abstract：:On the basis of previous reports on the importance of thienyl, furyl or phenol group substitution on 5H-indeno[1,2-b]pyridine skeleton, a new series of rigid 2-aryl-4-(4'-hydroxyphenyl)-5H-indeno[1,2-b]pyridine derivatives were systematically designed and synthesized. Topoisomerase inhibitory activity and antiprolifer...

journal_title：European journal of medicinal chemistry

authors： Park S,Kadayat TM,Jun KY,Thapa Magar TB,Bist G,Shrestha A,Lee ES,Kwon Y

更新日期：2017-01-05 00:00:00

abstract：:Acute lung injury (ALI) is a major cause of acute respiratory failure in critically-ill patients. Resveratrol and curcumin are proven to have potent anti-inflammatory efficacy, but their clinical application is limited by their metabolic instability. Here, a series of resveratrol and the Mono-carbonyl analogs of curcu...

journal_title：European journal of medicinal chemistry

authors： Pan J,Xu T,Xu F,Zhang Y,Liu Z,Chen W,Fu W,Dai Y,Zhao Y,Feng J,Liang G

更新日期：2017-01-05 00:00:00

abstract：:A new series of pyrazolo[3,4-d]pyridazin-7-one derivatives were synthesised and evaluated for their in vitro antileishmanial activity against Leishmania amazonensis promastigote and axenic amastigote forms. The results showed that the pyrazolo[3,4-d]-pyridazin-7-one-N-acylhydrazone-(bi)thiophene hybrids 5b, 6b and 6d ...

journal_title：European journal of medicinal chemistry

authors： Jacomini AP,Silva MJV,Silva RGM,Gonçalves DS,Volpato H,Basso EA,Paula FR,Nakamura CV,Sarragiotto MH,Rosa FA

更新日期：2016-11-29 00:00:00

abstract：:A series of novel hybrids β-carboline-4-thiazolidinones were synthesized and evaluated for their in vitro antitumor activity against human cancer cell lines and for antiviral activity towards Herpes simplex virus type-1 (HSV-1). From the N'-(2-ylidene-4-thiazolidinone)-β-carboline-3-carbohydrazide series (9-11), compo...

journal_title：European journal of medicinal chemistry

authors： Barbosa VA,Baréa P,Mazia RS,Ueda-Nakamura T,Costa WFD,Foglio MA,Goes Ruiz ALT,Carvalho JE,Vendramini-Costa DB,Nakamura CV,Sarragiotto MH

更新日期：2016-11-29 00:00:00

abstract：:Modifications to an N-methyl-(quinolin-4-yl)oxypropanamide scaffold were explored to discover leads for developing new radioligands for PET imaging of brain TSPO (translocator protein), a biomarker of neuroinflammation. Whereas contraction of the quinolinyl portion of the scaffold or cyclization of the tertiary amido ...

journal_title：European journal of medicinal chemistry

authors： Brouwer C,Jenko KJ,Zoghbi SS,Morse CL,Innis RB,Pike VW

更新日期：2016-11-29 00:00:00

abstract：:A series of peptidomimetic aldehydes were designed, synthesized, and evaluated for their biochemical activity against 3C protease (3Cpro) and anti-enterovirus 71 (EV71) activity in vitro. Molecular docking revealed that 5s (IC50 = 0.22 ± 0.07 μM, EC50 = 0.18 ± 0.05 μM) could bind well to the active site of EV71 3Cpro,...

journal_title：European journal of medicinal chemistry

authors： Zhai Y,Ma Y,Ma F,Nie Q,Ren X,Wang Y,Shang L,Yin Z

更新日期：2016-11-29 00:00:00

abstract：:Xanthine oxidase (XO) is the key enzyme in humans which is related to a variety of diseases such as gout, hyperuricemia and cardiovascular diseases. In this work, a series of 2-arylbenzo[b]furan derivatives were synthesized based on salvianolic acid C, and they were evaluated for xanthine oxidase inhibitory and antiox...

journal_title：European journal of medicinal chemistry

authors： Tang HJ,Zhang XW,Yang L,Li W,Li JH,Wang JX,Chen J

更新日期：2016-11-29 00:00:00

abstract：:The 4-substituted 1,2,3-triazole core in designed coumarin hybrids (4-35) with diverse physicochemical properties was introduced by eco-friendly copper(I)-catalyzed Huisgen 1,3-dipolar cycloaddition under microwave irradiation. Coumarin-1,2,3-triazole-benzofused heterocycle hybrids emerged as the class of compounds ex...

