Recent Advances in Synthetic α-Glucosidase Inhibitors.

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：:The natural product piperlonguminine (PL) has been shown to exert potential anticancer activity against several types of cancer via elevation of reactive oxidative species (ROS). However, the application of PL has been limited due to its poor water solubility and moderate activity. To improve PL's potency, we designed...

journal_title：ChemMedChem

authors： Wang X,Qian J,Zhu P,Hua R,Liu J,Hang J,Meng C,Shan W,Miao J,Ling Y

更新日期：2020-10-21 00:00:00

abstract：:Protein-protein interactions (PPIs) control many cellular processes in cancer and tumour growth. Of significant interest is the role PPIs play in regulating apoptosis. The overexpression of the antiapoptosis regulating Bcl-2 family of proteins is commonly observed in several cancers, leading to resistance towards both...

journal_title：ChemMedChem

authors： Beekman AM,O'Connell MA,Howell LA

更新日期：2016-04-19 00:00:00

abstract：:The NLRP3 inflammasome is an important regulator of the sterile inflammatory response, and its activation by host-derived sterile molecules leads to the intracellular activation of caspase-1, processing of the pro-inflammatory cytokines interleukin-1β (IL-1β)/IL-18, and pyroptotic cell death. Inappropriate activation ...

journal_title：ChemMedChem

authors： Baldwin AG,Tapia VS,Swanton T,White CS,Beswick JA,Brough D,Freeman S

更新日期：2018-02-20 00:00:00

abstract：:It has been 25 years since the development of the first efficient HIV-1/AIDS treatment. Scientists now know more about the HIV-1 infection life cycle, and more than 30 antiretroviral drugs have been developed, including HIV-1 fusion inhibitors. Fundamental work was begun in the early 1990s and led to the development o...

journal_title：ChemMedChem

authors： Cai L,Jiang S

更新日期：2010-11-08 00:00:00

abstract：:Protein disulfide isomerase (PDI) is overexpressed in glioblastoma, the most aggressive form of brain cancer, and folds nascent proteins responsible for the progression and spread of the disease. Herein we describe a novel nanomolar PDI inhibitor, pyrimidotriazinedione 35G8, that is toxic in a panel of human glioblast...

journal_title：ChemMedChem

authors： Kyani A,Tamura S,Yang S,Shergalis A,Samanta S,Kuang Y,Ljungman M,Neamati N

更新日期：2018-01-22 00:00:00

abstract：:Nucleoside analogues are extensively used as antiviral and anticancer agents. Their efficiency is dependent on their metabolism into the ultimately active nucleoside triphosphates. Often one step or even more in the metabolism of the nucleoside to the triphosphate is inefficient. To overcome this hurdle, prodrugs of t...

journal_title：ChemMedChem

authors： Weinschenk L,Gollnest T,Schols D,Balzarini J,Meier C

更新日期：2015-05-01 00:00:00

abstract：:LSD1 is a lysine demethylase highly involved in initiation and development of cancer. To design highly effective covalent inhibitors, a strategy is to fill its large catalytic cleft by designing tranylcypromine (TCP) analogs decorated with long, hindered substituents. We prepared three series of TCP analogs, carrying ...

journal_title：ChemMedChem

authors： Fioravanti R,Romanelli A,Mautone N,Di Bello E,Rovere A,Corinti D,Zwergel C,Valente S,Rotili D,Botrugno OA,Dessanti P,Vultaggio S,Vianello P,Cappa A,Binda C,Mattevi A,Minucci S,Mercurio C,Varasi M,Mai A

更新日期：2020-04-03 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：:Here we report the synthesis of a number of compounds structurally related to arginine methyltransferase inhibitor 1 (AMI-1). The structural alterations that we made included: 1) the substitution of the sulfonic groups with the bioisosteric carboxylic groups; 2) the replacement of the ureidic function with a bis-amidi...

journal_title：ChemMedChem

authors： Castellano S,Milite C,Ragno R,Simeoni S,Mai A,Limongelli V,Novellino E,Bauer I,Brosch G,Spannhoff A,Cheng D,Bedford MT,Sbardella G

更新日期：2010-03-01 00:00:00

abstract：:There is an urgent need for new drugs for the treatment of tropical parasitic diseases such as human African trypanosomiasis, which is caused by Trypanosoma brucei. The enzyme trypanothione reductase (TryR) is a potential drug target within these organisms. Herein we report the screening of a 62,000 compound library a...

