Differentiating Antiproliferative and Chemopreventive Modes of Activity for Electron-Deficient Aryl Isothiocyanates against Human MCF-7 Cells.

abstract：:β-Lactamases (BLs) are important antibiotic-resistance determinants that significantly compromise the efficacy of valuable β-lactam antibacterial drugs. Thus, combinations with BL inhibitor were developed. Avibactam is the first non-β-lactam BL inhibitor introduced into clinical practice. Ceftazidime-avibactam represe...

journal_title：ChemMedChem

authors： Pozzi C,Di Pisa F,De Luca F,Benvenuti M,Docquier JD,Mangani S

更新日期：2018-07-18 00:00:00

abstract：:Plasmodium parasites kill 435 000 people around the world every year due to unavailable vaccines, a limited arsenal of antimalarial drugs, delayed treatment, and the reduced clinical effectiveness of current practices caused by drug resistance. Therefore, there is an urgent need to discover and develop new antiplasmod...

journal_title：ChemMedChem

authors： de Souza Pereira C,Costa Quadros H,Magalhaes Moreira DR,Castro W,Santos De Deus Da Silva RI,Botelho Pereira Soares M,Fontinha D,Prudêncio M,Schmitz V,Dos Santos HF,Gendrot M,Fonta I,Mosnier J,Pradines B,Navarro M

更新日期：2020-11-24 00:00:00

abstract：:Compound 11 (3-(benzyloxy)-1'-methyl-1'-azonia-4H-1'-azaspiro[isoxazole-5,3'-bicyclo[2.2.2]octane] iodide) was selected from a previous set of nicotinic ligands as a suitable model compound for the design of new silent agonists of α7 nicotinic acetylcholine receptors (nAChRs). Silent agonists evoke little or no channe...

journal_title：ChemMedChem

authors： Quadri M,Matera C,Silnović A,Pismataro MC,Horenstein NA,Stokes C,Papke RL,Dallanoce C

更新日期：2017-08-22 00:00:00

abstract：:PH-797804 ((aS)-3-{3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl}-N,4-dimethylbenzamde) is a diarylpyridinone inhibitor of p38 mitogen-activated protein (MAP) kinase derived from a racemic mixture as the more potent atropisomer (aS), first proposed by molecular modeling and subsequently confirmed ...

journal_title：ChemMedChem

authors： Xing L,Devadas B,Devraj RV,Selness SR,Shieh H,Walker JK,Mao M,Messing D,Samas B,Yang JZ,Anderson GD,Webb EG,Monahan JB

更新日期：2012-02-06 00:00:00

abstract：:The first series of 2'-substituted 2-(3'-carboxybicyclo[1.1.1]pentyl)glycine derivatives, (2R)- and (2S)-(2',2'-dichloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (10) and (11), and 2-(2'-chloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (12) were synthesized and evaluated as mGluR ligands. Compounds 11 and 12 were shown to ...

journal_title：ChemMedChem

authors： Pellicciari R,Filosa R,Fulco MC,Marinozzi M,Macchiarulo A,Novak C,Natalini B,Hermit MB,Nielsen S,Sager TN,Stensbøl TB,Thomsen C

更新日期：2006-03-01 00:00:00

abstract：:In atomic force microscopy (AFM) a sharp cantilever tip is used to scan surfaces at the atomic level. One further application is force spectroscopy, in which force-distance curves between binding partners located on the cantilever and substrate surface are determined. This requires specifically immobilized molecules. ...

journal_title：ChemMedChem

authors： David R,Erdmann M,Fornof AR,Gaub HE

更新日期：2014-09-01 00:00:00

abstract：:Although the advantages of sp3 -rich, sterically complicated molecules in drug development have been pointed out, modern screening libraries are filled with planar, sp2 -rich components. Compounds that are sp3 -rich are difficult to synthesize, and thus we aimed to invent an efficient method to construct sp3 -rich lib...

journal_title：ChemMedChem

authors： Karaki F,Umemoto S,Ashizawa K,Oki T,Sato N,Ogino T,Ishibashi N,Someya R,Miyano K,Hirayama S,Uezono Y,Fujii H

