abstract：:A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds 8c-i, k, l, bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ring possess high CB2R ...

journal_title：European journal of medicinal chemistry

authors： Mugnaini C,Rabbito A,Brizzi A,Palombi N,Petrosino S,Verde R,Di Marzo V,Ligresti A,Corelli F

更新日期：2019-01-01 00:00:00

abstract：:Two platinum(II) complexes, [Pt(ClQ)(DMSO)Cl] (ClQ-Pt) and [Pt(BrQ)(DMSO)Cl] (BrQ-Pt), with 5,7-dichloro-2-methyl-8-quinolinol (H-ClQ) and 5,7-dibromo-2-methyl-8-quinolinol (H-BrQ) as ligands, respectively, have been synthesized and characterized. The single-crystal X-ray diffraction characterization as well as other ...

journal_title：European journal of medicinal chemistry

authors： Qin QP,Wang SL,Tan MX,Liu YC,Meng T,Zou BQ,Liang H

更新日期：2019-01-01 00:00:00

abstract：:Of the three enzymes that regulate the biosynthesis of melanin, tyrosinase and its related proteins TYRP-1 and TYRP-2, tyrosinase is the most important because of its ability to limit the rate of melanin production in melanocytes. For treating skin pigmentation disorders caused by an excess of melanin, the inhibition ...

journal_title：European journal of medicinal chemistry

authors： Ullah S,Kang D,Lee S,Ikram M,Park C,Park Y,Yoon S,Chun P,Moon HR

更新日期：2019-01-01 00:00:00

abstract：:In this study, three novel series of benzoxazinone, benzothiopyranone and benzopyranone derivatives were designed through scaffold morphing from benzothiazinones to target DprE1. All compounds were evaluated for their in vitro activities against Mycobacterium tuberculosis and cytotoxicity against Vero cell line. Among...

journal_title：European journal of medicinal chemistry

authors： Li P,Wang B,Zhang X,Batt SM,Besra GS,Zhang T,Ma C,Zhang D,Lin Z,Li G,Huang H,Lu Y

更新日期：2018-12-05 00:00:00

abstract：:We describe the design, synthesis, and biological evaluation of a series of novel HIV-1 protease inhibitors with carboxamide derivatives as the P2 ligands. We have specifically designed aminothiochromane and aminotetrahydronaphthalene-based carboxamide ligands to promote hydrogen bonding and van der Waals interactions...

journal_title：European journal of medicinal chemistry

authors： Ghosh AK,Jadhav RD,Simpson H,Kovela S,Osswald H,Agniswamy J,Wang YF,Hattori SI,Weber IT,Mitsuya H

更新日期：2018-12-05 00:00:00

abstract：:The design, synthesis and evaluation of a small series of potent amphiphilic norbornane antibacterial agents has been performed (compound 10 MIC = 0.25 μg/mL against MRSA). Molecular modelling indicates rapid aggregation of this class of antibacterial agent prior to membrane association and insertion. Two fluorescent ...

journal_title：European journal of medicinal chemistry

authors： Hickey SM,Ashton TD,Boer G,Bader CA,Thomas M,Elliott AG,Schmuck C,Yu HY,Li J,Nation RL,Cooper MA,Plush SE,Brooks DA,Pfeffer FM

更新日期：2018-12-05 00:00:00

abstract：:Protein-protein interactions are attractive targets because they control numerous cellular processes. In oncology, apoptosis regulating Bcl-2 family proteins are of particular interest. Apoptotic cell death is controlled via PPIs between the anti-apoptotic proteins hydrophobic groove and the pro-apoptotic proteins BH3...

journal_title：European journal of medicinal chemistry

authors： Hedir S,De Giorgi M,Fogha J,De Pascale M,Weiswald LB,Brotin E,Marekha B,Denoyelle C,Denis C,Suzanne P,Gautier F,Juin P,Ligat L,Lopez F,Carlier L,Legay R,Bureau R,Rault S,Poulain L,Oliveira Santos JS,Voisin-Chiret