journal_title：ChemMedChem

authors： Spinks D,Shanks EJ,Cleghorn LA,McElroy S,Jones D,James D,Fairlamb AH,Frearson JA,Wyatt PG,Gilbert IH

更新日期：2009-12-01 00:00:00

abstract：:A small set of aggrecanase inhibitors based on the pyrrolo[3,4-c]quinolin-1-one or oxoisoindoline frameworks bearing a 4-(benzyloxy)phenyl substituent and different zinc binding groups were rationally designed and evaluated in silico by docking studies using the crystal structure of the ADAMTS-5 catalytic domain (PDB ...

journal_title：ChemMedChem

authors： Cappelli A,Nannicini C,Valenti S,Giuliani G,Anzini M,Mennuni L,Giordani A,Caselli G,Stasi LP,Makovec F,Giorgi G,Vomero S

更新日期：2010-05-03 00:00:00

abstract：:β-Sheet antimicrobial peptides (AMPs) are well recognized as promising candidates for the treatment of multidrug-resistant bacterial infections. To dissociate antimicrobial activity and hemolytic effect of β-sheet AMPs, we hypothesize that N-methylation of the intramolecular hydrogen bond(s)-forming amides could impro...

journal_title：ChemMedChem

authors： Li Y,Bionda N,Yongye A,Geer P,Stawikowski M,Cudic P,Martinez K,Houghten RA

更新日期：2013-11-01 00:00:00

abstract：:Silent Night: Antagonism of the orexin (or hypocretin) system has recently been identified as a novel mechanism for the treatment of insomnia. Herein, we describe discovery of a dual (OX(1)R/OX(2)R) orexin receptor antagonist featuring a 1,4-diazepane central constraint that blocks orexin signaling in vivo. In telemet...

journal_title：ChemMedChem

authors： Whitman DB,Cox CD,Breslin MJ,Brashear KM,Schreier JD,Bogusky MJ,Bednar RA,Lemaire W,Bruno JG,Hartman GD,Reiss DR,Harrell CM,Kraus RL,Li Y,Garson SL,Doran SM,Prueksaritanont T,Li C,Winrow CJ,Koblan KS,Renger JJ,C

更新日期：2009-07-01 00:00:00

abstract：:A series of new C13-triazole-bridged and C13-ether leucomycin analogues with a reduced aldehyde group were synthesized. Derivatives with the highest antibacterial [MIC values (S. epidermidis, S. pneumoniae): ∼2-4 μg mL(-1) ; 2.55-5.09 μm] and cytotoxic [IC50 values (HeLa, KB, MCF-7, A549, HepG2 cells): ∼1.35-3.70 μm] ...

journal_title：ChemMedChem

authors： Domagalska J,Janas A,Pyta K,Pecyna P,Ruszkowski P,Celewicz L,Gajecka M,Bartl F,Przybylski P

更新日期：2016-09-06 00:00:00

abstract：:Soluble guanylate cyclase (sGC) is a key signal-transduction enzyme activated by nitric oxide (NO). Impairments of the NO-sGC signaling pathway have been implicated in the pathogenesis of cardiovascular and other diseases. Direct stimulation of sGC represents a promising therapeutic strategy particularly for the treat...

journal_title：ChemMedChem

authors： Mittendorf J,Weigand S,Alonso-Alija C,Bischoff E,Feurer A,Gerisch M,Kern A,Knorr A,Lang D,Muenter K,Radtke M,Schirok H,Schlemmer KH,Stahl E,Straub A,Wunder F,Stasch JP

更新日期：2009-05-01 00:00:00

abstract：:Clostridium difficile infection (CDI) symptoms range from diarrhea to severe toxic megacolon and even death. Due to its rapid acquisition of resistance, C. difficile is listed as an urgent antibiotic-resistant threat, and has surpassed methicillin-resistant Staphylococcus aureus (MRSA) as the most common hospital-acqu...

journal_title：ChemMedChem

authors： Li C,Teng P,Peng Z,Sang P,Sun X,Cai J

更新日期：2018-07-18 00:00:00

abstract：:3-Deazaneplanocin A (DzNep) is a potential epigenetic drug for the treatment of various cancers. DzNep has been reported to deplete histone methylations, including oncogenic EZH2 complex, giving rise to epigenetic modifications that reactivate many silenced tumor suppressors in cancer cells. Despite its promise as an ...