更新日期：2019-11-06 00:00:00

abstract：:Octa-O-bis-(R,R)-Tartarate Ditellurane (SAS) is a new Te(IV) compound, comprised of two tellurium atoms, each liganded by four oxygen atoms from two carboxylates and two alkoxides of two tartaric acids. Unlike many other Te(IV) compounds, SAS was highly stable in aqueous solution. It interacted with thiols to form an ...

journal_title：ChemMedChem

authors： Yosef S,Brodsky M,Sredni B,Albeck A,Albeck M

更新日期：2007-11-01 00:00:00

abstract：:A small library of 17 organoruthenium compounds with the general formula [RuII (fcl)(chel)(L)]n+ (in which fcl=face capping ligand, chel=chelating bidentate ligand, and L=monodentate ligand) were screened for inhibitory activity against cholinesterases and glutathione-S-transferases of human and animal origins. Compou...

journal_title：ChemMedChem

authors： Ristovski S,Uzelac M,Kljun J,Lipec T,Uršič M,Zemljič Jokhadar Š,Žužek MC,Trobec T,Frangež R,Sepčić K,Turel I

更新日期：2018-10-22 00:00:00

abstract：:The synthesis of a novel group of quinacridine-based ligands (MMQs) is described along with an evaluation of their G-quadruplex binding properties. A set of biophysical assays was applied to characterize their interaction with DNA quadruplexes: FRET-melting experiments and equilibrium microdialysis were used to evalua...

journal_title：ChemMedChem

authors： Hounsou C,Guittat L,Monchaud D,Jourdan M,Saettel N,Mergny JL,Teulade-Fichou MP

更新日期：2007-05-01 00:00:00

abstract：:S100B contributes to cell proliferation by binding the C terminus of p53 and inhibiting its tumor suppressor function. The use of multiple computational approaches to screen fragment libraries targeting the human S100B-p53 interaction site is reported. This in silico screening led to the identification of 280 novel pr...

journal_title：ChemMedChem

authors： Agamennone M,Cesari L,Lalli D,Turlizzi E,Del Conte R,Turano P,Mangani S,Padova A

更新日期：2010-03-01 00:00:00

abstract：:Greater than the sum of its parts: Artemisinins are currently in phase I-II clinical trials against breast, colorectal and non-small-cell lung cancers. In an attempt to offer increased specificity, a series of hybrid artemisinin-polypyrrole minor groove binder conjugates are described. DNA binding/modelling studies an...

journal_title：ChemMedChem

authors： La Pensée L,Sabbani S,Sharma R,Bhamra I,Shore E,Chadwick AE,Berry NG,Firman J,Araujo NC,Cabral L,Cristiano ML,Bateman C,Janneh O,Gavrila A,Wu YH,Hussain A,Ward SA,Stocks PA,Cosstick R,O'Neill PM

更新日期：2013-05-01 00:00:00

abstract：:Three photoswitchable tetrapeptides, based on a known synthetic antibacterial, were designed and synthesized to determine activity against Staphylococcus aureus. Each peptide contains an azobenzene photoswitch incorporated into either the N-terminal side chain (1), C-terminal side chain (2), or the C-terminus (3) to a...

journal_title：ChemMedChem

authors： Yeoh YQ,Horsley JR,Yu J,Polyak SW,Jovcevski B,Abell AD

更新日期：2020-08-19 00:00:00

abstract：:A series of new substituted 7-phenyl-3H-pyrrolo[3,2-f]quinolin-9-ones were synthesized and evaluated for their antiproliferative activity. The most active derivatives showed high selectivity against human leukemia cell lines and potently inhibited their growth, with GI(50) values in the nanomolar range. The active com...

journal_title：ChemMedChem

authors： Ferlin MG,Bortolozzi R,Brun P,Castagliuolo I,Hamel E,Basso G,Viola G

更新日期：2010-08-02 00:00:00

abstract：:The in silico design, synthesis, and biological evaluation of ten potent type II dehydroquinase inhibitors are described. These compounds contain an anhydroquinate core, incorporated as a mimic of the enolate reaction intermediate. This substructure is attached by a variety of linking units to a terminal phenyl group ...