更新日期：2018-11-05 00:00:00

abstract：:A series of 3-N-aryl substituted-2-heteroarylchromones was efficiently synthesized via Pd-mediated oxidative coupling under the influence of hetero-atoms neighboring group participation. Synthesized molecules were evaluated against human microtubule affinity regulating kinase 4 (MARK4) enzyme inhibitors, a recently id...

journal_title：European journal of medicinal chemistry

authors： Parveen I,Khan P,Ali S,Hassan MI,Ahmed N

更新日期：2018-11-05 00:00:00

abstract：:Resistance to combretastatin A-4 is mediated by metabolic modification of the phenolic hydroxyl and ether groups of the 3-hydroxy-4-methoxyphenyl (B ring). Replacement of the B ring of combretastatin A-4 by a N-methyl-5-indolyl reduces tubulin polymerization inhibition (TPI) and cytotoxicity against human cancer cell ...

journal_title：European journal of medicinal chemistry

authors： Álvarez R,Gajate C,Puebla P,Mollinedo F,Medarde M,Peláez R

更新日期：2018-10-05 00:00:00

abstract：:In this work, we designed and synthesized tacrine platinum(II) complexes [PtClL(DMSO)]⋅CH3OH (Pt1), [PtClL(DMP)] (Pt2), [PtClL(DPPTH)] (Pt3), [PtClL(PTH)] (Pt4), [PtClL(PIPTH)] (Pt5), [PtClL(PM)] (Pt6) and [PtClL(en)] (Pt7) with 4,4'-dimethyl-2,2'-bipyridine (DMP), 4,7-diphenyl-1,10-phenanthroline (DPPTH), 1,10-phenan...

journal_title：European journal of medicinal chemistry

authors： Qin QP,Wang SL,Tan MX,Wang ZF,Luo DM,Zou BQ,Liu YC,Yao PF,Liang H

更新日期：2018-10-05 00:00:00

abstract：:Aurora A, Aurora B and Kinase Insert Domain-containing Receptor (KDR) play essential roles in sustained cancer growth. In the present study, eighteen pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives were designed and synthesized. Most of the prepared compounds exhibited obviously enzymatic (Aurora A/B and KDR)...

journal_title：European journal of medicinal chemistry

authors： Zhang Q,Shen Q,Gao L,Tong L,Li J,Chen Y,Lu W

更新日期：2018-10-05 00:00:00

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

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

abstract：:Based on our previous studies and predictive docking results, furans and thiophenes were introduced to the privileged tetrahydro-β-carboline scaffold to generate more potent and selective PDE5 inhibitors. A total of 66 novel furyl/thienyl tetrahydro-β-carboline derivatives were designed, synthesized and evaluated for ...

journal_title：European journal of medicinal chemistry

authors： Zheng H,Wu Y,Sun B,Cheng C,Qiao Y,Jiang Y,Zhao S,Xie Z,Tan J,Lou H

更新日期：2018-10-05 00:00:00

abstract：:To identify ALK and ROS1 dual inhibitors conferring resistance to ALK secondary mutations, especially 'gatekeeper' L1196 M and the most predominant ceritinib-resistant G1202R mutations, a series of novel 2,4-diarylaminopyrimidine analogues were designed and synthesized by incorporating 2-alkoxy-6-alicyclic aminopyridi...

journal_title：European journal of medicinal chemistry

authors： Guo M,Zuo D,Zhang J,Xing L,Gou W,Jiang F,Jiang N,Zhang D,Zhai X

更新日期：2018-10-05 00:00:00

abstract：:The multifactorial nature of Alzheimer's disease (AD) calls for the development of multitarget agents addressing key pathogenic processes. A novel family of donepezil-butylated hydroxytoluene (BHT) hybrids were designed, synthesized and evaluated as multifunctional ligands against AD. The optimal compound 7d displayed...

