当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents.

Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents.

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 Estrogen Receptor Modulators (SERMs) i.e. Ospemifene and Tamoxifen, against these cell lines. Compound 8 was relatively more cytotoxic to MCF-7 cells similar to Ospemifene and Tamoxifen, while most potent compounds 6 and 7 were equally effective in inhibiting growth of both ER-positive and ER-negative cell lines. The observed activity profiles were further supported by the docking studies performed against estrogen receptors (ERα and ERβ). Compounds 6, 7 and 8 exhibited stronger binding affinities with both ERα and ERβ compared to Ospemifene and Tamoxifen.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

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

doi

10.1016/j.ejmech.2014.08.050

subject

Has Abstract

pub_date

2014-10-30 00:00:00

pages

211-8

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00785-5

journal_volume

86

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.

    abstract：:In this preliminary study we report the antiviral screening of triazolo[4,5-g]quinoline derivatives (compounds 1-6). 4,9-Dihydrotriazolo[4,5-g]quinoline-1-oxide (1) stood out as a new, small molecule endowed with a selective, promising activity in cell-based assays against HIV-1wt and clinically relevant NNRTI resista...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.08.012

    authors： Carta A,Pricl S,Piras S,Fermeglia M,La Colla P,Loddo R

    更新日期：2009-12-01 00:00:00

  • Repurposed drug candidates for antituberculosis therapy.

    abstract：:Antibiotics have been a key part of clinical treatments for more than 70 years. Long-term use of antimicrobial treatments has led to the development of severe bacterial resistance, which has become increasingly serious due to antibiotic abuse, resulting in the treatment of bacterial infections becoming challenging. Th...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.112175

    authors： An Q,Li C,Chen Y,Deng Y,Yang T,Luo Y

    更新日期：2020-04-15 00:00:00

  • 5-Substituted [1]pyrindine derivatives with antiproliferative activity.

    abstract：:We report herein the synthesis of 5-substituted [1]pyrindine derivatives and the evaluation of their antiproliferative properties on HeLa cells, a cervical carcinoma tumor cell line, and on the melanoma A2058 cell line. The most efficient compounds display cytotoxicity against tumor cells in the micromolar range but h...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.11.028

    authors： Kolb S,Goddard ML,Loukaci A,Mondésert O,Ducommun B,Braud E,Garbay C

    更新日期：2010-03-01 00:00:00

  • X-ray crystal structures of Enterococcus faecalis thymidylate synthase with folate binding site inhibitors.

    abstract：:Infections caused by Enterococcus faecalis (Ef) represent nowadays a relevant health problem. We selected Thymidylate synthase (TS) from this organism as a potential specific target for antibacterial therapy. We have previously demonstrated that species-specific inhibition of the protein can be achieved despite the re...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.07.066

    authors： Catalano A,Luciani R,Carocci A,Cortesi D,Pozzi C,Borsari C,Ferrari S,Mangani S

    更新日期：2016-11-10 00:00:00

  • Medicinal plants used as anthelmintics: Ethnomedical, pharmacological, and phytochemical studies.

    abstract：:Intestinal parasites delay mental and physical development in children. Infection with these parasites can result in complications during pregnancy and alter the health of newborns, which has long-term effects on educational attainment and economic productivity. The appearance of resistance against classical drug trea...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.02.005

    authors： Romero-Benavides JC,Ruano AL,Silva-Rivas R,Castillo-Veintimilla P,Vivanco-Jaramillo S,Bailon-Moscoso N

    更新日期：2017-03-31 00:00:00

  • Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.

    abstract：:Drug therapy for Chagas disease remains a major challenge as potential candidate drugs have failed clinical trials. Currently available drugs have limited efficacy and induce serious side effects. Thus, the discovery of new drugs is urgently needed in the fight against Chagas' disease. Here, we synthesized and evaluat...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111610

    authors： Monteiro ME,Lechuga G,Lara LS,Souto BA,Viganó MG,Bourguignon SC,Calvet CM,Oliveira FOR Jr,Alves CR,Souza-Silva F,Santos MS,Pereira MCS

    更新日期：2019-11-15 00:00:00

  • New 5-substituted thiazolo[3,2-b][1,2,4]triazol-6-ones: synthesis and anticancer evaluation.