journal_title：European journal of medicinal chemistry

authors： Kraljević TG,Harej A,Sedić M,Pavelić SK,Stepanić V,Drenjančević D,Talapko J,Raić-Malić S

更新日期：2016-11-29 00:00:00

abstract：:Eukaryotic translation initiation factor 4E (eIF4E) is considered as the corner stone in the cap-dependent translation initiation machinery. Its role is to recruit mRNA to the ribosome through recognition of the 5'-terminal mRNA cap structure (m7GpppN, where G is guanosine, N is any nucleotide). eIF4E is implicated in...

journal_title：European journal of medicinal chemistry

authors： Soukarieh F,Nowicki MW,Bastide A,Pöyry T,Jones C,Dudek K,Patwardhan G,Meullenet F,Oldham NJ,Walkinshaw MD,Willis AE,Fischer PM

更新日期：2016-11-29 00:00:00

abstract：:Herein we report the design, synthesis, bioinformatic and biological studies of benzimidazole and benzothiophene derivatives as new cannabinoid receptor ligands. To test the hypothesis that the lack of a hydrogen bond interaction between benzimidazole and benzothiophene derivatives with Lys192 reduces their affinity f...

journal_title：European journal of medicinal chemistry

authors： Romero-Parra J,Mella-Raipán J,Palmieri V,Allarà M,Torres MJ,Pessoa-Mahana H,Iturriaga-Vásquez P,Escobar R,Faúndez M,Di Marzo V,Pessoa-Mahana CD

更新日期：2016-11-29 00:00:00

abstract：:Trichomoniasis is the most prevalent, non-viral sexually transmitted diseases (STD) caused by amitochondriate protozoan Trichomonas vaginalis. Increased resistance of T. vaginalis to the marketed drug Metronidazole necessitates the development of newer chemical entities. A library of sixty 2-methyl-4/5-nitroimidazole ...

journal_title：European journal of medicinal chemistry

authors： Mandalapu D,Kushwaha B,Gupta S,Singh N,Shukla M,Kumar J,Tanpula DK,Sankhwar SN,Maikhuri JP,Siddiqi MI,Lal J,Gupta G,Sharma VL

更新日期：2016-11-29 00:00:00

abstract：:Among the different classes of antibiotics, oxazolidinone derivatives represent important drugs, since their unique mechanism of action overcomes commonly diffused multidrug-resistant bacteria. Anyway, the structural similarity of these molecules to monoamino oxidase (MAO) inhibitors, like toloxatone and blefoxatone, ...

journal_title：European journal of medicinal chemistry

authors： Ferrazzano L,Viola A,Lonati E,Bulbarelli A,Musumeci R,Cocuzza C,Lombardo M,Tolomelli A

更新日期：2016-11-29 00:00:00

abstract：:Calixarene-based compounds are highly effective therapeutic agents against cancer. This study aims to prepare a series of calix [n]arene (n = 4, 6, 8) polyhydroxyamine derivatives (3a-3m) and to study their potential antitumor activities. The single crystal structure of calixs[4]arene derivative 3a was determined thro...

journal_title：European journal of medicinal chemistry

authors： An L,Han LL,Zheng YG,Peng XN,Xue YS,Gu XK,Sun J,Yan CG

更新日期：2016-11-10 00:00:00

abstract：:β-Ionone is an end-ring analog of β-carotenoids which widely distributed in fruit and vegetables. Recent studies have demonstrated anti-proliferative, anti-metastatic and apoptosis induction properties of β-ionone in vitro and in vivo. Also, the studies have focused on investigating the β-ionone action on different ty...

journal_title：European journal of medicinal chemistry

authors： Ansari M,Emami S

更新日期：2016-11-10 00:00:00

abstract：:In this work, 27 novel hybrid derivatives containing diverse substituents with chalcogen atoms (selenium or sulfur) and several active heterocyclic scaffolds have been synthesized. Compounds were tested against two human cancer cells lines (MCF7 and PC-3) and a normal human mammary epithelial cell line (184B5) in orde...

