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：:A library of indolyl-isoxazolidines (6-9) has been synthesized by regio- and stereoselective microwave irradiated 1,3-dipolar cycloadditions of C-(3-indolyl)-N-phenylnitrone (2') with variedly substituted dipolarophiles (3'-5') and screened for their anti-inflammatory activities through inhibition of pro-inflammatory ...

journal_title：European journal of medicinal chemistry

authors： Singh G,Singh G,Bhatti R,Gupta M,Kumar A,Sharma A,Singh Ishar MP

更新日期：2018-06-10 00:00:00

abstract：:Naturally occurring coumarins 7-isopentenyloxycoumarin, auraptene, and umbelliprenin are able to modulate the biosynthesis of melanin in murine Melan-a cells probably through the interaction with selected biological targets like estrogen receptor β and aryl hydrocarbon receptor. Such a modulation strictly depends on t...

journal_title：European journal of medicinal chemistry

authors： Fiorito S,Epifano F,Preziuso F,Cacciatore I,di Stefano A,Taddeo VA,de Medina P,Genovese S

更新日期：2018-05-25 00:00:00

abstract：:Our previous studies reveal that indolizinoquinolinedione scaffold is a base to develop novel DNA topoisomerase IB (TOP1) catalytic inhibitors. In this work, twenty-three novel indolizinoquinolinedione derivatives were synthesized. TOP1-mediated relaxation, nicking and unwinding assays revealed that three fluorinated ...

journal_title：European journal of medicinal chemistry

authors： Yu Q,Yang H,Zhu TW,Yu LM,Chen JW,Gu LQ,Huang ZS,An LK

更新日期：2018-05-25 00:00:00

abstract：:The plant-derived, diterpenoid 7-keto-sempervirol was recently reported to display moderate activity against larval stages of Schistosoma mansoni (IC50 = 19.1 μM) and Fasciola hepatica (IC50 = 17.7 μM), two related parasitic blood and liver flukes responsible for the neglected tropical diseases schistosomiasis and fas...

journal_title：European journal of medicinal chemistry

authors： Crusco A,Bordoni C,Chakroborty A,Whatley KCL,Whiteland H,Westwell AD,Hoffmann KF

更新日期：2018-05-25 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：:Diabetes is a fast growing chronic metabolic disorder around the world. Dipeptidyl peptidase-4 (DPP-4) is a new promising target during type 2 diabetes glycemic control. Thus, a number of potent DPP-4 inhibitors were developed and play a rapidly evolving role in the management of type 2 diabetes in recent years. This ...

journal_title：European journal of medicinal chemistry

authors： Li N,Wang LJ,Jiang B,Li XQ,Guo CL,Guo SJ,Shi DY

更新日期：2018-05-10 00:00:00

abstract：:Identifying desired interactions with a target receptor is often the first step when designing new active compounds. However, attention should also be focused on contacts with other proteins that result in either selective or polypharmacological compounds. Here, the search for the structural determinants of selectivit...

journal_title：European journal of medicinal chemistry

authors： Podlewska S,Kafel R,Lacivita E,Satała G,Kooistra AJ,Vass M,de Graaf C,Leopoldo M,Bojarski AJ,Mordalski S

更新日期：2018-05-10 00:00:00

abstract：:We herein report the design and synthesis of benzothiazinones containing a piperidine moiety as new antitubercular agents based on the structure feature of IMB-ZR-1 discovered in our lab. Some of them were found to have good in vitro activity (MIC < 1 μg/mL) against drug-susceptible Mycobacterium tuberculosis H37RV st...

journal_title：European journal of medicinal chemistry

authors： Lv K,Tao Z,Liu Q,Yang L,Wang B,Wu S,Wang A,Huang M,Liu M,Lu Y

更新日期：2018-05-10 00:00:00

abstract：:A series of novel 1, 2, 4-triazole/chalcone hybrids was prepared and identified with different spectroscopic techniques. The prepared compounds showed remarkable cytotoxic activity against different cancer cell lines. Compounds 24, 25, 27, 41 and 47 had shown the highest cytotoxicity among the tested compounds against...

