Recent progress in the development of metal complexes as β-amyloid imaging probes in the brain.

abstract：:[This corrects the article DOI: 10.1039/C0MD00060D.]. ...

journal_title：MedChemComm

authors： Chen T,Mei WJ,Wong YS,Liu J,Liu Y,Xie HS,Zheng WJ

更新日期：2018-03-19 00:00:00

abstract：:The cytotoxic drug gemcitabine (GEM) has been conjugated to receptor-binding peptides to target melanoma tumors. A hexapeptide having a Lys-Gly-His-Lys sequence (pep-1), an octapeptide with an Arg-Gly-Asp-Lys-Gly-His-Lys sequence (pep-2), a GEM-conjugated Lys-Gly-His-Lys peptide (GEM-pep-3) and a GEM-conjugated Asp-Gl...

journal_title：MedChemComm

authors： Gaonkar RH,Baishya R,Paul B,Dewanjee S,Ganguly S,Debnath MC,Ganguly S

更新日期：2018-03-06 00:00:00

abstract：:The development of novel nanoscale vehicles for drug delivery promotes the growth of interest in investigations of interaction between nanomaterials. In this paper, we report the in vitro studies of eukaryotic cell physiological response to incubation with graphene oxide and planar kaolin nanoclay. Graphene family mat...

journal_title：MedChemComm

authors： Rozhina E,Batasheva S,Danilushkina A,Kryuchkova M,Gomzikova M,Cherednichenko Y,Nigamatzyanova L,Akhatova F,Fakhrullin R

更新日期：2019-06-10 00:00:00

abstract：:Herein we continued our previous work on the development of CB2 ligands, reporting the design and synthesis of a series of benzimidazole-containing derivatives that were explored as selective CB2 ligands with binding affinity towards both CB1 and CB2 receptors. Seven out of eighteen compounds exhibited preferential bi...

journal_title：MedChemComm

authors： Tonelli M,Cichero E,Mahmoud AM,Rabbito A,Tasso B,Fossa P,Ligresti A

更新日期：2018-10-10 00:00:00

abstract：:Two diazabicyclo analogues of maraviroc, in which the azabicyclooctane moiety is replaced by diazabicyclooctane or diazabicyclononane, were synthesized and tested, through a viral neutralization assay, on a panel of six pseudoviruses. The diazabicyclooctane derivative maintained a significant infectivity reduction pow...

journal_title：MedChemComm

authors： Legnani L,Colombo D,Venuti A,Pastori C,Lopalco L,Toma L,Mori M,Grazioso G,Villa S

更新日期：2016-12-16 00:00:00

abstract：:Previous studies have demonstrated that natural steroid compounds containing a peroxide bridge exhibited potential anti-hepatitis B virus activity. To continue our research, a simple and regioselective methodology, using Eosin Y as a clean photosensitized oxidation catalyst, was developed for the synthesis of a peroxi...

journal_title：MedChemComm

authors： Jia M,Zhao R,Xu B,Yan W,Chu F,Gu H,Xie T,Xiang H,Ren J,Chen D,Wang P,Lei H

更新日期：2016-10-19 00:00:00

abstract：:Transcriptomic phenotypes defined for melanoma have been reported to correlate with sensitivity to various drugs. In this study, we aimed to define a minimal signature that could be used to distinguish melanoma sub-types in vitro, and to determine suitable drugs by which these sub-types can be targeted. By using prima...

journal_title：MedChemComm

authors： Senses KM,Ghasemi M,Akbar MW,Isbilen M,Fallacara AL,Frankenburg S,Schenone S,Lotem M,Botta M,Gure AO

更新日期：2017-01-01 00:00:00

abstract：:Fungal infections directly affect millions of people each year. In addition to the invasive fungal infections of humans, the plants and animals that comprise our primary food source are also susceptible to diseases caused by these eukaryotic microbes. The need for antifungals, not only for our medical needs, but also ...

journal_title：MedChemComm

authors： Ngo HX,Garneau-Tsodikova S,Green KD

更新日期：2016-07-01 00:00:00

abstract：:Periodontal disease is an oral chronic immune-inflammatory disease highly prevalent worldwide that is initiated by specific oral bacterial species leading to local and systemic effects. The development of new preventive/therapeutic strategies to specifically target oral periodontopathogens without perturbing oral micr...

journal_title：MedChemComm

authors： Thamban Chandrika N,Fosso MY,Alimova Y,May A,Gonzalez OA,Garneau-Tsodikova S

更新日期：2019-06-10 00:00:00

abstract：:As the protein databank (PDB) recently passed the cap of 123 456 structures, it stands more than ever as an important resource not only to analyze structural features of specific biological systems, but also to study the prevalence of structural patterns observed in a large body of unrelated structures, that may refle...

journal_title：MedChemComm

authors： Ferreira de Freitas R,Schapira M

更新日期：2017-10-01 00:00:00

abstract：:Zampanolide and dactylolide are microtubule-stabilizing polyketides possessing potent cytotoxicity towards a variety of cancer cell lines. Using our understanding of the conformational preferences of the macrolide core in both natural products, we hypothesized that analogues lacking the C17-methyl group would maintain...