journal_title：European journal of medicinal chemistry

authors： Cai P,Fang SQ,Yang HL,Yang XL,Liu QH,Kong LY,Wang XB

更新日期：2018-09-05 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 novel series of 4, 6-disubstituted pyrimidines derivatives were designed, synthesized, and evaluated as epidermal growth factor receptor (EGFR) inhibitors for non-small cell lung cancer(NSCLC). 4, 6-disubstituted pyrimidines as core structure was utilized to substitute the lead structure AZD3759 of the quinazoline b...

journal_title：European journal of medicinal chemistry

authors： Zhang Y,Lv H,Luo L,Xu Y,Pan Y,Wang Y,Lin H,Xiong J,Guo P,Zhang J,Li X,Ye F

更新日期：2018-09-05 00:00:00

abstract：:Aurora kinases play critical roles in the regulation of the cell cycle and mitotic spindle assembly. Aurora A kinase, a member of the Aurora protein family, is frequently highly expressed in tumors, and selective Aurora A inhibition serves as a significant component of anticancer therapy. However, designing highly sel...

journal_title：European journal of medicinal chemistry

authors： Long L,Wang YH,Zhuo JX,Tu ZC,Wu R,Yan M,Liu Q,Lu G

更新日期：2018-09-05 00:00:00

abstract：:Immunotherapy has been increasingly utilized for the treatment of cancer. Currently available cancer immunotherapies mainly involve the use of antibodies, which have advantages in terms of pharmacodynamics such as efficacy and specificity, however, they exhibit disadvantages in regard to the pharmacokinetics including...

journal_title：European journal of medicinal chemistry

authors： Cheng B,Yuan WE,Su J,Liu Y,Chen J

更新日期：2018-09-05 00:00:00

abstract：:Piperidine is an important pharmacophore, a privileged scaffold and an excellent heterocyclic system in the field of drug discovery which provides numerous opportunities in studying/exploring this moiety as an anticancer agent by acting on various receptors of utmost importance. Cancer is an uncontrolled division of c...

journal_title：European journal of medicinal chemistry

authors： Goel P,Alam O,Naim MJ,Nawaz F,Iqbal M,Alam MI

更新日期：2018-09-05 00:00:00

abstract：:SH2 domain-containing inositol 5'-phosphatase 2 (SHIP2) is a lipid phosphatase that produce phosphatidylinositol 3,4-bisphosphate (PI(3,4)P2) from phosphatidylinositol 3,4,5-triphosphate (PI(3,4,5)P3), and is involved in many diseases such as neurodegenerative diseases. A recent report demonstrating that SHIP2 inhibit...

journal_title：European journal of medicinal chemistry

authors： Lim JW,Kim SK,Choi SY,Kim DH,Gadhe CG,Lee HN,Kim HJ,Kim J,Cho SJ,Hwang H,Seong J,Jeong KS,Lee JY,Lim SM,Lee JW,Pae AN

更新日期：2018-09-05 00:00:00

abstract：:A series of bis-salicylaldimine ligands bearing two ON-donor functions were reacted with dichloro(p-cymene)ruthenium(II) dimer in the presence of base (NaOAc) and a series of four dimetallic Ru(II) arene complexes (Ru(p-cymene))2(bis-salicylaldimine)Cl2 (C1C4) were prepared. These complexes were obtained in excellent ...

journal_title：European journal of medicinal chemistry

authors： Rahman FU,Bhatti MZ,Ali A,Duong HQ,Zhang Y,Ji X,Lin Y,Wang H,Li ZT,Zhang DW

更新日期：2018-09-05 00:00:00

abstract：:Escherichia coli (E. coli) is the most common pathogen in both hospital and community settings, and is capable of causing infections that can lead to serious consequences. Quinolones, one of the most common antibiotics in clinical use, are effective weapons to treat E. coli infections. However, the resistance of E. co...