journal_title：European journal of medicinal chemistry

authors： Ahmed FF,Abd El-Hafeez AA,Abbas SH,Abdelhamid D,Abdel-Aziz M

更新日期：2018-05-10 00:00:00

abstract：:A series of novel pyridone conjugated monobactams with various substituents at the (4) position were synthesized and evaluated for their antibacterial activities against a panel of multidrug-resistant (MDR) Gram-negative bacteria in vitro. Compounds 46d, 54 and 75e displayed good to moderate activities against P. aeru...

journal_title：European journal of medicinal chemistry

authors： Kou Q,Wang T,Zou F,Zhang S,Chen Q,Yang Y

更新日期：2018-05-10 00:00:00

abstract：:Three new iridium (III) complexes [Ir (ppy)2 (ipbc)](PF6) (1), [Ir (bzq)2 (ipbc)](PF6) (2) and [Ir (piq)2 (ipbc)](PF6) (3) were designed and synthesized. All the complexes were tested for anticancer activity using 3-(4,5-dimethylthiazole)-2,5-diphenyltetraazolium bromide (MTT) method. The complexes show no cytotoxic a...

journal_title：European journal of medicinal chemistry

authors： Zhang WY,Yi QY,Wang YJ,Du F,He M,Tang B,Wan D,Liu YJ,Huang HL

更新日期：2018-05-10 00:00:00

abstract：:To develop novel agents with anticancer activities, thirty-four new dihydroartemisinin-coumarin hybrids were designed and synthesized in this study. Those compounds were identified that had great anticancer activity against two cancer cell lines (MDA-MB-231 and HT-29). The structure-activity relationships of the deriv...

journal_title：European journal of medicinal chemistry

authors： Yu H,Hou Z,Tian Y,Mou Y,Guo C

更新日期：2018-05-10 00:00:00

abstract：:African trypanosomiasis is a neglected parasitic disease that is still of great public health relevance, and a severe impediment to agriculture in endemic areas. The pathogens possess certain unique metabolic features that can be exploited for the development of new drugs. Notably, they rely on an essential, mitochond...

journal_title：European journal of medicinal chemistry

authors： Ebiloma GU,Ayuga TD,Balogun EO,Gil LA,Donachie A,Kaiser M,Herraiz T,Inaoka DK,Shiba T,Harada S,Kita K,de Koning HP,Dardonville C

更新日期：2018-04-25 00:00:00

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

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

abstract：:As we are interested in synthetizing biologically active leads with dual anticancer and antibacterial activity, we adopted biology oriented drug synthesis (BIODS) strategy to synthesize a series of novel ciprofloxacin (CP) hybrids. The National Cancer Institute (USA) selected seventeen newly synthesized compounds for ...

journal_title：European journal of medicinal chemistry

authors： Kassab AE,Gedawy EM

更新日期：2018-04-25 00:00:00

abstract：:Leukotrienes (LTs) and prostaglandin (PG)E2 are enzymatically produced from arachidonic acid and represent highly bioactive lipid mediators with pro-inflammatory functions. Here, we report on novel multi-target inhibitors that potently and dually interfere with 5-lipoxygenase-activating protein (FLAP) and microsomal p...

journal_title：European journal of medicinal chemistry

authors： Gür ZT,Çalışkan B,Garscha U,Olgaç A,Schubert US,Gerstmeier J,Werz O,Banoglu E

更新日期：2018-04-25 00:00:00

abstract：:Conjugation to carrier proteins is a way to improve the immunogenicity of peptides. Such is the case for peptides mimicking carbohydrate tumor-associated antigens in cancer vaccine development. The most used protein for this purpose is the keyhole limpet hemocyanin (KLH) from Megathura crenulata. Its limited bioavaila...

journal_title：European journal of medicinal chemistry

authors： Palacios M,Tampe R,Del Campo M,Zhong TY,López MN,Salazar-Onfray F,Becker MI

