In vitro PAI-1 inhibitory activity of oxalamide derivatives.

abstract：:Glycogen synthase kinase 3β (GSK-3β) is widely recognised as a relevant player in the pathogenesis of several highly prevalent disorders such as Alzheimer's disease, mood disorders, diabetes and cancer. Therefore, this enzyme constitutes a highly attractive therapeutic target for the development of selective inhibitor...

journal_title：European journal of medicinal chemistry

authors： Bidon-Chanal A,Fuertes A,Alonso D,Pérez DI,Martínez A,Luque FJ,Medina M

更新日期：2013-02-01 00:00:00

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

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

abstract：:A series of aminopropylindenes, designed as mimics of a cationic high energy intermediate in the oxidosqualene cyclase(1) (OSC)-mediated cyclization of 2,3-oxidosqualen to lanosterol was prepared from Grundmann's ketone. Screening on OSCs from five different organisms revealed interesting activities and selectivities ...

journal_title：European journal of medicinal chemistry

authors： Lange S,Keller M,Müller C,Oliaro-Bosso S,Balliano G,Bracher F

更新日期：2013-05-01 00:00:00

abstract：:InhA, the enoyl acyl carrier protein reductase of Mycobacterium tuberculosis (MTB) is an attractive target for developing novel anti-tubercular agents. Twenty eight 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives were synthesized and evaluated for their in vitro MTB InhA inhibition. Compounds were further evaluated ...

journal_title：European journal of medicinal chemistry

authors： Pedgaonkar GS,Sridevi JP,Jeankumar VU,Saxena S,Devi PB,Renuka J,Yogeeswari P,Sriram D

更新日期：2014-10-30 00:00:00

abstract：:(S)-Blebbistatin is a widely used research tool to study myosin II, an important regulator of many motility based diseases. Its potency is too low to be of clinical relevance, but identification of analogs with enhanced potency could deliver leads for targeted pharmacotherapeutics. This, however, requires a profound i...

journal_title：European journal of medicinal chemistry

authors： Verhasselt S,Roman BI,Bracke ME,Stevens CV

更新日期：2017-08-18 00:00:00

abstract：:Six new type binuclear platinum(II) complexes (a-f) have been synthesized and characterized by elemental analysis, conductivity, thermal analysis, IR, UV, (1)H NMR and mass spectra techniques. The cytotoxicity of the complexes was tested by MTT and SRB assays. The cell cycle analysis and the levels of total platinum b...

journal_title：European journal of medicinal chemistry

authors： Zhang J,Li Y,Sun J,Li W,Gong Y,Zheng X,Cui J,Wang R,Wu J

更新日期：2009-11-01 00:00:00

abstract：:The binding of lead compounds and drugs to human serum albumin (HSA) is a ubiquitous problem in drug discovery since it modulates the availability of the leads and drugs to their intended target, which is linked to biological efficacy. In our continuing efforts to identify small molecule alpha(V)beta(3) and alpha(V)be...

journal_title：European journal of medicinal chemistry

authors： Raboisson P,Manthey CL,Chaikin M,Lattanze J,Crysler C,Leonard K,Pan W,Tomczuk BE,Marugán JJ

更新日期：2006-07-01 00:00:00

abstract：:Molecular hybridization is a ligand based drug design approach is well known recent medicinal chemistry to design anti-parasitic agents. In the present study, we have designed a series of (1-phenyl-9H-pyrido [3,4-b]indol-3-yl) (4-phenylpiperazin-1-yl)methanone derivatives using molecular hybridization approach. Design...

journal_title：European journal of medicinal chemistry

authors： Ashok P,Chander S,Smith TK,Sankaranarayanan M

更新日期：2018-04-25 00:00:00

abstract：:A novel series of the biheterocycles-based compounds with core structure distinguished from combretastatin A-4 (1) and colchicine (5) have been synthesized and evaluated as potent anti-mitotic agents. Compound 1-(4'-Indolyl and 6'-quinolinyl)-4,5,6-trimethoxyindoles 13 and 19 showed substantial anti-proliferative acti...

journal_title：European journal of medicinal chemistry

authors： Lai MJ,Chang JY,Lee HY,Kuo CC,Lin MH,Hsieh HP,Chang CY,Wu JS,Wu SY,Shey KS,Liou JP

更新日期：2011-09-01 00:00:00

abstract：:Thirty-five 3-aryl-4-arylaminofuran-2(5H)-one derivatives were designed, prepared and tested for their inhibitory activity against tyrosyl-tRNA synthetase. Out of these compounds, 3-(3-bromophenyl)-4-(3,5-dichlorophenylamino)furan-2(5H)-one (35) was the most active with IC(50) of 0.09 ± 0.02 μM. The structure-activity...

journal_title：European journal of medicinal chemistry

authors： Xiao ZP,Ma TW,Liao ML,Feng YT,Peng XC,Li JL,Li ZP,Wu Y,Luo Q,Deng Y,Liang X,Zhu HL

更新日期：2011-10-01 00:00:00

abstract：:With the continued rise of antibiotic resistance and reduced susceptibility to almost all front-line antibiotics, multidrug-resistant Gram-positive bacterial infections represent an incessant threat to healthcare providers. This study presents a new series of phenylthiazole compounds where two active moieties were com...

