Recent advances of analogues of curcumin for treatment of cancer.

abstract：:The conjugation of biologically active molecules is a powerful tool for drug discovery used to target a variety of multifunctional diseases including cancer. Conjugated drugs can provide combination therapies in a single multi-functional agent and, by doing so, be more specific and powerful than conventional classic t...

journal_title：European journal of medicinal chemistry

authors： А Zolottsev V,Latysheva АS,Pokrovsky VS,Khan II,Misharin AY

更新日期：2021-01-15 00:00:00

abstract：:In the present study a quantitative structure activity relationship (QSAR) analysis was applied to a series of 100 of 7- and 3-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine derivatives. The Chem-X (version 2000) software was used to develop 3D QSAR models. The steric and electrostatic interactions be...

journal_title：European journal of medicinal chemistry

authors： Atanasova M,Ilieva S,Galabov B

更新日期：2007-09-01 00:00:00

abstract：:Emulsions have shown great potential in the delivery of various types of cargoes such as nucleic acids and proteins. In this study, fluorinated polymer emulsions (PFx@PFD-n) were prepared using fluorinated polymers with different structures as surfactant in PFD emulsions under ultrasound. These polymer emulsions gave ...

journal_title：European journal of medicinal chemistry

authors： Xiao YP,Zhang J,Liu YH,Huang Z,Yu XQ

更新日期：2020-12-01 00:00:00

abstract：:Twenty 4-hydroxycoumarin derivatives were synthesized. Five of them are described for the first time. The X-ray crystal structure analysis of 3,3'-(2,3,4-trimethoxyphenylmethylene)bis-(4-hydroxy-2H-1-benzopyran-2-one) (7) and 3,3'-(3,5-dimethoxy-4-hydroxyphenylmethylene)bis-(4-hydroxy-2H-1-benzopyran-2-one) (9) confir...

journal_title：European journal of medicinal chemistry

authors： Manolov I,Maichle-Moessmer C,Danchev N

更新日期：2006-07-01 00:00:00

abstract：:The ruthenium DMSO complexes cis-Ru(II)C12(DMSO)4 and [(DMSO)2H][trans-Ru(III)Cl4(DMSO)2] reacted with 4-(3'-chloro-4'-fluoroanilino)-6-(2-(2-aminoethyl)aminoethoxy)-7-methoxyquinazoline (L1), 4-(3'-chloro-4'-fluoroanilino)-6-(2-(1H-imidazol-1-yl)ethoxy)-7-methoxy quinazoline (L2), N-(benzo[d]imidazol-4-yl)-6,7-dimeth...

journal_title：European journal of medicinal chemistry

authors： Ji L,Zheng W,Lin Y,Wang X,Lü S,Hao X,Luo Q,Li X,Yang L,Wang F

更新日期：2014-04-22 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：: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

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

abstract：:A series of novel 2-aminobenzamide derivatives decorated with thioquinazolinone were designed and synthesized as histone deacetylase (HDAC) inhibitors. These derivatives were evaluated for their antiproliferative activities against several human cancer cell lines including A375, Hela, A549, HCT116 and SMMC7721. It's s...

journal_title：European journal of medicinal chemistry

authors： Cheng C,Yun F,He J,Ullah S,Yuan Q

更新日期：2019-07-01 00:00:00

abstract：:Estradiol is the most potent estrogen in humans. It is known to be involved in the development and proliferation of estrogen dependent diseases such as breast cancer and endometriosis. The last step of its biosynthesis is catalyzed by 17β-hydroxysteroid dehydrogenase type 1 (17β- HSD1) which consequently is a promisin...

journal_title：European journal of medicinal chemistry

authors： Abdelsamie AS,Bey E,Hanke N,Empting M,Hartmann RW,Frotscher M

更新日期：2014-07-23 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：: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：:Many drugs are available for the treatment of systemic or superficial mycoses, but only a limited number of them are effective antifungal drugs, devoid of toxic and undesirable side effects. Furthermore, resistance development and fungistatic rather than fungicidal activities represent limitations of current antifunga...