journal_title：European journal of medicinal chemistry

authors： Gao F,Wang P,Yang H,Miao Q,Ma L,Lu G

更新日期：2018-09-05 00:00:00

abstract：:Six series of semisynthetic lipophilic glycopeptide antibiotic derivatives were evaluated for in vitro activity against influenza A and B viruses. The new teicoplanin pseudoaglycon-derived lipoglycopeptides were prepared by coupling one or two side chains to the N-terminus of the glycopeptide core, using various conju...

journal_title：European journal of medicinal chemistry

authors： Szűcs Z,Kelemen V,Le Thai S,Csávás M,Rőth E,Batta G,Stevaert A,Vanderlinden E,Naesens L,Herczegh P,Borbás A

更新日期：2018-09-05 00:00:00

abstract：:New series of 5-(morpholinosulfonyl) isatin derivatives were designed and synthesized. The new compounds were characterized on the basis of spectral and elemental analyses. They were examined for their cytotoxic effects using SRB assay on four cancer cell lines HepG2, HCT116, CACO and MCF-7 in addition to the non-canc...

journal_title：European journal of medicinal chemistry

authors： Ammar YA,Sh El-Sharief AM,Belal A,Abbas SY,Mohamed YA,Mehany ABM,Ragab A

更新日期：2018-08-05 00:00:00

abstract：:Leukotrienes (LTs) and prostaglandin (PG)E2, produced by 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1), respectively, are key players in inflammation, and pharmacological suppression of these lipid mediators (LM) represents a strategy to intervene with inflammatory disorders. Previous stud...

journal_title：European journal of medicinal chemistry

authors： Cheung SY,Werner M,Esposito L,Troisi F,Cantone V,Liening S,König S,Gerstmeier J,Koeberle A,Bilancia R,Rizza R,Rossi A,Roviezzo F,Temml V,Schuster D,Stuppner H,Schubert-Zsilavecz M,Werz O,Hanke T,Pace S

更新日期：2018-08-05 00:00:00

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

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

abstract：:A series of dihydropyrimidinone derivatives bearing various N-heterocyclic moieties was designed and synthesized. Twelve new compounds were screened for their cytotoxic activity using 60 cancer cell lines according to NCI (USA) protocol. Compound 19 showed a significant activity against NCI-H460, SK-MEL-5, and HL-60 (...

journal_title：European journal of medicinal chemistry

authors： Mostafa AS,Selim KB

更新日期：2018-08-05 00:00:00

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

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

abstract：:In the last two decades, trans-sialidase of Trypanosoma cruzi (TcTS) has been an important pharmacological target for developing new anti-Chagas agents. In a continuous effort to discover new potential TcTS inhibitors, 3-amino-3-arylpropionic acid derivatives (series A) and novel phthaloyl derivatives (series B, C and...

journal_title：European journal of medicinal chemistry

authors： Kashif M,Chacón-Vargas KF,López-Cedillo JC,Nogueda-Torres B,Paz-González AD,Ramírez-Moreno E,Agusti R,Uhrig ML,Reyes-Arellano A,Peralta-Cruz J,Ashfaq M,Rivera G

更新日期：2018-08-05 00:00:00

abstract：:The development of safe and affordable antiparasitic agents effective against neglected tropical diseases is a big challenge of the drug discovery. The drugs currently employed have limitations such as poor efficacy, drug resistance or side effects. Thus, the search for new promising drugs is more and more crucial. Me...

journal_title：European journal of medicinal chemistry

authors： Ravera M,Moreno-Viguri E,Paucar R,Pérez-Silanes S,Gabano E

更新日期：2018-07-15 00:00:00

abstract：:This paper describes the synthesis and characterization of N5-(hetero)arylalkyl-substituted-thiazolo [5,4-d]pyrimidine-5,7-diamine derivatives (4-19) as novel human (h) A2A adenosine receptor (AR) inverse agonists. Competition binding and cyclic AMP assays indicate that the examined compounds behave as hA2A AR inverse...