journal_title：ChemMedChem

authors： Payne RJ,Peyrot F,Kerbarh O,Abell AD,Abell C

更新日期：2007-07-01 00:00:00

abstract：:Two libraries, each consisting of 48 16beta-aminopropyl estradiol derivatives, phenols and sulfamates, respectively, were synthesized by solid-phase parallel chemistry through a seven-step reaction sequence. Following the attachment of a C18-steroid sulfamate precursor on a trityl chloride resin, diversity elements we...

journal_title：ChemMedChem

authors： Ciobanu LC,Poirier D

更新日期：2006-11-01 00:00:00

abstract：:Polo-like kinase 1 (PLK1) plays crucial functions in multiple stages of mitosis and is considered to be a potential drug target for cancer therapy. The functions of PLK1 are mediated by its N-terminal kinase domain and C-terminal polo-box domain (PBD). Most inhibitors targeting the kinase domain of PLK1 have a selecti...

journal_title：ChemMedChem

authors： Shan HM,Shi Y,Quan J

更新日期：2015-01-01 00:00:00

abstract：:Some hybrid foldamers of various length, all containing the (4R,5S)-4-carboxy-5-methyloxazolidin-2-one (d-Oxd) moiety alternating with an l-amino acid (l-Val, l-Lys, or l-Ala), were prepared in order to study their preferred conformations and to evaluate their biological activity. Surprisingly, only the longer oligome...

journal_title：ChemMedChem

authors： Del Secco B,Malachin G,Milli L,Zanna N,Papini E,Cornia A,Tavano R,Tomasini C

更新日期：2017-02-20 00:00:00

abstract：:Iron is essential for the pathogenicity and virulence of Mycobacterium tuberculosis, which synthesises salicyl-capped siderophores (mycobactins) to acquire this element from the host. MbtA is the adenylating enzyme that catalyses the initial reaction of mycobactin biosynthesis and is solely expressed by mycobacteria. ...

journal_title：ChemMedChem

authors： Ferguson L,Wells G,Bhakta S,Johnson J,Guzman J,Parish T,Prentice RA,Brucoli F

更新日期：2019-10-04 00:00:00

abstract：:Discovered as a modulator of the toxic response to environmental pollutants, aryl hydrocarbon receptor (AhR) has recently gained attention for its involvement in various physiological and pathological pathways. AhR is a ligand-dependent transcription factor activated by a large array of chemical compounds, which inclu...

journal_title：ChemMedChem

authors： Dolciami D,Gargaro M,Cerra B,Scalisi G,Bagnoli L,Servillo G,Fazia MAD,Puccetti P,Quintana FJ,Fallarino F,Macchiarulo A

更新日期：2018-02-06 00:00:00

abstract：:N-Acylethanolamine acid amidase (NAAA) is a cysteine hydrolase that catalyzes the hydrolysis of endogenous lipid mediators such as palmitoylethanolamide (PEA). PEA has been shown to exert anti-inflammatory and antinociceptive effects in animals by engaging peroxisome proliferator-activated receptor α (PPAR-α). Thus, p...

journal_title：ChemMedChem

authors： Fiasella A,Nuzzi A,Summa M,Armirotti A,Tarozzo G,Tarzia G,Mor M,Bertozzi F,Bandiera T,Piomelli D

更新日期：2014-07-01 00:00:00

abstract：:Disulfide bridges that stabilize the native conformation of conotoxins pose a challenge in the synthesis of smaller conotoxin analogues. Herein we describe the synthesis of a minimized analogue of the analgesic mu-conotoxin KIIIA that blocks two sodium channel subtypes, the neuronal Na(V)1.2 and skeletal muscle Na(V)1...

journal_title：ChemMedChem

authors： Han TS,Zhang MM,Walewska A,Gruszczynski P,Robertson CR,Cheatham TE 3rd,Yoshikami D,Olivera BM,Bulaj G