journal_title：ChemMedChem

authors： Tam EK,Nguyen TM,Lim CZ,Lee PL,Li Z,Jiang X,Santhanakrishnan S,Tan TW,Goh YL,Wong SY,Yang H,Ong EH,Hill J,Yu Q,Chai CL

更新日期：2015-01-01 00:00:00

abstract：:A series of deuterated curcuminoids (CUR) were synthesized, bearing two to six OCD3 groups, in some cases in combination with methoxy groups, and in others together with fluorine or chlorine atoms. A model ring-deuterated hexamethoxy-CUR-BF2 and its corresponding CUR compound were also synthesized from a 2,4,6-trimeth...

journal_title：ChemMedChem

authors： Laali KK,Zwarycz AT,Bunge SD,Borosky GL,Nukaya M,Kennedy GD

更新日期：2019-06-18 00:00:00

abstract：:Aberrant WNT pathway activation, leading to nuclear accumulation of β-catenin, is a key oncogenic driver event. Mutations in the tumor suppressor gene APC lead to impaired proteasomal degradation of β-catenin and subsequent nuclear translocation. Restoring cellular degradation of β-catenin represents a potential thera...

journal_title：ChemMedChem

authors： Kessler D,Mayer M,Zahn SK,Zeeb M,Wöhrle S,Bergner A,Bruchhaus J,Ciftci T,Dahmann G,Dettling M,Döbel S,Fuchs JE,Geist L,Hela W,Kofink C,Kousek R,Moser F,Puchner T,Rumpel K,Scharnweber M,Werni P,Wolkerstorfer B,

更新日期：2020-12-04 00:00:00

abstract：:Having recently identified a so-far unexplored area adjacent to the known binding site of allosteric mitogen-activated protein kinase kinase (MEK) inhibitors, we now report an extension of these studies by combining our new side chains with different MEK inhibitor cores in a modular manner. Replacement of the amide he...

journal_title：ChemMedChem

authors： Hartung IV,Pühler F,Neuhaus R,Scholz A,Siemeister G,Geisler J,Hillig RC,von Ahsen O,Hitchcock M

更新日期：2015-12-01 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：:Nanoscale materials hold great promise in the therapeutic field. In particular, as carriers or vectors, they help bioactive molecules reach their primary targets. Furthermore, by themselves, certain nanomaterials-regarded as protective-can modulate particular metabolic pathways that are deregulated in pathological sit...

journal_title：ChemMedChem

authors： Bianco A,Muller S

更新日期：2016-01-19 00:00:00

abstract：:Global pharmaceutical and biotechnology companies have been building increasingly on the skills and services offered by Indian biotech companies through strategic collaborative partnerships and alliances to fuel their in-house discovery and development pipelines. With the exception of generic press releases, however, ...

journal_title：ChemMedChem

authors： Differding E

更新日期：2014-01-01 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：:The concise synthesis and structure-activity relationship (SAR) studies of 3-aroylindoles were carried out in an effort to improve the potency and solubility of anticancer drug candidate BPR0L075 (8) by exploring structure modifications through three regimens: substitution of the B ring, at the N1 position, and of the...

journal_title：ChemMedChem

authors： Liou JP,Mahindroo N,Chang CW,Guo FM,Lee SW,Tan UK,Yeh TK,Kuo CC,Chang YW,Lu PH,Tung YS,Lin KT,Chang JY,Hsieh HP

更新日期：2006-10-01 00:00:00

abstract：:The development of more selective chemotherapeutic agents for benign treatments of malicious diseases is highly desirable. In recent years model systems for the release of small molecule drugs from nucleic acid conjugates by templated chemical or photochemical reactions have been designed. Common for these systems is ...

journal_title：ChemMedChem

authors： Jacobsen MF,Cló E,Mokhir A,Gothelf KV

更新日期：2007-06-01 00:00:00

abstract：:Despite bioavailability issues, tea catechins have emerged as promising chemopreventive agents because of their efficacy in various animal models. We synthesized two catechin-derived compounds, 3-O-(3,4,5-trimethoxybenzoyl)-(-)-catechin (TMCG) and 3-O-(3,4,5-trimethoxybenzoyl)-(-)-epicatechin (TMECG), in an attempt to...

journal_title：ChemMedChem

authors： Sáez-Ayala M,Sánchez-del-Campo L,Montenegro MF,Chazarra S,Tárraga A,Cabezas-Herrera J,Rodríguez-López JN

更新日期：2011-03-07 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