journal_title：European journal of medicinal chemistry

authors： Alcolea V,Plano D,Encío I,Palop JA,Sharma AK,Sanmartín C

更新日期：2016-11-10 00:00:00

abstract：:Approaches of targeting excessive activation and differentiation of osteoclasts were considered as an effective treatment option for osteoporosis or osteopenia. In the present work, a series of rhein derivatives were synthesized and employed for their cytotoxicity screening against bone marrow-derived macrophages cell...

journal_title：European journal of medicinal chemistry

authors： Xu X,Qi X,Yan Y,Qi J,Qian N,Guo L,Li C,Wang F,Huang P,Zhou H,Jiang M,Yang C,Deng L

更新日期：2016-11-10 00:00:00

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

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

abstract：:Oxindole has emerged as a valuable scaffold in medicinal chemistry possessing diverse range of pharmacological activities. Its value has further been increased by its natural occurrence as alkaloids in variety of plants. It was first extracted from the cat claw's plant Uncaria tomentosa found in the Amazon rainforest ...

journal_title：European journal of medicinal chemistry

authors： Kaur M,Singh M,Chadha N,Silakari O

更新日期：2016-11-10 00:00:00

abstract：:Topoisomerase II poison blocks the transitorily generated DNA double-strand breaks (DSBs) from religation, thereby causes severe DNA damage and gene toxicity. While topoisomerase II catalytic inhibitor does not form cleavable DNA-enzyme complex because its function attributes to inhibition of the catalytic steps of th...

journal_title：European journal of medicinal chemistry

authors： Park S,Hong E,Kwak SY,Jun KY,Lee ES,Kwon Y,Na Y

更新日期：2016-11-10 00:00:00

abstract：:A possible ability of twelve new derivatives of known antioxidants trolox (TroH), trolox succinate (TroS), α-tocopheryl succinate (α-TOS) containing nitroxyl radicals (1-12) to protect bacterial cells from spontaneous and peroxide-induced mutagenesis and their cytotoxicity against six different tumor cells as well as ...

journal_title：European journal of medicinal chemistry

authors： Zakharova OD,Frolova TS,Yushkova YV,Chernyak EI,Pokrovsky AG,Pokrovsky MA,Morozov SV,Sinitsina OI,Grigor'ev IA,Nevinsky GA

更新日期：2016-10-21 00:00:00

abstract：:A new series of 2-substituted imino-3-substituted-5- heteroarylidene-1,3-thiazolidine-4-ones as the potent bidentate PTP1B inhibitors were designed and synthesized in this paper. All of the new compounds were characterized and identified by spectra analysis. The biological screening test against PTP1B showed that some...

journal_title：European journal of medicinal chemistry

authors： Meng G,Zheng M,Wang M,Tong J,Ge W,Zhang J,Zheng A,Li J,Gao L,Li J

更新日期：2016-10-21 00:00:00

abstract：:A series of new imidazolidineiminothione derivatives with various halogenated and alkylated aromatic substituents at N-(1) and at N-(3) was synthesized through the reaction of N-arylcyanothioformamides with arylisocyanate derivatives. Structure of imidazolidineiminothione derivatives were established based on spectros...

journal_title：European journal of medicinal chemistry

authors： Moussa Z,El-Sharief MAMS,Abbas SY

更新日期：2016-10-21 00:00:00

abstract：:In an attempt to improve the efficacy and stability of current, clinically used artemisinins, a series non-hemiacetal ester derivatives of artemisinin were synthesized and evaluated for their in vitro antiplasmodial and anticancer activities as well as cytotoxicities. These esters were synthesized through the reaction...

journal_title：European journal of medicinal chemistry

authors： Zuma NH,Smit FJ,de Kock C,Combrinck J,Smith PJ,N'Da DD

更新日期：2016-10-21 00:00:00

abstract：:A new series of 4-dimethylamine flavonoid derivatives were designed and synthesized as potential multifunctional anti-Alzheimer agents. The inhibition of cholinesterase activity, self-induced β-amyloid (Aβ) aggregation, and antioxidant activity by these derivatives was investigated. Most of the compounds exhibited pot...

journal_title：European journal of medicinal chemistry

authors： Luo W,Wang T,Hong C,Yang YC,Chen Y,Cen J,Xie SQ,Wang CJ

更新日期：2016-10-21 00:00:00

abstract：:The design and synthesis of a novel bis-furan scaffold tailored for high efficiency at inhibiting transthyretin amyloid formation is reported. In vitro results show that the discovered compounds are more efficient inhibitors of amyloid formation than tafamidis, a drug currently used in the treatment of familial amyloi...

