EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全第8页

((S)-3-Mercapto-2-methylpropanamido)acetic acid derivatives as metallo-β-lactamase inhibitors: Synthesis, kinetic and crystallographic studies.
abstract：:The emergence and global spread of metallo-β-lactamase (MBL) mediated resistance to almost all β-lactam antibacterials poses a serious threat to public health. Since no clinically useful MBL inhibitors have been reported, there is an urgent need to develop new potent broad-spectrum MBL inhibitors effective against ant...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2018.01.032

authors： Liu S,Jing L,Yu ZJ,Wu C,Zheng Y,Zhang E,Chen Q,Yu Y,Guo L,Wu Y,Li GB

更新日期：2018-02-10 00:00:00
Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors.
abstract：:Shikonin exhibits powerful anticancer activities for various cancer cells, but its poor solubility and strong toxicity hinder its development as clinical anticancer agent. We previously confirmed that shikonin and its derivatives can disturb mitosis through targeting tubulin. In this study, α-lipoic acid, the naturall...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.12.019

authors： Lin HY,Han HW,Sun WX,Yang YS,Tang CY,Lu GH,Qi JL,Wang XM,Yang YH

更新日期：2018-01-20 00:00:00
Design, synthesis and biological evaluation of novel pyridine-thiazolidinone derivatives as anticancer agents: Targeting human carbonic anhydrase IX.
abstract：:In order to obtain novel Human carbonic anhydrase IX (CAIX) inhibitors, a series of pyridine-thiazolidinone derivatives was synthesized and characterized by various spectroscopic techniques. The binding affinity of the compounds was measured by fluorescence binding studies and enzyme inhibition activity using esterase...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.12.049

authors： Ansari MF,Idrees D,Hassan MI,Ahmad K,Avecilla F,Azam A

更新日期：2018-01-20 00:00:00
Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation.
abstract：:Antagonists addressing selectively NMDA receptors containing the GluN2B subunit are of particular interest for the treatment of various neurological disorders including neurodegenerative diseases. With the aim to bioisosterically replace the metabolically labile phenol of 7-amino-6,7,8,9-tetrahydro-5H-benzo[7]annulen-...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.12.054

authors： Temme L,Frehland B,Schepmann D,Robaa D,Sippl W,Wünsch B

更新日期：2018-01-20 00:00:00
Nitrogen-containing ecdysteroid derivatives vs. multi-drug resistance in cancer: Preparation and antitumor activity of oximes, oxime ethers and a lactam.
abstract：:Multidrug resistance is a widespread problem among various diseases and cancer is no exception. We had previously described the chemo-sensitizing activity of ecdysteroid derivatives with low polarity on drug susceptible and multi-drug resistant (MDR) cancer cells. We have also shown that these molecules have a marked ...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.12.032

authors： Vágvölgyi M,Martins A,Kulmány Á,Zupkó I,Gáti T,Simon A,Tóth G,Hunyadi A

更新日期：2018-01-20 00:00:00
Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.
abstract：:Cathepsin (Cat) K is a critical bone-resorbing protease and is a relevant target for the treatment of osteoporosis and bone metastasis, while CatS is an attractive target for drugs in autoimmune diseases (e.g. rheumatoid arthritis), emphysema or neuropathic pain. Despite major achievements, current pharmacological inh...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.12.012

authors： Galibert M,Wartenberg M,Lecaille F,Saidi A,Mavel S,Joulin-Giet A,Korkmaz B,Brömme D,Aucagne V,Delmas AF,Lalmanach G

更新日期：2018-01-20 00:00:00
Structure-activity studies on N-Substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation.
abstract：:FAD-dependent lysine-specific demethylase 1 (LSD1) is overexpressed or deregulated in many cancers such as AML and prostate cancer and hence is a promising anticancer target with first inhibitors in clinical trials. Clinical candidates are N-substituted derivatives of the dual LSD1-/monoamine oxidase-inhibitor tranylc...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.12.001

authors： Schulz-Fincke J,Hau M,Barth J,Robaa D,Willmann D,Kürner A,Haas J,Greve G,Haydn T,Fulda S,Lübbert M,Lüdeke S,Berg T,Sippl W,Schüle R,Jung M