journal_title：MedChemComm

authors： Henry JL,Wilson MR,Mulligan MP,Quinn TR,Sackett DL,Taylor RE

更新日期：2019-04-09 00:00:00

abstract：:Bruton's tyrosine kinase (BTK) plays a critical role in B cell receptor (BCR)-mediated signaling pathways responsible for the development and function of B cells, which makes it an attractive target for the treatment of many types of B-cell malignancies. Herein, a series of N5-substituted 6,7-dioxo-6,7-dihydropteridin...

journal_title：MedChemComm

authors： Chen H,Song P,Diao Y,Hao Y,Dou D,Wang W,Fang X,Wang Y,Zhao Z,Ding J,Li H,Xie H,Xu Y

更新日期：2018-03-13 00:00:00

abstract：:Heat shock factor 1 (HSF1) is a transcription factor that plays key roles in cancer, including providing a mechanism for cell survival under proteotoxic stress. Therefore, inhibition of the HSF1-stress pathway represents an exciting new opportunity in cancer treatment. We employed an unbiased phenotypic screen to disc...

journal_title：MedChemComm

authors： Rye CS,Chessum NE,Lamont S,Pike KG,Faulder P,Demeritt J,Kemmitt P,Tucker J,Zani L,Cheeseman MD,Isaac R,Goodwin L,Boros J,Raynaud F,Hayes A,Henley AT,de Billy E,Lynch CJ,Sharp SY,Te Poele R,Fee LO,Foote KM,Gree

更新日期：2016-08-01 00:00:00

abstract：:A novel series of 2-pyrazoline derivatives were designed, synthesized, and evaluated for cholinesterase (ChE) inhibitory, Aβ anti-aggregating and neuroprotective activities. Among these, 3d, 3e, 3g, and 3h were established as the most potent and selective BChE inhibitors (IC50 = 0.5-3.9 μM), while 3f presented dual in...

journal_title：MedChemComm

authors： Unsal-Tan O,Tüylü Küçükkılınç T,Ayazgök B,Balkan A,Ozadali-Sari K

更新日期：2019-05-09 00:00:00

abstract：:A novel and simplified synthetic scaffold based on pladienolide was designed using a consensus pharmacophore hypothesis. An initial target was synthesized and evaluated to examine the role of the 3-hydroxy group and the methyl groups present at positions 10, 16, 20, 22 in 1, on biological activity. We report the first...

journal_title：MedChemComm

authors： Gundluru MK,Pourpak A,Cui X,Morris SW,Webb TR

更新日期：2011-01-01 00:00:00

abstract：:The natural products colchicine and combretastatin A-4 (CA4) have provided inspiration for the discovery and development of a wide array of derivatives and analogues that inhibit tubulin polymerization through a binding interaction at the colchicine site on β-tubulin. A water-soluble phosphate prodrug salt of CA4 (ref...

journal_title：MedChemComm

authors： Maguire CJ,Chen Z,Mocharla VP,Sriram M,Strecker TE,Hamel E,Zhou H,Lopez R,Wang Y,Mason RP,Chaplin DJ,Trawick ML,Pinney KG

更新日期：2018-08-24 00:00:00

abstract：:New derivatives of aminoglycosides containing 6'-carboxylic acid or 6'-amide on their ring I were designed, synthesized and their ability to readthrough nonsense mutations was examined in vitro, along with the protein translation inhibition in prokaryotic and eukaryotic systems. The observed structure-activity relatio...

journal_title：MedChemComm

authors： Sabbavarapu NM,Pieńko T,Zalman BH,Trylska J,Baasov T

更新日期：2018-02-02 00:00:00

abstract：:To increase the diversity of estrogen receptor (ER) ligands having novel structures and activities, series of selenophene derivatives with a basic side chain (BSC) were synthesized and their biological activity as subtype-selective antagonists for the ER was explored. Compared with the selenophenes without a BSC, most...

journal_title：MedChemComm

authors： Luo J,Hu Z,Xiao Y,Yang T,Dong C,Huang J,Zhou HB

更新日期：2017-05-24 00:00:00

abstract：:A series of 18 new 5-[3-(4-aryl-1-piperazinyl)propoxy]coumarin derivatives from the corresponding bromoalkyl derivatives have been designed and synthesized by us using a microwave-assisted protocol. Radioligand binding assays of this series of compounds as well as a previously synthesized series of 17 structurally-sim...

journal_title：MedChemComm

authors： Ostrowska K,Grzeszczuk D,Głuch-Lutwin M,Gryboś A,Siwek A,Dobrzycki Ł,Trzaskowski B

更新日期：2017-07-03 00:00:00

abstract：:A series of 4-thiazolidinone derivatives were synthesized and evaluated as novel human dihydroorotate dehydrogenase (hDHODH) inhibitors. Compounds 26 and 31 displayed IC50 values of 1.75 and 1.12 μM, respectively. The structure-activity relationship was summarized. Further binding mode analysis revealed that compound ...