更新日期：2009-03-01 00:00:00

abstract：:Herbal medicines (HMs) are an important source of drugs. In this study, an efficient strategy integrating ultrafiltration LC-MS, microplate bioassays, and molecular docking was proposed to screen high-potency enzyme inhibitors from HMs. Using this strategy, the structure-activity relationships (SARs) including binding...

journal_title：ChemMedChem

authors： Song HP,Wang H,Liang JX,Qian C,Wu SQ,Xu WJ,Wu B,Liu XG,Li P,Yang H

更新日期：2016-12-06 00:00:00

abstract：:Using the original approach, a series of metallated N-confused porphyrins and metallated porphyrins have been synthesized and characterized. For all the synthesized porphyrins, in vitro studies of cytotoxic activity against K562, U937, HL-60, Jurkat, A549 and HeLa cancer cell lines, the ability to induce apoptosis and...

journal_title：ChemMedChem

authors： Halder N,Dzhemileva LU,Ramazanov IR,D'yakonov VA,Dzhemilev UM,Rath H

更新日期：2020-04-03 00:00:00

abstract：:Loperamide (1a), an opioid receptor agonist, is in clinical use as an antidiarrheal agent. Carbon/silicon exchange (sila-substitution) at the 4-position of the piperidine ring of 1a (R3 COH→R3 SiOH) leads to sila-loperamide (1b). Sila-loperamide was synthesized in a multistep procedure, starting from triethoxyvinylsil...

journal_title：ChemMedChem

authors： Geyer M,Wellner E,Jurva U,Saloman S,Armstrong D,Tacke R

更新日期：2015-05-01 00:00:00

abstract：:Given the number of monogenic ocular diseases and the number of non-monogenic degenerative ocular diseases for which gene therapy is considered as a treatment, the development of effective therapeutic delivery strategies for DNA is a critical research goal. In this work, nonviral nanoparticles (NPs) composed of glycol...

journal_title：ChemMedChem

authors： Mitra RN,Han Z,Merwin M,Al Taai M,Conley SM,Naash MI

更新日期：2014-01-01 00:00:00

abstract：:A novel and facile synthesis of quinoxalinone derivatives was developed in which a wide range of 3-chloroquinoxalin-2(1H)-ones as key intermediates can be generated chemo- and regioselectively in good yields from corresponding quinoxaline-2,3(1H,4H)-diones. This new protocol is arguably superior, as it allows the desi...

journal_title：ChemMedChem

authors： Yang Y,Zhang S,Wu B,Ma M,Chen X,Qin X,He M,Hussain S,Jing C,Ma B,Zhu C

更新日期：2012-05-01 00:00:00

abstract：:Intraoperative imaging technologies recently entered the operating room, and their implementation is revolutionizing how physicians plan, monitor, and perform surgical interventions. In this work, we present a novel surgical imaging reporter system: intraoperative chemiluminescence imaging (ICI). To this end, we have ...

journal_title：ChemMedChem

authors： Büchel GE,Carney B,Shaffer TM,Tang J,Austin C,Arora M,Zeglis BM,Grimm J,Eppinger J,Reiner T

更新日期：2016-09-20 00:00:00

abstract：:Targeting the biosynthetic pathway of neuroactive steroids with specific 18 kDa translocator protein (TSPO) ligands may be a viable therapeutic approach for a variety of neurodegenerative and neuropsychiatric diseases. However, the lack of correlation between binding affinity and in vitro steroidogenic efficacy has li...

journal_title：ChemMedChem

authors： Costa B,Taliani S,Da Pozzo E,Barresi E,Robello M,Cavallini C,Cosconati S,Da Settimo F,Novellino E,Martini C

更新日期：2017-08-22 00:00:00

abstract：:A severe limitation in cancer therapy is the often insufficient differentiation between malign and benign tissue using known chemotherapeutics. One approach to decrease side effects is antibody-directed enzyme prodrug therapy (ADEPT). We have developed new glycosidic prodrugs such as (-)-(1S)-26 b based on the antibio...

journal_title：ChemMedChem

authors： Tietze LF,von Hof JM,Krewer B,Müller M,Major F,Schuster HJ,Schuberth I,Alves F

更新日期：2008-12-01 00:00:00