更新日期：2018-01-20 00:00:00
Colchicine prodrugs and codrugs: Chemistry and bioactivities.
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

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2017.12.029

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

更新日期：2018-01-20 00:00:00
Polymeric bile acid sequestrants: Review of design, in vitro binding activities, and hypocholesterolemic effects.
abstract：:Polymeric bile acid sequestrants (BAS) have recently attracted much attention as lipid-lowering agents. These non-absorbable materials specifically bind bile acids (BAs) in the intestine, preventing bile acid (BA) reabsorption into the blood through enterohepatic circulation. Therefore, it is important to understand t...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2017.12.015

authors： Heřmánková E,Žák A,Poláková L,Hobzová R,Hromádka R,Širc J

更新日期：2018-01-20 00:00:00
Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.
abstract：:To address drug resistance caused by ALK kinase mutations, especially the most refractory and predominant mutation G1202R for the second-generation ALK inhibitor, a series of new diarylaminopyrimidine analogues were designed by incorporating a resorcinol moiety (A-ring) to interact the ALK kinase domain where the G120...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.12.060

authors： Geng K,Xia Z,Ji Y,Zhang RR,Sun D,Ai J,Song Z,Geng M,Zhang A

更新日期：2018-01-20 00:00:00
Design, synthesis, and biological evaluation of new 1,2,3-triazolo-2'-deoxy-2'-fluoro- 4'-azido nucleoside derivatives as potent anti-HBV agents.
abstract：:Novel drugs are urgently needed to combat hepatitis B virus (HBV) infection due to drug-resistant virus. In this paper, a series of novel 4-monosubstituted 2'-deoxy-2'-β-fluoro-4'-azido-β-d-arabinofuranosyl 1,2,3-triazole nucleoside analogues (1a-g) were designed, synthesized and screened for in vitro anti-HBV activit...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.11.028

authors： Liu Y,Peng Y,Lu J,Wang J,Ma H,Song C,Liu B,Qiao Y,Yu W,Wu J,Chang J

更新日期：2018-01-01 00:00:00
2-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.
abstract：:Microtubules are recognized as crucial components of the mitotic spindle during cell division, and, for this reason, the microtubule system is an attractive target for the development of anticancer agents. Continuing our search strategy for novel tubulin targeting-compounds, a new series of 2-alkoxycarbonyl-3-(3',4',5...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.11.096

authors： Romagnoli R,Kimatrai Salvador M,Schiaffino Ortega S,Baraldi PG,Oliva P,Baraldi S,Lopez-Cara LC,Brancale A,Ferla S,Hamel E,Balzarini J,Liekens S,Mattiuzzo E,Basso G,Viola G

更新日期：2018-01-01 00:00:00
Design and synthesis of novel quinacrine-[1,3]-thiazinan-4-one hybrids for their anti-breast cancer activity.
abstract：:In an attempt to develop effective and safe anticancer agents, we designed, synthesized and examined 23 novel quinacrine (QC) derivatives by combining the 9-aminoacridine scaffold and the [1,3]thiazinan-4-ones group. Most of these hybrids showed strong anticancer activities, among which 3-(3-(6-chloro-2-methoxyacridin...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.11.097

authors： Solomon VR,Pundir S,Le HT,Lee H

更新日期：2018-01-01 00:00:00
Synthesis and biological evaluation of novel alkylated polyamine analogues as potential anticancer agents.
abstract：:A new class of polyamine analogues modified by alkylation at the terminal of the polyamine chain has been synthesized and their structures were determined by 1H NMR, 13C NMR, ESI-MS and elemental analysis. As the representative compound, 3f displayed a broad spectrum of anti-cancer effects by MTT assays. Tumor xenogra...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.10.069