journal_title：European journal of medicinal chemistry

authors： Di Marino S,Scrima M,Grimaldi M,D'Errico G,Vitiello G,Sanguinetti M,De Rosa M,Soriente A,Novellino E,D'Ursi AM

更新日期：2012-05-01 00:00:00

abstract：:Cancer has been the second heath killer being next only to cardiovascular diseases in human society. Although many efforts have been taken for cancer therapy and many achievements have been yielded in the diagnosis and treatment of cancer, the current first-line anti-cancer agents are insufficient owing to the emergen...

journal_title：European journal of medicinal chemistry

authors： Wan Y,Long J,Gao H,Tang Z

更新日期：2021-01-15 00:00:00

abstract：:A series of thirty two novel pyrrolo[2,3-b]pyridine analogues synthesized, characterized ((1)H NMR, (13)C NMR and MS) and cytotoxic evaluation of these molecules carried out over a panel of three human cancer cell lines including A549 (lung cancer), HeLa (cervical cancer) and MDA MB-231 (breast cancer), using sulforho...

journal_title：European journal of medicinal chemistry

authors： Narva S,Chitti S,Bala BR,Alvala M,Jain N,Kondapalli VG

更新日期：2016-05-23 00:00:00

abstract：:Non-steroidal anti-inflammatory drugs are widely used therapeutic agents in the treatment of inflammation, pain and fever. Cyclooxygenase catalyzes the initial step of biotransformation of arachidonic acid to prostanoids, and exist as three distinct isozymes; COX-I, COX-II and COX-III. Selective COX-II inhibitors are ...

journal_title：European journal of medicinal chemistry

authors： Dadiboyena S,Nefzi A

更新日期：2010-11-01 00:00:00

abstract：:A striking dual inhibition of enzymes α-glucosidase and butyrylcholinesterase by small drug-like molecules, including 1,4-disubstituted-1,2,3-triazoles, chalcones, and benzothiazepines, was rationalized with the help of Molecular Field Topology Analysis, a 3D QSAR technique similar to CoMFA. A common pharmacophore sup...

journal_title：European journal of medicinal chemistry

authors： Jabeen F,Oliferenko PV,Oliferenko AA,Pillai GG,Ansari FL,Hall CD,Katritzky AR

更新日期：2014-06-10 00:00:00

abstract：:We synthesized two mixed-ligand Cu(II) complexes containing different aroylhydrazone ligands and a pyridine co-ligand, namely, [Cu(L1)(Py)] (C1) and [Cu(L2)(Py)(Br)] (C2) (L1 = (E)-2-hydroxy-N'-((2-hydroxynaphthalen-1-yl)methylene)benzohydrazide, Py = pyridine, L2 = (E)-2-hydroxy-N'-(phenyl(pyridin-2-yl)methylene)benz...

journal_title：European journal of medicinal chemistry

authors： Gou Y,Li J,Fan B,Xu B,Zhou M,Yang F

更新日期：2017-07-07 00:00:00

abstract：:A new class of PDE4 inhibitors were designed and synthesized via the InCl3 mediated heteroarylation of indoles and their further derivatization through the Pd(II)-catalyzed CH activation strategy. This effort allowed us to discover a series of 2-(1H-indol-3-yl)-quinoxaline based inhibitors possessing PDE4B selectivity...

journal_title：European journal of medicinal chemistry

authors： Sunke R,Bankala R,Thirupataiah B,Ramarao EVVS,Kumar JS,Doss HM,Medishetti R,Kulkarni P,Kapavarapu RK,Rasool M,Mudgal J,Mathew JE,Shenoy GG,Parsa KVL,Pal M

更新日期：2019-07-15 00:00:00

abstract：:The activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6 kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most active compounds indica...

journal_title：European journal of medicinal chemistry

authors： Andreani A,Granaiola M,Leoni A,Locatelli A,Morigi R,Rambaldi M,Varoli L,Lannigan D,Smith J,Scudiero D,Kondapaka S,Shoemaker RH