journal_title：European journal of medicinal chemistry

authors： ElAwamy M,Mohammad H,Hussien A,Abutaleb NS,Hagras M,Serya RAT,Taher AT,Abouzid KA,Seleem MN,Mayhoub AS

更新日期：2018-05-25 00:00:00

abstract：:Rhinovirus (RV), member of the Enterovirus genus, is known to be involved in more than half of the common colds. Through advances in molecular biology, rhinoviruses have also been associated with exacerbations of chronic pulmonary diseases (e.g. asthma, chronic obstructive pulmonary disease (COPD) and cystic fibrosis)...

journal_title：European journal of medicinal chemistry

authors： Da Costa L,Scheers E,Coluccia A,Rosetti A,Roche M,Neyts J,Terme T,Cirilli R,Mirabelli C,Silvestri R,Vanelle P

更新日期：2017-11-10 00:00:00

abstract：:Oxyprenylated secondary metabolites from plants, fungi, and bacteria, and their semisynthetic derivatives have been subject of growing interest during the last decade. Such natural products in fact have been discovered as potentially novel lead compounds for a series of pharmacological activities, mainly in terms of a...

journal_title：European journal of medicinal chemistry

authors： Fiorito S,Epifano F,Taddeo VA,Genovese S

更新日期：2018-06-10 00:00:00

abstract：:To further engineer dienones with optimal combinations of potency and bioavailability, thirty-four asymmetric 1,5-diarylpenta-1,4-dien-3-ones (25-58) have been designed and synthesized for the evaluation of their in vitro anti-proliferative activity in three human prostate cancer cell lines and one non-neoplastic pros...

journal_title：European journal of medicinal chemistry

authors： Zhang X,Guo S,Chen C,Perez GR,Zhang C,Patanapongpibul M,Subrahmanyam N,Wang R,Keith J,Chen G,Dong Y,Zhang Q,Zhong Q,Zheng S,Wang G,Chen QH

更新日期：2017-09-08 00:00:00

abstract：:With the aim of discovering potent and selective kinase inhibitors targeting ROS1 kinase, we designed, synthesized and screened a series of new pyrazol-4-ylpyrimidine derivatives based on our previously discovered lead compound KIST301072. Compounds 6a-e and 7a-e showed good to excellent activities against ROS1 kinase...

journal_title：European journal of medicinal chemistry

authors： Abdelazem AZ,Al-Sanea MM,Park BS,Park HM,Yoo KH,Sim T,Park JB,Lee SH,Lee SH

更新日期：2015-01-27 00:00:00

abstract：:A series of indole sesquiterpenes analogues of polyalthenol and pentacyclindole have been synthesized starting from ent-halimic acid in order to test their biological activity. These analogues include diverse oxidation levels at the sesquiterpenyl moiety and different functionalization on the indole ring. All syntheti...

journal_title：European journal of medicinal chemistry

authors： Marcos IS,Moro RF,Costales I,Basabe P,Díez D,Gil A,Mollinedo F,Pérez-de la Rosa F,Pérez-Roth E,Padrón JM

更新日期：2014-02-12 00:00:00

abstract：:A series of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives have been synthesized. The structures of these compounds were established by IR, 1H NMR, 13C NMR, Mass spectral data and elemental analyses. Compounds were evaluated for their anti-inflammatory and analgesic activity as well as gastri...

journal_title：European journal of medicinal chemistry

authors： Gaba M,Singh D,Singh S,Sharma V,Gaba P

更新日期：2010-06-01 00:00:00

abstract：:While nonsteroidal androgen receptor (AR) antagonists have been known for many years, and used in the clinic for the treatment of hormone dependent prostate cancer, very little is known about nonsteroidal AR agonists. We designed and synthesized a series of chiral bicalutamide analogs, which bear electron-withdrawing ...

journal_title：European journal of medicinal chemistry

authors： He Y,Yin D,Perera M,Kirkovsky L,Stourman N,Li W,Dalton JT,Miller DD

更新日期：2002-08-01 00:00:00

abstract：:New series of benzothiazole and pyrimido[2,1-b]benzothiazole derivatives were synthesized and characterized by analytical and spectrometrical methods (IR, HRMS, (1)H and (13)C NMR). Nineteen of the synthesized compounds were selected by the National Cancer Institute (NCI), USA, to be screened for their antitumor activ...

journal_title：European journal of medicinal chemistry

authors： Gabr MT,El-Gohary NS,El-Bendary ER,El-Kerdawy MM

更新日期：2014-10-06 00:00:00

abstract：:In order to discover new anticancer drug leads, a series of novel alkylamino pyrimidine derivatives were designed and synthesized based on our previous work via a ring-opening strategy. Biological evaluation with four human cancer cell lines (MDA-MB-231, A549, HepG2, and MCF-7) showed that most of these compounds poss...