    abstract：:Following [2+3]-cyclocondensation reaction of 1,2,4-triazole-3(5)-thiol with N-arylmaleimides or with monochloroacetic acid and oxocompounds, N-(R-phenyl)-(6-oxo-5,6-dihydro[1,3]thiazol[3,2-b][1,2,4]triazol-5-yl)acetamides (1-5) and 5-ylidene-[1,3]thiazolo[3,2-b][1,2,4]triazol-6-ones (6-11) were synthesized as possibl...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.12.006

    authors： Lesyk R,Vladzimirska O,Holota S,Zaprutko L,Gzella A

    更新日期：2007-05-01 00:00:00

  • New diarylamides and diarylureas possessing 8-amino(acetamido)quinoline scaffold: synthesis, antiproliferative activities against melanoma cell lines, kinase inhibition, and in silico studies.

    abstract：:Synthesis of a new series of diarylureas and diarylamides possessing 4-aryl-8-amino(acetamido)quinoline scaffold is described. Their in vitro antiproliferative activities against ten melanoma cell lines were tested. Compounds 1l, 2l, 3c, and 4c showed the highest potency against A375P cell line with IC50 values in sub...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.06.060

    authors： Koh EJ,El-Gamal MI,Oh CH,Lee SH,Sim T,Kim G,Choi HS,Hong JH,Lee SG,Yoo KH

    更新日期：2013-01-01 00:00:00

  • Designing dendrimers for ocular drug delivery.

    abstract：:New series of phosphorus-containing dendrimers, having one quaternary ammonium salt as core and carboxylic acid terminal groups have been synthesized from generation 0 (3 carboxylic acid terminal groups) to generation 2 (12 carboxylic acid terminal groups). These dendrimers react with the neutral form of carteolol (an...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.10.017

    authors： Spataro G,Malecaze F,Turrin CO,Soler V,Duhayon C,Elena PP,Majoral JP,Caminade AM

    更新日期：2010-01-01 00:00:00

  • Synthesis and biological activity of novel mycophenolic acid conjugates containing nitro-acridine/acridone derivatives.

    abstract：:Hybrid pharmacophore anti-proliferative compounds, comprised of mycophenolic acid (MPA) and 1-nitroacridine/4-nitroacridone derivative have been synthesized and evaluated as inhibitors of five different leukemia cell lines (Jurkat, Molt-4, HL-60, CCRF-CEM, L1210) and human peripheral blood mononuclear cells from healt...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.04.040

    authors： Malachowska-Ugarte M,Cholewinski G,Dzierzbicka K,Trzonkowski P

    更新日期：2012-08-01 00:00:00

  • Regioselective chemical and rapid enzymatic synthesis of a novel redox – Antiproliferative molecular hybrid.

    abstract：:Recent science evidenced the interlinkage of oxidative stress and cancer. Due to the inherent complexity of cancer and its accompanying effect of oxidative stress, novel molecules, containing combinatorial functionalities should be targeted. Herein, we synthesized gemcitabine-5'-O-lipoate derived from a regioselective...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.03.064

    authors： Geromichalou E,Sayyad N,Kyriakou E,Chatzikonstantinou AV,Giannopoulou E,Vrbjar N,Kalofonos HP,Stamatis H,Tzakos AG

    更新日期：2015-01-01 00:00:00

  • Antidyslipidemic and antioxidative activities of 8-hydroxyquinoline derived novel keto-enamine Schiffs bases.

    abstract：:8-Hydroxyquinoline when subjected to Duff reaction resulted in the formation of unexpected 7-methylaminomethylene-8-oxo-7, 8-dihydroquinoline-5-carbaldehyde 2, which existed in the keto-enamine form, in which the aromaticity of the relevant ring was disrupted, which upon subsequent treatment with various primary amine...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.08.004

    authors： Sashidhara KV,Kumar A,Bhatia G,Khan MM,Khanna AK,Saxena JK

    更新日期：2009-04-01 00:00:00

  • The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119.