authors： Li M,Wang Y,Ge C,Chang L,Wang C,Tian Z,Wang S,Dai F,Zhao L,Xie S

更新日期：2018-01-01 00:00:00
Newly designed organotin(IV) carboxylates with peptide linkage: Synthesis, structural elucidation, physicochemical characterizations and pharmacological investigations.
abstract：:Fourteen new organotin(IV) carboxylate complexes with peptide linkage of (2-(4-methoxy-2-nitrophenylcarbamoyl)benzoic acid) were successfully synthesized and characterized by elemental analyses, FT-IR, NMR (1H, 13C and 119Sn) and single crystal X-ray techniques. FT-IR results of the sodium salt of 2-(4-methoxy-2-nitro...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.11.001

authors： Sirajuddin M,McKee V,Tariq M,Ali S

更新日期：2018-01-01 00:00:00
Recent advances in the discovery of potent and selective HDAC6 inhibitors.
abstract：:Histone deacetylase HDAC6, a member of the class IIb HDAC family, is unique among HDAC enzymes in having two active catalytic domains, and has unique physiological function. In addition to the modification of histone, HDAC6 targets specific substrates including α-tubulin and HSP90, and are involved in protein traffick...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2017.10.040

authors： Wang XX,Wan RZ,Liu ZP

更新日期：2018-01-01 00:00:00
Structure-activity analysis of CJ-15,801 analogues that interact with Plasmodium falciparum pantothenate kinase and inhibit parasite proliferation.
abstract：:Survival of the human malaria parasite Plasmodium falciparum is dependent on pantothenate (vitamin B5), a precursor of the fundamental enzyme cofactor coenzyme A. CJ-15,801, an enamide analogue of pantothenate isolated from the fungus Seimatosporium sp. CL28611, was previously shown to inhibit P. falciparum proliferat...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.08.050

authors： Spry C,Sewell AL,Hering Y,Villa MVJ,Weber J,Hobson SJ,Harnor SJ,Gul S,Marquez R,Saliba KJ

更新日期：2018-01-01 00:00:00
Xanthine oxidase inhibitory activity of natural and hemisynthetic flavonoids from Gardenia oudiepe (Rubiaceae) in vitro and molecular docking studies.
abstract：:Xanthine oxidase (XO), an enzyme widely distributed among mammalian tissues, is associated with the oxidation of xanthine and hypoxanthine to form uric acid. Reactive oxygen species are also released during this process, leading to oxidative damages and to the pathology called gout. Available treatments mainly based o...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.11.071

authors： Santi MD,Paulino Zunini M,Vera B,Bouzidi C,Dumontet V,Abin-Carriquiry A,Grougnet R,Ortega MG

更新日期：2018-01-01 00:00:00
Platanic acid: A new scaffold for the synthesis of cytotoxic agents.
abstract：:Thirty-seven different derivatives (2-38) have been prepared from platanic acid, a natural occurring triterpenoid. Main emphasis was the introduction of several N-containing functional groups such as amines, amides and oximes and their screening for cytotoxic activity employing several human tumor cell lines using SRB...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.11.046

authors： Kahnt M,Heller L,Grabandt P,Al-Harrasi A,Csuk R

更新日期：2018-01-01 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
Optimization of pharmacokinetic properties by modification of a carbazole-based cannabinoid receptor subtype 2 (CB2) ligand.
abstract：:Recently, the development of the fluorinated PET tracer [18F]1a for imaging of CB2 receptors in the central nervous system was reported. [18F]1a showed high CB2 affinity and selectivity over the CB1 subtype, but rapid biotransformation in mice. In addition to the amide hydrolysis, oxidative N-dealkylation and carbazol...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.10.049

authors： Heimann D,Börgel F,de Vries H,Bachmann K,Rose VE,Frehland B,Schepmann D,Heitman LH,Wünsch B

更新日期：2018-01-01 00:00:00
Synthesis of unprecedented steroidal spiro heterocycles as potential antiproliferative drugs.
abstract：:Herein we report the straightforward preparation of novel conformationally-restricted steroids from trans-androsterone and estrone, decorated with spiranic oxazolidin-2-one or 2-aminooxazoline motifs at C-17 as potential antiproliferative agents. Such unprecedented pharmacophores were accessed using an aminomethylalco...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.10.063

authors： Romero-Hernández LL,Merino-Montiel P,Meza-Reyes S,Vega-Baez JL,López Ó,Padrón JM,Montiel-Smith S