journal_title：European journal of medicinal chemistry

authors： Varano F,Catarzi D,Vincenzi F,Falsini M,Pasquini S,Borea PA,Colotta V,Varani K

更新日期：2018-07-15 00:00:00

abstract：:A series of new dithiocarbamates containing a 2(5H)-furanone-piperazine group was synthesized. These compounds show good in vitro cytoxic activity. Among them, compound 6c exhibits the best inhibitory activity against HeLa cell lines with an IC50 of 0.06 ± 0.01 μM for 72 h, and it has good inhibitory activity against ...

journal_title：European journal of medicinal chemistry

authors： Wei MX,Zhang J,Ma FL,Li M,Yu JY,Luo W,Li XQ

更新日期：2018-07-15 00:00:00

abstract：:Epidermal growth factor receptor (EGFR) signaling pathway has been previously investigated for its significant role in the progression of different types of malignant tumors, where development of small molecules targeting EGFR is well known strategy for design of antitumor agents. Herein, we report the design and synt...

journal_title：European journal of medicinal chemistry

authors： Ismail RSM,Abou-Seri SM,Eldehna WM,Ismail NSM,Elgazwi SM,Ghabbour HA,Ahmed MS,Halaweish FT,Abou El Ella DA

更新日期：2018-07-15 00:00:00

abstract：:Bromodomain and plant homeodomain (PHD) finger containing protein 1 (BRPF1) is a member of subfamily IV of the human bromodomains. Experimental evidence suggests that BRPF1 is involved in leukemia. In a previous high-throughput docking campaign we identified several chemotypes targeting the BRPF1 bromodomain. Here, ph...

journal_title：European journal of medicinal chemistry

authors： Zhu J,Zhou C,Caflisch A

更新日期：2018-07-15 00:00:00

abstract：:Radiolabeled heterobivalent peptidic ligands (HBPLs), being able to address different receptors, are highly interesting tumor imaging agents as they can offer multiple advantages over monovalent peptide receptor ligands. However, few examples of radiolabeled HBPLs have been described so far. One promising approach is ...

journal_title：European journal of medicinal chemistry

authors： Lindner S,Fiedler L,Wängler B,Bartenstein P,Schirrmacher R,Wängler C

更新日期：2018-07-15 00:00:00

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

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

abstract：:The endocannabinoid system (ECS) represents one of the major neuromodulatory systems involved in different physiological and pathological processes. Multi-target compounds exert their activities by acting via multiple mechanisms of action and represent a promising pharmacological modulation of the ECS. In this work we...

journal_title：European journal of medicinal chemistry

authors： Chicca A,Arena C,Bertini S,Gado F,Ciaglia E,Abate M,Digiacomo M,Lapillo M,Poli G,Bifulco M,Macchia M,Tuccinardi T,Gertsch J,Manera C

更新日期：2018-06-25 00:00:00

abstract：:NEDD8 activating enzyme (NAE) plays an important role in regulating intracellular proteins with key parts in a broad array of cellular functions. On the basis of previously work, a series of 2H-chromen-2-one based NAE inhibitors were designed and synthesized. Through enzyme-based and cell-based assays, LP0040 was iden...

journal_title：European journal of medicinal chemistry

authors： Lu P,Guo Y,Zhu L,Xia Y,Zhong Y,Wang Y

更新日期：2018-06-25 00:00:00

abstract：:Inflammation comprises the reaction of the body to injury, in which a series of changes of the terminal vascular bed, blood, and connective tissue tends to eliminate the injurious agent and to repair the damaged tissue. It is a complex process, which involves the release of diverse regulatory mediators. The current an...

journal_title：European journal of medicinal chemistry

authors： Khan H,Rengasamy KRR,Pervaiz A,Nabavi SM,Atanasov AG,Kamal MA

更新日期：2018-06-10 00:00:00