journal_title：European journal of medicinal chemistry

authors： Simões CJV,Almeida ZL,Costa D,Jesus CSH,Cardoso AL,Almeida MR,Saraiva MJ,Pinho E Melo TMVD,Brito RMM

更新日期：2016-10-04 00:00:00

abstract：:Modified purine derivatives exemplified by pyrazolopyrimidines have emerged as highly selective inhibitors of several angiogenic receptor tyrosine kinases. Herein, we designed and synthesized a new series of substituted pyrazolopyridines and explored their ability to influence crucial pro-angiogenic attributes of endo...

journal_title：European journal of medicinal chemistry

authors： Michailidou M,Giannouli V,Kotsikoris V,Papadodima O,Kontogianni G,Kostakis IK,Lougiakis N,Chatziioannou A,Kolisis FN,Marakos P,Pouli N,Loutrari H

更新日期：2016-10-04 00:00:00

abstract：:Currently available drugs against Alzheimer's disease (AD) are only able to ameliorate the disease symptoms resulting in a moderate improvement in memory and cognitive function without any efficacy in preventing and inhibiting the progression of the pathology. In an effort to obtain disease-modifying anti-Alzheimer's ...

journal_title：European journal of medicinal chemistry

authors： Wu MY,Esteban G,Brogi S,Shionoya M,Wang L,Campiani G,Unzeta M,Inokuchi T,Butini S,Marco-Contelles J

更新日期：2016-10-04 00:00:00

abstract：:Four mexiletine analogues have been tested for their antiarrhythmic, inotropic, and chronotropic effects on isolated guinea pig heart tissues and to assess calcium antagonist activity, in comparison with the parent compound mexiletine. All analogues showed from moderate to high antiarrhythmic activity. In particular, ...

journal_title：European journal of medicinal chemistry

authors： Roselli M,Carocci A,Budriesi R,Micucci M,Toma M,Di Cesare Mannelli L,Lovece A,Catalano A,Cavalluzzi MM,Bruno C,De Palma A,Contino M,Perrone MG,Colabufo NA,Chiarini A,Franchini C,Ghelardini C,Habtemariam S,Lentini G

更新日期：2016-10-04 00:00:00

abstract：:A number of N-(2-(1H-indol-3-yl)ethyl)-2-oxo-2H-chromene-3-carboxamides were synthesized and tested against AChE and BuChE. The in vitro assessment of the synthesized compounds 4a-o revealed that most of them had significant activity toward AChE. The SAR study demonstrated that the introduction of benzyloxy moiety on ...

journal_title：European journal of medicinal chemistry

authors： Ghanei-Nasab S,Khoobi M,Hadizadeh F,Marjani A,Moradi A,Nadri H,Emami S,Foroumadi A,Shafiee A

更新日期：2016-10-04 00:00:00

abstract：:A series of chalcone derivatives were synthesized and evaluated for their μ-calpain and cathepsin B inhibitory activities. Among the tested chalcone derivatives, two compounds, 7 and 11, showed potent inhibitory activities against μ-calpain and cathepsin B and were selected for further evaluation. Compounds 7 and 11 s...

journal_title：European journal of medicinal chemistry

authors： Jeon KH,Lee E,Jun KY,Eom JE,Kwak SY,Na Y,Kwon Y

更新日期：2016-10-04 00:00:00

abstract：:We report a convenient synthesis of carbazole-1,4-quinone alkaloid koeniginequinones A and B using a tandem ring-closing metathesis with the dehydrogenation reaction sequence under an O2 atmosphere as an important step. Using this method, carbazole-1,4-quinones substituted at the 5-, 6-, 7-, and/or 8-positions have be...

journal_title：European journal of medicinal chemistry

authors： Nishiyama T,Hatae N,Yoshimura T,Takaki S,Abe T,Ishikura M,Hibino S,Choshi T

更新日期：2016-10-04 00:00:00

abstract：:Plants of the Amaryllidaceae family produce a large variety of alkaloids and non-basic secondary metabolites, many of which are investigated for their promising anticancer activities. Of these, crinine-type alkaloids based on the 5,10b-ethanophenanthridine ring system were recently shown to be effective at inhibiting ...