更新日期：2018-04-25 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 series of α-santonin-derived compounds as potentially anti-hepatoma agents were designed and synthesized in an effort to find novel therapeutic agents. Among them, derivative 5h was more potent than the positive control 5-fluorouracil (5-Fu) on HepG-2, QGY-7703 and SMMC-7721 with IC50 values of 7.51, 3.06 and 4.08 μ...

journal_title：European journal of medicinal chemistry

authors： Chen H,Yang X,Yu Z,Cheng Z,Yuan H,Zhao Z,Wu G,Xie N,Yuan X,Sun Q,Zhang W

更新日期：2018-04-10 00:00:00

abstract：:The CXC chemokine receptor 4 (CXCR4) is a highly reserved G-protein coupled 7-transmembrane (TM) chemokine receptor which consists of 352 amino acids. CXCR4 has only one endogenous chemokine ligand of CXCL12, besides several other natural nonchemokine ligands such as extracellular ubiquitin and noncognate ligand of MI...

journal_title：European journal of medicinal chemistry

authors： Peng D,Cao B,Zhou YJ,Long YQ

更新日期：2018-04-10 00:00:00

abstract：:A new series of Schizandrin (1) derivatives were synthesized utilizing the C-9 position of the Schizandrin core and evaluated for their cytotoxic activities against HeLa (cervical cancer), A549 (lung cancer), MCF-7 (breast cancer) and DU-145 (prostate cancer) cell lines. Among the synthesized series, 4e, 4f, 4g and 5 ...

journal_title：European journal of medicinal chemistry

authors： Amujuri D,Siva B,Poornima B,Sirisha K,Sarma AVS,Lakshma Nayak V,Tiwari AK,Purushotham U,Suresh Babu K

更新日期：2018-04-10 00:00:00

abstract：:Here we report the design, synthesis, and molecular modeling of new potent and selective imidazole-based HO-1 inhibitors in which the imidazole nucleus and the hydrophobic groups are linked by a phenylethanolic spacer. Most of the tested compounds showed a good inhibitor activity with IC50 values in the low micromolar...

journal_title：European journal of medicinal chemistry

authors： Salerno L,Amata E,Romeo G,Marrazzo A,Prezzavento O,Floresta G,Sorrenti V,Barbagallo I,Rescifina A,Pittalà V

更新日期：2018-03-25 00:00:00

abstract：:Modification of a HCV NS5A inhibitor, ombitasvir, led to the identification of 10d with improved pan-genotype NS5A inhibition and better pharmacokinetic properties. The key structural changes to ombitasvir include bioisosteric replacement of carbon with silicon atom. Compared with ombitasvir, the activity of anti-HCV ...

journal_title：European journal of medicinal chemistry

authors： Liu B,Gai K,Qin H,Liu X,Cao Y,Lu Q,Lu D,Chen D,Shen H,Song W,Zhang Y,Wang X,Xu H,Zhang Y

更新日期：2018-03-25 00:00:00

abstract：:The coupling of gemcitabine with functionalized carboxylic acids using peptide coupling conditions afforded 4-N-alkanoyl analogues with a terminal alkyne or azido moiety. Reaction of 4-N-tosylgemcitabine with azidoalkyl amine provided 4-N-alkyl gemcitabine with a terminal azido group. Click reaction with silane buildi...

journal_title：European journal of medicinal chemistry

authors： Gonzalez C,Sanchez A,Collins J,Lisova K,Lee JT,Michael van Dam R,Alejandro Barbieri M,Ramachandran C,Wnuk SF

更新日期：2018-03-25 00:00:00

abstract：:Ovarian cancer is one of the leading causes of death related to the female reproductive system in western countries. Adverse side effects and resistance to platinum based chemotherapy have become the major obstacles for ovarian cancer treatment. Natural products have gained great attention in cancer treatment in recen...