journal_title：European journal of medicinal chemistry

authors： Zhao PL,Li YH,Yang HK,Chen P,Zhang B,Sun Q,Li Q,You WW

更新日期：2016-08-08 00:00:00

abstract：:Identification of potent anticancer agents with high selectivity and low toxicity remains on the way to human health. Pyridazine featuring advantageous physicochemical properties and antitumor potential usually is regarded as a central core in numerous anticancer derivatives. There are several approved pyridazine-base...

journal_title：European journal of medicinal chemistry

authors： He ZX,Gong YP,Zhang X,Ma LY,Zhao W

更新日期：2021-01-01 00:00:00

abstract：:A series of novel spirolactone-type diterpenoid derivatives of oridonin (12a-j) were designed and synthesized. All the target compounds showed improved anti-proliferative activity against a panel of human cancer cell lines and the most effective compound 12j was more potent than positive control Taxol in K562 and Bel-...

journal_title：European journal of medicinal chemistry

authors： Li D,Cai H,Jiang B,Liu G,Wang Y,Wang L,Yao H,Wu X,Sun Y,Xu J

更新日期：2013-01-01 00:00:00

abstract：:Twelve novel 8-hydroxyquinoline derivatives were synthesized with good yields by performing copper-catalyzed Huisgen 1,3-dipolar cycloaddition ("click" reaction) between an 8-O-alkylated-quinoline containing a terminal alkyne and various aromatic or protected sugar azides. These compounds were evaluated in vitro for t...

journal_title：European journal of medicinal chemistry

authors： Freitas LB,Borgati TF,de Freitas RP,Ruiz AL,Marchetti GM,de Carvalho JE,da Cunha EF,Ramalho TC,Alves RB

更新日期：2014-09-12 00:00:00

abstract：:[1,2,4]Triazolo[1,5-c]pyrimidine is a promising platform to develop adenosine receptor antagonists. Here, we tried to investigate the effect of the substituent at the 8 position of [1,2,4]triazolo[1,5-c]pyrimidine derivatives on affinity and selectivity at the human A3 adenosine receptor subtype. In particular, we hav...

journal_title：European journal of medicinal chemistry

authors： Federico S,Margiotta E,Salmaso V,Pastorin G,Kachler S,Klotz KN,Moro S,Spalluto G

更新日期：2018-09-05 00:00:00

abstract：:A series of ortho-, meta- and para-bis-N9-(methylphenylmethyl)purine derivatives 4-15 were obtained by two-step synthesis from various substituted chloropurines with alpha,alpha'-dichloroxylenes. These bis-N9-(methylphenylmethyl)purines 4-15 were evaluated for the primary cytotoxic activity against a panel of NCI-H460...

journal_title：European journal of medicinal chemistry

authors： Kode N,Chen L,Murthy D,Adewumi D,Phadtare S

更新日期：2007-03-01 00:00:00

abstract：:In an effort to develop potent antiamoebic agents, we have synthesized chalcones (1-8), amino-5-substituted-(3-phenyl(2-pyrazolinyl))methane-1-thione derivatives (1a-8a) and 2-(5-substituted-3-phenyl-2-pyrazolinyl)-1,3-thiazolino[5,4-b]quinoxaline derivatives (1b-8b) and evaluated for their in vitro antiamoebic activi...

journal_title：European journal of medicinal chemistry

authors： Budakoti A,Bhat AR,Azam A

更新日期：2009-03-01 00:00:00

abstract：:Heterocyclic compounds are the interesting core structures for the development of new bioactive compounds. Fatty acids are derived from renewable raw materials and exhibit various biological activities. Several researchers are amalgamating these two bioactive components to yield bioactive hybrid molecules with some de...

journal_title：European journal of medicinal chemistry

authors： Venepally V,Reddy Jala RC

更新日期：2017-12-01 00:00:00

abstract：:In this study, a series of 1,3,4-oxadiazole derivatives (5a-s, 10a-s, and 16a-d) were designed and synthesized using maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) models, to test the anticonvulsant activity of the target compounds in vivo. The neurotoxicity (NT) of the target compounds was mea...

journal_title：European journal of medicinal chemistry

authors： Wang S,Liu H,Wang X,Lei K,Li G,Li J,Liu R,Quan Z

更新日期：2020-11-15 00:00:00

abstract：:Antimitotic colchicine possesses low therapeutic index due to high toxicity effects in non-target cell. However, diverse colchicine analogs have been derivatized as intentions for toxicity reduction and structure-activity relationship (SAR) studying. Hybrid system of colchicine structure with nontoxic biofunctional co...

journal_title：European journal of medicinal chemistry

authors： Ghawanmeh AA,Chong KF,Sarkar SM,Bakar MA,Othaman R,Khalid RM

更新日期：2018-01-20 00:00:00

abstract：:GSK805 (1) is a potent RORγt inverse agonist, but a drawback of 1 is its low solubility, leading to a limited absorption in high doses. We have explored detailed structure-activity relationship on the amide linker, biaryl and arylsulfonyl moieties of 1 trying to improve solubility while maintaining RORγt activity. As ...

journal_title：European journal of medicinal chemistry

authors： Sun N,Huang Y,Yu M,Zhao Y,Chen JA,Zhu C,Song M,Guo H,Xie Q,Wang Y

更新日期：2020-09-15 00:00:00