更新日期：2011-09-01 00:00:00

abstract：:A series of 3- and 5-methylthiophene-2-carboxaldehyde alpha-(N)-heterocyclichydrazones were synthesized and submitted to an in vitro investigation of their anticancer, anti-HIV and antimicrobial activities. Some of the newly synthesized compounds were found to possess antiproliferative properties, whereas no anti-HIV ...

journal_title：European journal of medicinal chemistry

authors： Savini L,Chiasserini L,Travagli V,Pellerano C,Novellino E,Cosentino S,Pisano MB

更新日期：2004-02-01 00:00:00

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

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

更新日期：2018-01-20 00:00:00

abstract：:Most N,N-disubstituted 5-amino-N,N-diethyl-9-isopropyl [1,2,4]triazolo[4,3-a] [1,8]naphthyridine-6-carboxamides 9 (compounds 9a, c-i) and the N-monosubstituted one 8c were obtained by treating with excess amine the corresponding 5-chloroderivative 7a, which was in turn prepared by cyclocondensation of the 2,4-dichloro...

journal_title：European journal of medicinal chemistry

authors： Grossi G,Di Braccio M,Roma G,Ballabeni V,Tognolini M,Barocelli E

更新日期：2005-02-01 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：:Based on the co-crystal structures of LXRβ and its agonists (spiro [pyrrolidine-3,3'-oxindole] derivatives) discovered by us previously, we designed and synthesized a compound library to explore the agonistic activities. The library was screened with luciferase reporter assays, interestingly, it resulted in the discov...

journal_title：European journal of medicinal chemistry

authors： Chen Z,Chen H,Zhang Z,Ding P,Yan X,Li Y,Zhang S,Gu Q,Zhou H,Xu J

更新日期：2020-11-15 00:00:00

abstract：:We report herein the synthesis of 5-substituted [1]pyrindine derivatives and the evaluation of their antiproliferative properties on HeLa cells, a cervical carcinoma tumor cell line, and on the melanoma A2058 cell line. The most efficient compounds display cytotoxicity against tumor cells in the micromolar range but h...

journal_title：European journal of medicinal chemistry

authors： Kolb S,Goddard ML,Loukaci A,Mondésert O,Ducommun B,Braud E,Garbay C

更新日期：2010-03-01 00:00:00

abstract：:A series of sixteen novel thiazolidinone derivatives were synthesized from the efficient one-pot reaction of 2-(piperidin-1-yl)ethylamine, arenealdehydes and mercaptoacetic acid in good yields. Identification and characterization of products were achieved by NMR and GC-MS techniques. The in vitro antifungal activities...

journal_title：European journal of medicinal chemistry

authors： Kunzler A,Neuenfeldt PD,das Neves AM,Pereira CM,Marques GH,Nascente PS,Fernandes MH,Hübner SO,Cunico W

更新日期：2013-06-01 00:00:00

abstract：:A number of phenothiazine-, phenoxazine- and related tricyclics-derived chloroacetamides were synthesized and evaluated in vitro for antiprotozoal activities against Leishmania major (L. major) promastigotes. Several analogs were remarkably potent inhibitors, with antileishmanial activities being comparable or superio...

journal_title：European journal of medicinal chemistry

authors： Marcu A,Schurigt U,Müller K,Moll H,Krauth-Siegel RL,Prinz H

更新日期：2016-01-27 00:00:00

abstract：:Quinolones are widely used broad-spectrum antibacterials with incomplete elucidated mechanism of action. Here, molecular basis for the antibacterial action of quinolones, from target to network, is fully discussed and updated. Quinolones trap DNA gyrase or topoisomerase IV to form reversible drug-enzyme-DNA cleavage c...

journal_title：European journal of medicinal chemistry

authors： Cheng G,Hao H,Dai M,Liu Z,Yuan Z

更新日期：2013-08-01 00:00:00

abstract：:Boronic acid (and ester) prodrugs targeting the overexpressed level of reactive oxygen species within tumor microenvironment represent a promising area for the discovery of new selective anticancer chemotherapy. This strategy that emerged only ten years ago is exponentially growing and could demonstrate its clinical u...

journal_title：European journal of medicinal chemistry

authors： Maslah H,Skarbek C,Pethe S,Labruère R

更新日期：2020-12-01 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