journal_title：MedChemComm

authors： Zeng F,Qi T,Li C,Li T,Li H,Li S,Zhu L,Xu X

更新日期：2017-04-26 00:00:00

abstract：:2-Arylethynyl derivatives of (N)-methanocarba adenosine 5'-uronamides are selective A3AR (adenosine receptor) agonists. Here we substitute a 1,2,3-triazol-1-yl linker in place of the rigid, linear ethynyl group to eliminate its potential metabolic liability. Docking of nucleosides containing possible short linker moie...

journal_title：MedChemComm

authors： Tosh DK,Paoletta S,Chen Z,Crane S,Lloyd J,Gao ZG,Gizewski ET,Auchampach JA,Salvemini D,Jacobson KA

更新日期：2015-01-01 00:00:00

abstract：:Covalent probes and drugs have found widespread use as research tools and clinical agents. Covalent probes are useful because of their increased intracellular potency and because covalent labeling of cellular proteins can be tracked using click chemistry. Covalent drugs, on the other hand, can overcome drug resistance...

journal_title：MedChemComm

authors： Kathman SG,Statsyuk AV

更新日期：2016-04-01 00:00:00

abstract：:Diabetes mellitus is a chronic, complex and multifactorial disease associated characteristically with hyperglycemia. One of the most recently approved antidiabetic drug classes for clinical use are sodium-glucose cotransporter type 2 (SGLT-2) inhibitors. SGLT-2 is a protein expressed in the kidneys, responsible for gl...

journal_title：MedChemComm

authors： da Silva PN,da Conceição RA,do Couto Maia R,de Castro Barbosa ML

更新日期：2018-06-06 00:00:00

abstract：:Potent, selective, and cell active small molecule kinase inhibitors are useful tools to help unravel the complexities of kinase signaling. As the biological functions of individual kinases become better understood, they can become targets of drug discovery efforts. The small molecules used to shed light on function ca...

journal_title：MedChemComm

authors： Wells CI,Kapadia NR,Couñago RM,Drewry DH

更新日期：2017-12-08 00:00:00

abstract：:A series of indole derivatives was designed and synthesised to improve on activity and circumvent pharmacokinetic limitations experienced with the structurally related compound, ladostigil. The compounds consisted of a propargylamine moiety (a known MAO inhibitor and neuroprotector) at the N1 position and a ChE inhibi...

journal_title：MedChemComm

authors： Denya I,Malan SF,Enogieru AB,Omoruyi SI,Ekpo OE,Kapp E,Zindo FT,Joubert J

更新日期：2018-01-16 00:00:00

abstract：:In the last three decades, protein and nucleic acid structure determination and comprehension of the mechanisms, leading to their physiological and pathological functions, have become a cornerstone of biomedical sciences. A deep understanding of the principles governing the fates of cells and tissue at the molecular l...

journal_title：MedChemComm

authors： Bernetti M,Cavalli A,Mollica L

更新日期：2017-01-30 00:00:00

abstract：:A series of N-alkyl tethered C-5 functionalized bis-isatins were synthesized and evaluated for antimicrobial activity against pathogenic microorganisms. The preliminary evaluation studies revealed the compound 4t, with an optimal combination of bromo-substituent at the C-5 position of isatin ring along with propyl cha...

journal_title：MedChemComm

authors： Singh A,Nisha,Bains T,Hahn HJ,Liu N,Tam C,Cheng LW,Kim J,Debnath A,Land KM,Kumar V

更新日期：2017-01-01 00:00:00

abstract：:The dynamic and crucial role of tubulin in different cellular functions rendered it a promising target in anticancer drug development. Combretastatin A-4 (CA-4), an inhibitor of tubulin polymerization isolated from natural sources, is a lead molecule with significant cytotoxicity against tumour cells. Owing to its non...

journal_title：MedChemComm

authors： Seddigi ZS,Malik MS,Saraswati AP,Ahmed SA,Babalghith AO,Lamfon HA,Kamal A

更新日期：2017-07-04 00:00:00

abstract：:Glutamine and tyrosine-based amino acid conjugates of monocarboxylate transporter types 1 and 2 inhibitors (MCT1/2) were designed, synthesized and evaluated for their potency in blocking the proliferation of a human B lymphoma cell line that expresses the transporters Asct2, LAT1 and MCT1. Appropriate placement of an ...

journal_title：MedChemComm

authors： Nair RN,Mishra JK,Li F,Tortosa M,Yang C,Doherty JR,Cameron M,Cleveland JL,Roush WR,Bannister TD

更新日期：2016-05-01 00:00:00

abstract：:The dopamine D3 receptor (D3R) is a proven therapeutic target for the treatment of neurological and neuropsychiatric disorders. In particular, D3R-selective ligands that can eliminate side effects associated with dopamine D2 receptor (D2R) therapeutics have been validated. However, the high homology in signaling pathw...

journal_title：MedChemComm

authors： Cao Y,Sun N,Zhang J,Liu Z,Tang YZ,Wu Z,Kim KM,Cheon SH

更新日期：2018-06-14 00:00:00