abstract

pub_date

2013-11-01 00:00:00

pages

278-93

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00488-1

journal_volume

69

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Optimization of troglitazone derivatives as potent anti-proliferative agents: towards more active and less toxic compounds.

    abstract：:Δ2-Troglitazone derivatives were shown to exhibit anti-proliferative activity in a PPARγ-independent manner. We prepared various compounds in order to increase their potency and decrease their toxicity towards non-malignant primary cultured hepatocytes. Many compounds induced viabilities less than 20% at 10 μM on vari...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.06.015

    authors： Bordessa A,Colin-Cassin C,Grillier-Vuissoz I,Kuntz S,Mazerbourg S,Husson G,Vo M,Flament S,Martin H,Chapleur Y,Boisbrun M

    更新日期：2014-08-18 00:00:00

  • 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 meth...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.10.018

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

    更新日期：2011-01-01 00:00:00

  • Synthesis and evaluation of some new benzimidazole derivatives as potential antimicrobial agents.

    abstract：:The efficient synthesis of novel azetidin-2-ones 6 has been established. Thus, condensation of 5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-1,3,4-thiadiazol-2-amine 4 with various aromatic aldehydes afforded 5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-N-[(substituted) phenylmethylidene]-1,3,4-thiadiazol-2-amine 5 which on ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.01.022

    authors： Ansari KF,Lal C

    更新日期：2009-05-01 00:00:00

  • Targeting gliomas with triazene-based hybrids: Structure-activity relationship, mechanistic study and stability.

    abstract：:Herein we report novel hybrid compounds based on valproic acid and DNA-alkylating triazene moieties, 1, with therapeutic potential for glioblastoma multiforme chemotherapy. We identified hybrid compounds 1d and 1e to be remarkably more potent against glioma and more efficient in decreasing invasive cell properties tha...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.03.048

    authors： Braga C,Vaz AR,Oliveira MC,Matilde Marques M,Moreira R,Brites D,Perry MJ

    更新日期：2019-06-15 00:00:00

  • Indoles as therapeutics of interest in medicinal chemistry: Bird's eye view.

    abstract：:Indoles constitute extensively explored heterocyclic ring systems with wide range of applications in pathophysiological conditions that is, cancer, microbial and viral infections, inflammation, depression, migraine, emesis, hypertension, etc. Presence of indole nucleus in amino acid tryptophan makes it prominent in ph...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.04.003

    authors： Chadha N,Silakari O

    更新日期：2017-07-07 00:00:00

  • Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine.

    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

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.06.010

    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

  • Dihydropyrimidinone/1,2,3-triazole hybrid molecules: Synthesis and anti-varicella-zoster virus (VZV) evaluation.

    abstract：:By combining the structural features of dihydropyrimidinone and 1,2,3-triazole heterocycles, novel hybrid compounds were synthesized using a simple and convenient method. A series of novel mono and bis 1,2,3-triazole was synthesized via copper-catalyzed Huisgen azide-alkyne cycloadditions (CuAAC) under microwave irrad...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.06.028

    authors： Kaoukabi H,Kabri Y,Curti C,Taourirte M,Rodriguez-Ubis JC,Snoeck R,Andrei G,Vanelle P,Lazrek HB

    更新日期：2018-07-15 00:00:00

  • Fructose-1,6-bisphosphatase inhibitors: A new valid approach for management of type 2 diabetes mellitus.

    abstract：:The rising incidence of diabetes and confines allied with clinical therapies emphasized the need to explore new molecular targets to develop novel, effective and safer antihyperglycemic agents. Excessive endogenous glucose production by gluconeogenesis is a primary determinant of hyperglycemia in patients with type 2 ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.09.029

    authors： Kaur R,Dahiya L,Kumar M

    更新日期：2017-12-01 00:00:00

  • Synthesis of new N3-substituted dihydropyrimidine derivatives as L-/T- type calcium channel blockers.

    abstract：:Cardiovascular diseases (CVDs) are the main cause of deaths worldwide. Up-to-date, hypertension is the most significant contributing factor to CVDs. Recent clinical studies recommend calcium channel blockers (CCBs) as effective treatment alone or in combination with other medications. Being the most clinically useful ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.03.080

    authors： Teleb M,Zhang FX,Farghaly AM,Aboul Wafa OM,Fronczek FR,Zamponi GW,Fahmy H

    更新日期：2017-07-07 00:00:00

  • 3D-QSAR analysis of human immunodeficiency virus entry-1 inhibitors by CoMFA and CoMSIA.

    abstract：:3D-QSAR studies namely CoMFA, CoMFA region focusing and CoMSIA have been carried out on a series (36 compounds) of HIV-1 entry inhibitors. An alignment rule for the compounds was defined using Distill in SYBYL 7.3. Models were validated using a data set obtained by dividing the data set into a training set and test se...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.07.062

    authors： Pirhadi S,Ghasemi JB

    更新日期：2010-11-01 00:00:00

  • Synthesis, evaluation and 3D QSAR analysis of novel estradiol-RGD octapeptide conjugates with oral anti-osteoporosis activity.