    abstract：:A series of xanthine compounds derived from the previous hit 20i with modification on the terminal side chain was discovered through ring formation strategy. Systematic optimization of the compounds with rigid heterocycles in the hydrophobic side chain led to the new lead compound HBK001 (21h) with the improved DPP-IV...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.112017

    authors： Li G,Meng B,Yuan B,Huan Y,Zhou T,Jiang Q,Lei L,Sheng L,Wang W,Gong N,Lu Y,Ma C,Li Y,Shen Z,Huang H

    更新日期：2020-02-15 00:00:00

  • Structure-based virtual screening for identification of novel 11beta-HSD1 inhibitors.

    abstract：:Structure-based pharmacophore models were built by using LigandScout and used for virtual screening of the SPECS database to identify new potential 11beta-HSD1 inhibitors. As a refinement of the results obtained from virtual 3D pharmacophore screening, the best fitting virtual hits were subjected to docking study. The...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.06.005

    authors： Yang H,Shen Y,Chen J,Jiang Q,Leng Y,Shen J

    更新日期：2009-03-01 00:00:00

  • Synthesis of stilbene derivatives with inhibition of SARS coronavirus replication.

    abstract：:Stilbene derivatives have wide range of activities. In an effort to find other potential activities of this kind of compounds, 17 derivatives, including resveratrol, were synthesized. Twelve of them were evaluated for their antiviral potential against severe acute respiratory syndrome (SARS)-CoV-induced cytopathicity ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.03.024

    authors： Li YQ,Li ZL,Zhao WJ,Wen RX,Meng QW,Zeng Y

    更新日期：2006-09-01 00:00:00

  • Classification of estrogen receptor-beta ligands on the basis of their binding affinities using support vector machine and linear discriminant analysis.

    abstract：:Classification models of estrogen receptor-beta ligands were proposed using linear and nonlinear models. The data set was divided into active and inactive classes on the basis of their binding affinities. The two-class problem (active, inactive) was firstly explored by linear classifier approach, linear discriminant a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.03.002

    authors： Luan F,Liu HT,Ma WP,Fan BT

    更新日期：2008-01-01 00:00:00

  • QSAR study on tetrahydroquinoline analogues as plasmodium protein farnesyltransferase inhibitors: a comparison of rationales of malarial and mammalian enzyme inhibitory activities for selectivity.

    abstract：:The quantitative structure-activity relationships of Plasmodium falciparum and Rat protein farnesyltransferase (PFT) inhibitory activities of 6-cyano-1-(3-methyl-3H-imidazoly-4-ylmethyl)-3-substituted-1,2,3,4-tetrahydroquinoline (THQ) analogues are investigated in order to explore the similarities/deviations between t...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.01.025

    authors： Gupta MK,Prabhakar YS

    更新日期：2008-12-01 00:00:00

  • Novel inhibitors of nitric oxide synthase with antioxidant properties.

    abstract：:We previously described a series of imidazole-based inhibitors substituted at N-1 with an arylethanone chain as interesting inhibitors of neuronal nitric oxide synthase (nNOS), endowed with good selectivity vs endothelial nitric oxide synthase (eNOS). As a follow up of these studies, several analogs characterized by t...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.01.002

    authors： Salerno L,Modica MN,Romeo G,Pittalà V,Siracusa MA,Amato ME,Acquaviva R,Di Giacomo C,Sorrenti V

    更新日期：2012-03-01 00:00:00

  • Doing the methylene shuffle--further insights into the inhibition of mitotic kinesin Eg5 with S-trityl L-cysteine.

    abstract：:S-Trityl L-cysteine (STLC) is an inhibitor of the mitotic kinesin Eg5 with potential as an antimitotic chemotherapeutic agent. We previously reported the crystal structure of the ligand-protein complex, and now for the first time, have quantified the interactions using a molecular dynamics based approach. Based on the...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.05.034

    authors： Abualhasan MN,Good JA,Wittayanarakul K,Anthony NG,Berretta G,Rath O,Kozielski F,Sutcliffe OB,Mackay SP

    更新日期：2012-08-01 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

  • Cyclopentadienyl ruthenium(II) carbosilane metallodendrimers as a promising treatment against advanced prostate cancer.