更新日期：2018-01-01 00:00:00
Synthesis and in vitro evaluation of novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids for their anti-mycobacterial activities.
abstract：:Twelve novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids 5a-l were designed, synthesized and screened for their in vitro anti-mycobacterial activities against drug-sensitive and multidrug-resistant Mycobacterium tuberculosis as well as cytotoxicity in VERO cell line. All hybrids exh...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.11.090

authors： Yan X,Lv Z,Wen J,Zhao S,Xu Z

更新日期：2018-01-01 00:00:00
Discovery of caffeic acid phenethyl ester derivatives as novel myeloid differentiation protein 2 inhibitors for treatment of acute lung injury.
abstract：:Myeloid differentiation protein 2 (MD2) is an essential molecule which recognizes lipopolysaccharide (LPS), leading to initiation of inflammation through the activation of Toll-like receptor 4 (TLR4) signaling. Caffeic acid phenethyl ester (CAPE) from propolis of honeybee hives could interfere interactions between LPS...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.11.066

authors： Chen L,Jin Y,Chen H,Sun C,Fu W,Zheng L,Lu M,Chen P,Chen G,Zhang Y,Liu Z,Wang Y,Song Z,Liang G

更新日期：2018-01-01 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
The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.
abstract：:Histone deacetylase (HDAC) enzymes govern the post-translational acetylation state of lysine residues on protein substrates, leading to regulatory changes in cell function. Due to their role in cancers, HDAC proteins have emerged as promising targets for cancer treatment. Four HDAC inhibitors have been approved as ant...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.10.076

authors： Negmeldin AT,Knoff JR,Pflum MKH

更新日期：2018-01-01 00:00:00
Identification of an oxime-containing C-glucosylarene as a potential inhibitor of sodium-dependent glucose co-transporter 2.
abstract：:Treatment of hyperglycemia with drugs that block renal glucose reabsorption via inhibition of sodium-dependent glucose cotransporter 2 (SGLT2) is a novel approach to diabetes management. In this study, twenty-seven aryl C-glycosides bearing a C=N/C-N linkage at the glucosyl C6 position were designed, synthesized and e...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.11.019

authors： Yuan MC,Yeh TK,Chen CT,Song JS,Huang YC,Hsieh TC,Huang CY,Huang YL,Wang MH,Wu SH,Yao CH,Chao YS,Lee JC

更新日期：2018-01-01 00:00:00
Recent advances in HER2 positive breast cancer epigenetics: Susceptibility and therapeutic strategies.
abstract：:HER2 amplification/overexpression accounts for aggressive clinical features of HER2 positive breast cancer. Epigenetic changes including DNA methylation, histone modifications and ncRNAs/miRNAs are associated with regulation of DNA chromatin and specifically, gene transcription. Hence, these produce eminent effects up...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2017.07.075

authors： Singla H,Ludhiadch A,Kaur RP,Chander H,Kumar V,Munshi A

更新日期：2017-12-15 00:00:00
Targeting Eph/ephrin system in cancer therapy.
abstract：:It is well established that the Eph/ephrin system plays a central role in the embryonic development, with minor implications in the physiology of the adult. However, it is overexpressed and deregulated in a variety of tumors, with a primary involvement in tumorigenesis, tumor angiogenesis, metastasis development, and ...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2017.07.029

authors： Lodola A,Giorgio C,Incerti M,Zanotti I,Tognolini M

更新日期：2017-12-15 00:00:00
Oleanane-, ursane-, and quinone methide friedelane-type triterpenoid derivatives: Recent advances in cancer treatment.
abstract：:Natural pentacyclic triterpenoids (PTs) have been often reported to exhibit a wide range of biological activities. Among them, the anticancer and anti-inflammatory activities are the most studied. Over the last two decades, the number of publications reporting the anticancer effects of PTs has risen exponentially, ref...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2017.07.013

authors： Salvador JAR,Leal AS,Valdeira AS,Gonçalves BMF,Alho DPS,Figueiredo SAC,Silvestre SM,Mendes VIS