    abstract：:To enhance the potency, reduce the side effects and improve oral property of estradiol in estrogen replacement therapy (ERT), 6 novel estradiol-RGD octapeptide conjugates have been prepared. In an ovariectomized mouse osteoporotic model, at an oral dosage of 110.3 nmol/kg per day, their anti-osteoporosis activity was ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.09.036

    authors： Liu J,Zhang X,Zhao M,Peng S

    更新日期：2009-04-01 00:00:00

  • Anti-inflammatory hybrids of secondary amines and amide-sulfamide derivatives.

    abstract：:The CXCR4/CXCL12 chemokine axis can chemotactically accumulate inflammatory cells to local tissues and regulate the release of inflammatory factors. Developing novel CXCR4 modulators may provide a desirable strategy to control the development of inflammation. A series of novel hybrids were designed by integrating the ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.02.085

    authors： Bai R,Sun J,Liang Z,Yoon Y,Salgado E,Feng A,Oum Y,Xie Y,Shim H

    更新日期：2018-04-25 00:00:00

  • An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.

    abstract：:Estrogen-related receptor gamma (ERRγ) is the NR3B subgroup of associated transcription factors. In this report, a new generation of a potent and selective ERRγ inverse agonist (25) with good biocompatibility was proposed. We also explored the potential of the newly developed compound 25 in the PDTC model to expand th...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112501

    authors： Kim J,Hwang H,Yoon H,Lee JE,Oh JM,An H,Ji HD,Lee S,Cha E,Ma MJ,Kim DS,Lee SJ,Kadayat TM,Song J,Lee SW,Jeon JH,Park KG,Lee IK,Jeon YH,Chin J,Cho SJ

    更新日期：2020-11-01 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

  • A series of 1, 2-coupled indane dimers with mast cell stabilisation and smooth muscle relaxation properties.

    abstract：:Asthma is characterised by bronchoconstriction and inflammation, with infiltration and activation of inflammatory cells such as eosinophils and mast cells, and subsequent release of inflammatory mediators. Much of the therapy directed at the treatment of asthma is either to provide symptomatic relief through bronchodi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.09.005

    authors： Sheridan H,Walsh JJ,Jordan M,Cogan C,Frankish N

    更新日期：2009-12-01 00:00:00

  • Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.

    abstract：:A series of linezolid analogues containing a hydrazone moiety were designed, synthesized and evaluated for their antibacterial activity. Most compounds exhibited more potent antibacterial activity against S.aureus, MRSA, MSSA, LREF and VRE pathogens as compared with linezolid and radezolid. Compounds 9a, 9c, 9f, 9g, 1...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.09.004

    authors： Wu Y,Ding X,Ding L,Zhang Y,Cui L,Sun L,Li W,Wang D,Zhao Y

    更新日期：2018-10-05 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 biological evaluation of geniposide derivatives as potent and selective PTPlB inhibitors.

    abstract：:Herein a series of Geniposide derivatives were designed, synthesized and evaluated as protein tyrosine phosphatase 1B (PTPlB) inhibitors. Most of these compounds exhibited potent in vitro PTP1B inhibitory activities, the representative 7a and 17f were found to be the most potent inhibitors against the enzyme with IC50...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112508

    authors： Lei S,Zhang D,Qi Y,Chowdhury SR,Sun R,Wang J,Du Y,Fu L,Jiang F

    更新日期：2020-11-01 00:00:00

  • Identification of novel aminothiazole and aminothiadiazole conjugated cyanopyridines as selective CHK1 inhibitors.

    abstract：:Inhibitors of checkpoint kinase 1 (CHK1) are of current interest as potential anti-tumor agents. Novel series of cyanopyridyl-aminothiadiazoles (synthesized from reaction of 1-(3-cyano-4,6-diphenylpyridin-2-yl)-3-phenylthiourea (14) with hydrazonoyl halides) and cyanopyridyl-aminothiazolyl-thiadiazoles (synthesized fr...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,收录出版

    doi：10.1016/j.ejmech.2015.01.019

    authors： Gomha SM,Abdulla MM,Abou-Seri SM

    更新日期：2015-03-06 00:00:00

  • New naphthopyran analogues of LY290181 as potential tumor vascular-disrupting agents.

    abstract：:A series of 19 analogues of the antiproliferative naphthopyran LY290181 were prepared for structure-activity relationship studies. We found the best activities for test compounds bearing small substituents at the meta position of the phenyl ring. The mode of action of LY290181 and eight new analogues was studied in de...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.11.055

    authors： Schmitt F,Gold M,Rothemund M,Andronache I,Biersack B,Schobert R,Mueller T