journal_title：European journal of medicinal chemistry

authors： Zhang Y,Chen S,Wei C,Rankin GO,Ye X,Chen YC

更新日期：2018-03-10 00:00:00

abstract：:A new series of sixteen multifunctional N-benzyl-piperidine-aryl-acylhydrazones hybrid derivatives was synthesized and evaluated for multi-target activities related to Alzheimer's disease (AD). The molecular hybridization approach was based on the combination, in a single molecule, of the pharmacophoric N-benzyl-piper...

journal_title：European journal of medicinal chemistry

authors： Dias Viegas FP,de Freitas Silva M,Divino da Rocha M,Castelli MR,Riquiel MM,Machado RP,Vaz SM,Simões de Lima LM,Mancini KC,Marques de Oliveira PC,Morais ÉP,Gontijo VS,da Silva FMR,D'Alincourt da Fonseca Peçanha D,Castro NG,N

更新日期：2018-03-10 00:00:00

abstract：:A series of newly asymmetric dimeric β-carbolines with a spacer of 4-6 methylene units between the indole nitrogen and the harmine oxygen were synthesized. Structures of all the novel synthesized compounds were confirmed by their spectral and analytical studies. All of the synthesized compounds were screened for their...

journal_title：European journal of medicinal chemistry

authors： Guo L,Chen W,Cao R,Fan W,Ma Q,Zhang J,Dai B

更新日期：2018-03-10 00:00:00

abstract：:The most common fullerene member C60 displays many biological applications, such as, anticancer, human immunodeficiency virus and hepatitis C virus inhibitors, O2 uptake inhibitor and vectors for drug and DNA. Nevertheless, the innate hydrophobicity of C60 constrains its further development. We introduced cyclodextrin...

journal_title：European journal of medicinal chemistry

authors： Zhu X,Xiao S,Zhou D,Sollogoub M,Zhang Y

更新日期：2018-02-25 00:00:00

abstract：:The enoyl-ACP reductase InhA from the mycobacterial fatty acid biosynthesis pathway has become a target of interest for the development of new anti-tubercular drugs. This protein has been identified as essential for the survival of Mycobacterium tuberculosis, the causative agent of tuberculosis, and as the main target...

journal_title：European journal of medicinal chemistry

authors： Chollet A,Maveyraud L,Lherbet C,Bernardes-Génisson V

更新日期：2018-02-25 00:00:00

abstract：:Five bioactive dehydroabietylamine Schiff-base derivatives (L1-L5) had been synthesized from Dehydroabietylamine (L0), and the complex Cu(L1)2 had been obtained from the compound L1 and copper(II) acetate. Their activities against Hela (cervix), MCF-7 (breast), A549 (lung), HepG2 (liver) and HUVEC (umbilical vein, nor...

journal_title：European journal of medicinal chemistry

authors： Zhao F,Wang W,Lu W,Xu L,Yang S,Cai XM,Zhou M,Lei M,Ma M,Xu HJ,Cao F

更新日期：2018-02-25 00:00:00

abstract：:Tuberculosis (TB) remains one of the most widespread and leading deadliest diseases, around one-third of the world's population harbor a latent infection by Mycobacterium tuberculosis (MTB), and 5-10% eventually develop an active TB. The emergency of MTB new virulent forms as well as the co-infection between MTB and H...

journal_title：European journal of medicinal chemistry

authors： Fan YL,Wu JB,Cheng XW,Zhang FZ,Feng LS

更新日期：2018-02-25 00:00:00

abstract：:Several hitherto unknown (E)-but-2-enyl nucleoside phosphonoamidate analogs (ANPs) were prepared directed with nitrogen reagents by cross-metathesis in water-under ultrasound irradiation. Two diastereoisomers were formally identified by X-ray diffraction. These compounds were evaluated against a large spectrum of DNA ...

journal_title：European journal of medicinal chemistry

authors： Bessières M,Hervin V,Roy V,Chartier A,Snoeck R,Andrei G,Lohier JF,Agrofoglio LA