更新日期：2017-12-15 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
Covalent binding design strategy: A prospective method for discovery of potent targeted anticancer agents.
abstract：:Cancer remains the most serious disease that threatens human health. Molecularly targeted cancer therapies, specifically small-molecule protein kinase inhibitors, form an important part of cancer therapy. Targeted covalent modification represents a proven approach to drug discovery with the recent FDA approvals of afa...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2017.09.024

authors： Wang L,Zhao J,Yao Y,Wang C,Zhang J,Shu X,Sun X,Li Y,Liu K,Yuan H,Ma X

更新日期：2017-12-15 00:00:00
Platinum, palladium, gold and ruthenium complexes as anticancer agents: Current clinical uses, cytotoxicity studies and future perspectives.
abstract：:Metallodrugs offer potential for unique mechanism of drug action based on the choice of the metal, its oxidation state, the types and number of coordinated ligands and the coordination geometry. This review illustrates notable recent progress in the field of medicinal bioinorganic chemistry as many new approaches to t...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2017.04.007

authors： Lazarević T,Rilak A,Bugarčić ŽD

更新日期：2017-12-15 00:00:00
A pentanoic acid derivative targeting matrix metalloproteinase-2 (MMP-2) induces apoptosis in a chronic myeloid leukemia cell line.
abstract：:Depending on our previous observations, some compounds of pentanoic acid were designed and synthesized. Characterization of the synthesized compounds was done by mass, NMR and IR spectroscopy as well as elemental analysis. Among the synthesized molecules, (2S)-5-oxo-2-[(nitrobenzene-4-yl sulfonyl) amino]-5-(pentylamin...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.09.052

authors： Mukherjee A,Adhikari N,Jha T

更新日期：2017-12-01 00:00:00
An insight into the biological activities of heterocyclic-fatty acid hybrid molecules.
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

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2017.09.069

authors： Venepally V,Reddy Jala RC

更新日期：2017-12-01 00:00:00
Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.
abstract：:Starting from nature as original source, new potential agents with pleiotropic activities have been synthesized and evaluated as neuroprotective agents. In this work, novel nature-based hybrids, combining antioxidant motifs with rivastigmine, have been designed and synthesized. The biological results revealed that the...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.10.006

authors： Nesi G,Chen Q,Sestito S,Digiacomo M,Yang X,Wang S,Pi R,Rapposelli S

更新日期：2017-12-01 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
Design, synthesis and biological evaluation of N-(4-alkoxy-3-cyanophenyl)isonicotinamide/nicotinamide derivatives as novel xanthine oxidase inhibitors.
abstract：:A series of N-(4-alkoxy-3-cyanophenyl)isonicotinamide/nicotinamide derivatives was designed, synthesized and evaluated for inhibitory potency in vitro against xanthine oxidase. The isonicotinamide series was considerably more effective than the nicotinamide series. SARs analysis revealed that the isonicotinoyl moiety ...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.09.051

authors： Zhang TJ,Li SY,Wang L,Sun Q,Wu QX,Zhang Y,Meng FH

更新日期：2017-12-01 00:00:00
African trypanosomiasis: Synthesis & SAR enabling novel drug discovery of ubiquinol mimics for trypanosome alternative oxidase.
abstract：:African trypanosomiasis is a parasitic disease affecting 5000 humans and millions of livestock animals in sub-Saharan Africa every year. Current treatments are limited, difficult to administer and often toxic causing long term injury or death in many patients. Trypanosome alternative oxidase is a parasite specific enz...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.09.067

authors： West RA,O'Doherty OG,Askwith T,Atack J,Beswick P,Laverick J,Paradowski M,Pennicott LE,Rao SPS,Williams G,Ward SE

更新日期：2017-12-01 00:00:00
Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
abstract：:Twenty hybrid compounds, tethering dihydroartemisinin (DHA) with diaryl-pyrazoline/diaryl-pyrazole through ether linkage, were synthesized based on hybridization strategy and assessed for their anticancer activity. The representative compound 6f exhibited significantly elevated antiproliferative activity compared with...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2017.10.023

authors： Luan S,Zhong H,Zhao X,Yang J,Jing Y,Liu D,Zhao L

更新日期：2017-12-01 00:00:00

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