    更新日期：2019-02-01 00:00:00

  • Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.

    abstract：:In recent years, drug discovery paradigm has been shifted from conventional single target inhibition toward multitarget design concept. In current research, we have reported synthesis, in-vitro, in-vivo and acute toxicity determination of N-substituted pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111863

    authors： Jan MS,Ahmad S,Hussain F,Ahmad A,Mahmood F,Rashid U,Abid OU,Ullah F,Ayaz M,Sadiq A

    更新日期：2020-01-15 00:00:00

  • Synthesis of polyfluoroalkyl sp2-iminosugar glycolipids and evaluation of their immunomodulatory properties towards anti-tumor, anti-leishmanial and anti-inflammatory therapies.

    abstract：:Immunomodulatory glycolipids, among which α-galactosylceramide (KRN7000) is an iconic example, have shown strong therapeutic potential in a variety of conditions ranging from cancer and infection to autoimmune or neurodegenerative diseases. A main difficulty for those channels is that they often provoke a cytokine sto...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111604

    authors： Sánchez-Fernández EM,García-Moreno MI,Arroba AI,Aguilar-Diosdado M,Padrón JM,García-Hernández R,Gamarro F,Fustero S,Sánchez-Aparicio JE,Masgrau L,García Fernández JM,Ortiz Mellet C

    更新日期：2019-11-15 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

  • A new class of β-carboline alkaloid-peptide conjugates with therapeutic efficacy in acute limb ischemia/reperfusion injury.

    abstract：:We describe a novel class of β-carboline alkaloid-peptide conjugates that possess both free radical scavenging and thrombolytic activity. These conjugates demonstrate therapeutic efficacy in a rat arterial thrombosis assay, as well as free radical scavenging capacity as evaluated in a PC12 cell survival assay. Our res...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.01.021

    authors： Bi W,Bi Y,Xue P,Zhang Y,Gao X,Wang Z,Li M,Baudy-Floc'h M,Ngerebara N,Gibson KM,Bi L

    更新日期：2011-05-01 00:00:00

  • Umbelliferone aminoalkyl derivatives, a new class of squalene-hopene cyclase inhibitors.

    abstract：:The synthesis is described of several aminoalkyl derivatives of coumarin, obtained in good yields under microwave or high-intensity ultrasound irradiation. These compounds proved uniformly active as inhibitors of squalene-hopene cyclase (SHC) from Alicyclobacillus acidocaldarius. Their design stemmed from our recent f...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2004.06.010

    authors： Cravotto G,Balliano G,Tagliapietra S,Palmisano G,Penoni A

    更新日期：2004-11-01 00:00:00

  • Bioactive thiazole and benzothiazole derivatives.

    abstract：:The heterocycles are the versatile compounds existing in almost all natural products and synthetic organic compounds, usually associated with one or the other biological activity. Among the heterocycles the thiazoles and benzothiazoles occupy a prominent position. They possess a broad range of biological activities an...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2014.10.058

    authors： Rouf A,Tanyeli C

    更新日期：2015-06-05 00:00:00

  • Synthesis and evaluation of antimicrobial activity of 4H-pyrimido[2,1-b]benzothiazole, pyrazole and benzylidene derivatives of curcumin.

    abstract：:A novel, one-pot, simple, efficient procedure for 4H-pyrimido[2,1-b]benzothiazole (4a-h), pyrazole (6a-d) and benzylidene (7a-d) derivatives of curcumin under solvent and solvent free conditions in microwave with good yield is have been synthesized. The synthesized compounds were evaluated for their antibacterial acti...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.05.020

    authors： Sahu PK,Sahu PK,Gupta SK,Thavaselvam D,Agarwal DD

    更新日期：2012-08-01 00:00:00

  • Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors.

    abstract：:We have developed a series of 6, 7-disubstituted-4-(arylamino) quinazoline derivatives that functioned as irreversible EGFR inhibitors, and these compounds exhibited excellent enzyme inhibition potency. As compared with afatinib, some of them showed significantly enhanced activities towards H1975 cells (EGFR-T790M). F...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.08.026

    authors： Zhang L,Yang Y,Zhou H,Zheng Q,Li Y,Zheng S,Zhao S,Chen D,Fan C

    更新日期：2015-09-18 00:00:00

  • Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.

    abstract：:Histone Deacetylases (HDACs) have become important targets for the treatment of cancer and other diseases. In previous studies we described the development of novel spirocyclic HDAC inhibitors based on the combination of privileged structures with hydroxamic acid moieties as zinc binding group. Herein, we report furth...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.03.061

    authors： Thaler F,Varasi M,Abate A,Carenzi G,Colombo A,Bigogno C,Boggio R,Zuffo RD,Rapetti D,Resconi A,Regalia N,Vultaggio S,Dondio G,Gagliardi S,Minucci S,Mercurio C

    更新日期：2013-06-01 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