journal_title：European journal of medicinal chemistry

authors： Henry S,Kidner R,Reisenauer MR,Magedov IV,Kiss R,Mathieu V,Lefranc F,Dasari R,Evidente A,Yu X,Ma X,Pertsemlidis A,Cencic R,Pelletier J,Cavazos DA,Brenner AJ,Aksenov AV,Rogelj S,Kornienko A,Frolova LV

更新日期：2016-09-14 00:00:00

abstract：:Fms-like tyrosine kinase 3 (FLT3) is a well-known and important target for the treatment of acute myeloid leukemia (AML). A series of thieno[2,3-d]pyrimidine derivatives from a modification at the 6-position were synthesized to identify effective FLT3 inhibitors. Although compounds 1 and 2 emerged as promising FLT3 in...

journal_title：European journal of medicinal chemistry

authors： Kim H,Lee C,Yang JS,Choi S,Park CH,Kang JS,Oh SJ,Yun J,Kim MH,Han G

更新日期：2016-09-14 00:00:00

abstract：:Development of novel anticancer drugs is inevitable to improve treatment of cancers. In this study, novel derivatives of indoline and morpholine were synthesized and tested for their cytotoxic effects on osteosarcoma and Human Embryonic Kidney cells. To characterize cytotoxicity and the mechanism of cell death, we use...

journal_title：European journal of medicinal chemistry

authors： Doan P,Karjalainen A,Chandraseelan JG,Sandberg O,Yli-Harja O,Rosholm T,Franzen R,Candeias NR,Kandhavelu M

更新日期：2016-09-14 00:00:00

abstract：:Steroid sulfatase (STS), the enzyme which converts inactive sulfated steroid precursors into active hormones, is a promising therapeutic target for the treatment of estrogen-sensitive breast cancer. We report herein the synthesis and in vitro study of dual-action STS inhibitors with selective estrogen-receptor modulat...

journal_title：European journal of medicinal chemistry

authors： Ouellet C,Maltais R,Ouellet É,Barbeau X,Lagüe P,Poirier D

更新日期：2016-08-25 00:00:00

abstract：:Protein tyrosine phosphatase 1B (PTP1B) as a key negative regulator of both insulin and leptin receptor pathways has been an attractive therapeutic target for the treatment of type 2 diabetes mellitus (T2DM) and obesity. With the goal of enhancing potency and selectivity of the PTP1B inhibitors, a series of methyl sal...

journal_title：European journal of medicinal chemistry

authors： Liu P,Du Y,Song L,Shen J,Li Q

更新日期：2016-08-08 00:00:00

abstract：:Adipose Triglyceride Lipase (ATGL) performs the first and rate-limiting step in lipolysis by hydrolyzing triacylglycerols stored in lipid droplets to diacylglycerols. By mediating lipolysis in adipose and non-adipose tissues, ATGL is a major regulator of overall energy metabolism and plasma lipid levels. Since chronic...

journal_title：European journal of medicinal chemistry

authors： Roy PP,D'Souza K,Cuperlovic-Culf M,Kienesberger PC,Touaibia M

更新日期：2016-08-08 00:00:00

abstract：:5-(1-Methyl-4-phenyl-imidazol-5-yl)indoles 5 were prepared and tested as analogs of the natural vascular-disrupting agent combretastatin A-4 (CA-4). The 3-bromo-4,5-dimethoxyphenyl derivative 5c was far more active than CA-4 with low nanomolar IC50 concentrations against multidrug-resistant KB-V1/Vbl cervix and MCF-7/...

journal_title：European journal of medicinal chemistry

authors： Mahal K,Biersack B,Schruefer S,Resch M,Ficner R,Schobert R,Mueller T

更新日期：2016-08-08 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：:Pursuing our recent outcomes regarding the antifungal activity of N-substituted 1,3-thiazolidin-4-ones, we synthesized thirty-six new derivatives introducing aliphatic, cycloaliphatic and heteroaromatic moieties at N1-hydrazine connected with C2 position of the thiazolidinone nucleus and functionalizing the lactam nit...

journal_title：European journal of medicinal chemistry

authors： Secci D,Carradori S,Bizzarri B,Chimenti P,De Monte C,Mollica A,Rivanera D,Zicari A,Mari E,Zengin G,Aktumsek A

更新日期：2016-07-19 00:00:00