    abstract：:In searching for efficient and selective antitumour drugs, a new family of carbosilane metallodendrimers functionalized with [Ru(η5-C5H5)(PTA)Cl] (PTA = 1,3,5-triaza-7-phosphatricyclo-[3.3.1.1] decane) is reported. Experiments of the biophysical characterization showed an ability to interact with biological membranes,...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112414

    authors： Sanz Del Olmo N,Bajo AM,Ionov M,García-Gallego S,Bryszewska M,Gómez R,Ortega P,de la Mata FJ

    更新日期：2020-08-01 00:00:00

  • Is it possible docking and scoring new ligands with few experimental data? Preliminary results on estrogen receptor as a case study.

    abstract：:Estrogens are steroid hormones playing critical roles in several physiological processes, which bind the estrogen receptors ERalpha and ERbeta. Aim of this work is to analyze, by different docking experiments, the behavior of a set of compounds, mimicking estrogens activity, in order to understand the relationship bet...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2004.02.014

    authors： Cozzini P,Dottorini T

    更新日期：2004-07-01 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

  • Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.

    abstract：:Xanthine oxidase (XO), a versatile metalloflavoprotein enzyme, catalyzes the oxidative hydroxylation of hypoxanthine and xanthine to uric acid in purine catabolism while simultaneously producing reactive oxygen species. Both lead to the gout-causing hyperuricemia and oxidative damage of the tissues where overactivity ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.04.031

    authors： Šmelcerović A,Tomović K,Šmelcerović Ž,Petronijević Ž,Kocić G,Tomašič T,Jakopin Ž,Anderluh M

    更新日期：2017-07-28 00:00:00

  • Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives.

    abstract：:As a continuation of our research and with the aim of obtaining new anti-tuberculosis agents which can improve the current chemotherapeutic anti-tuberculosis treatments, forty-three new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives were synthesized and evaluated for in vitro anti-tuberculosis activity against M...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.06.036

    authors： Moreno E,Ancizu S,Pérez-Silanes S,Torres E,Aldana I,Monge A

    更新日期：2010-10-01 00:00:00

  • Design, synthesis and biological evaluation of novel 2-methoxyestradiol analogs as dual selective estrogen receptor modulators (SERMs) and antiangiogenic agents.

    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

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.08.016

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

    更新日期：2017-10-20 00:00:00

  • Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line.

    abstract：:Some triazinone derivatives are designed and synthesized as potential antitumor agents. Triazinone derivatives 4c, 5e and 7c show potent anticancer activity over MCF-7 breast cancer cells higher than podophyllotoxin (podo) by approximate 6-fold. DNA flow cytometry analysis for the compounds 3c, 4c, 5e, 6c and 7c show ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.07.003

    authors： Zaki I,Abdelhameid MK,El-Deen IM,Abdel Wahab AHA,Ashmawy AM,Mohamed KO

    更新日期：2018-08-05 00:00:00

  • Synthesis and biological evaluation of (1-aryl-1H-pyrazol-4-yl) (3,4,5-trimethoxyphenyl)methanone derivatives as tubulin inhibitors.

    abstract：:A series of (1-aryl-1H-pyrazol-4-yl) (3,4,5-trimethoxyphenyl)methanones (8a-p, 9a-p) and ketoxime (10c) derivatives were designed and synthesized as antitubulin agents. All of the target compounds were evaluated for the in vitro anti-proliferative activities against three tumor cell lines (A549, HT-1080, SGC-7901). Th...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.05.058

    authors： Zhai M,Wang L,Liu S,Wang L,Yan P,Wang J,Zhang J,Guo H,Guan Q,Bao K,Wu Y,Zhang W

    更新日期：2018-08-05 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

  • Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.

    abstract：:PI3K/Akt/mTOR signaling pathway plays an important role in cancer cell growth and survival. In this study, a new class of molecules with skeleton of 4-phenyl-2H-benzo[b] [1,4]oxazin-3(4H)-one were designed and synthesized targeting this pathway. Bioassays showed that, among all the molecules, 8d-1 was a pan-class I PI...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.06.021

    authors： Yan G,Pu C,Lan S,Zhong X,Zhou M,Hou X,Yang J,Shan H,Zhao L,Li R

    更新日期：2019-09-15 00:00:00