更新日期：2018-02-25 00:00:00

abstract：:Cannabinoid type 2 (CB2) receptor continues to emerge as a promising drug target for many diseases and conditions. New tools for studying CB2 receptor are required to further inform how this receptor functions in healthy and diseased states. The alkyl indole scaffold is a well-recognised ligand for cannabinoid recepto...

journal_title：European journal of medicinal chemistry

authors： Cooper AG,MacDonald C,Glass M,Hook S,Tyndall JDA,Vernall AJ

更新日期：2018-02-10 00:00:00

abstract：:Lapachol is an abundant prenyl naphthoquinone occurring in Brazilian Bignoniaceae that was clinically used, in former times, as an antimalarial drug, despite its moderate effect. Aiming to search for potentially better antimalarials, a series of 1,2,3-triazole derivatives was synthesized by chemical modification of la...

journal_title：European journal of medicinal chemistry

authors： Brandão GC,Rocha Missias FC,Arantes LM,Soares LF,Roy KK,Doerksen RJ,Braga de Oliveira A,Pereira GR

更新日期：2018-02-10 00:00:00

abstract：:Many diseases are believed to be driven by pathological levels of reactive oxygen species (ROS) and oxidative stress has long been recognized as a driver for inflammatory disorders. Apoptosis signal-regulating kinase 1 (ASK1) has been reported to be activated by intracellular ROS and its inhibition leads to a down reg...

journal_title：European journal of medicinal chemistry

authors： Lovering F,Morgan P,Allais C,Aulabaugh A,Brodfuehrer J,Chang J,Coe J,Ding W,Dowty H,Fleming M,Frisbie R,Guzova J,Hepworth D,Jasti J,Kortum S,Kurumbail R,Mohan S,Papaioannou N,Strohbach JW,Vincent F,Lee K,Zapf CW

更新日期：2018-02-10 00:00:00

abstract：:Using a dengue replicon cell line-based screening, we identified 3-(dimethylamino)propyl(3-((4-(4-fluorophenyl)-1-oxophthalazin-2(1H)-yl)methyl)phenyl)carbamate (10a) as a potent DENV-2 inhibitor, with an IC50 value of 0.64 μM. A series of novel phthalazinone derivatives based on hit 10a were synthesized and evaluated...

journal_title：European journal of medicinal chemistry

authors： Lu D,Liu J,Zhang Y,Liu F,Zeng L,Peng R,Yang L,Ying H,Tang W,Chen W,Zuo J,Tong X,Liu T,Hu Y

更新日期：2018-02-10 00:00:00

abstract：:This review aims to be a comprehensive, authoritative, critical, and readable review of general interest to the medicinal chemistry community because it focuses on the pharmacological, chemical, structural and computational aspects of diverse chemical categories as monoamine oxidase inhibitors (MAOIs). Monoamine oxida...

journal_title：European journal of medicinal chemistry

authors： Tripathi AC,Upadhyay S,Paliwal S,Saraf SK

更新日期：2018-02-10 00:00:00

abstract：:Cardiac glycosides exhibit significant anticancer effects and the glycosyl substitution at C3 position of digoxigenin is pivotal for their biological activity. In order to study the structure-activity relationship (SAR) of cardiac glycosides toward cancers and explore more potent anticancer agents, a series of C3-O-ne...

journal_title：European journal of medicinal chemistry

authors： Li XS,Ren YC,Bao YZ,Liu J,Zhang XK,Zhang YW,Sun XL,Yao XS,Tang JS

更新日期：2018-02-10 00:00:00

abstract：:Heat shock protein 90 (HSP90) inhibition has aroused increasing enthusiasm in antitumor strategies in recent years. According to our previous studies, we synthesized a series of coumarin pyrazoline compounds HCP1-HCP6 that might be HSP90 inhibitors. Interactions between HCP1-HCP6 and HSP90 were examined and antitumor ...

journal_title：European journal of medicinal chemistry

authors： Wei Q,Ning JY,Dai X,Gao YD,Su L,Zhao BX,Miao JY

更新日期：2018-02-10 00:00:00