The use of 111Ag as a tool for studying biological distribution of silver-based antimicrobials.

abstract：:Much effort has been devoted to targeting agents for imaging and chemotherapy of tumors in cancer research, but there remain significant unmet needs in that area. We have reported a series of preclinical TrkC targeting agents for diagnoses and treatment of metastatic breast cancer; however, with respect to optical ima...

journal_title：MedChemComm

authors： Yang Z,Usama SM,Li F,Burgess K,Li Z

更新日期：2018-08-03 00:00:00

abstract：:The benzophenone scaffold represents a ubiquitous structure in medicinal chemistry because it is found in several naturally occurring molecules which exhibit a variety of biological activities, such as anticancer, anti-inflammatory, antimicrobial, and antiviral. In addition, various synthetic benzophenone motifs are p...

journal_title：MedChemComm

authors： Surana K,Chaudhary B,Diwaker M,Sharma S

更新日期：2018-08-23 00:00:00

abstract：:A focused library of 24 N-aryl urea derivatives was prepared and evaluated against serine esterases of Mycobacterium tuberculosis (Mtb) Rv3802c and Mtb Ag85C. The members of the library were evaluated for both selectivity and mode of inhibition. Furan-based urea derivative 6c was found to be the most potent non-covale...

journal_title：MedChemComm

authors： Vartak A,Goins C,de Moura VCN,Schreidah CM,Landgraf AD,Lin B,Du J,Jackson M,Ronning DR,Sucheck SJ

更新日期：2019-06-04 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：:β-Carbolines have been assessed for osteoclastogenesis. However, their effect on osteoblasts during estrogen deficiency is still unclear. Here, a series of novel piperazine and tetrazole tag β-carbolines have been synthesized and examined for osteoblast differentiation in vitro. In vitro data suggest that compound 8g ...

journal_title：MedChemComm

authors： Karvande A,Khan S,Khan I,Singh D,Khedgikar V,Kushwaha P,Ahmad N,Kothari P,Dhasmana A,Kant R,Trivedi R,Chauhan PMS

更新日期：2018-06-12 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：: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：:Tuberculosis is an ever-evolving infectious disease that urgently needs new drugs. In the search for new antituberculosis agents, a library of 3-cinnamoyl-4-hydroxy-6-methyl-2H-pyran-2-ones (CHPs) (2a-2y) was synthesized and evaluated against a standard virulent laboratory strain of Mycobacterium tuberculosis H37Rv. O...

journal_title：MedChemComm

authors： Bhat ZS,Ul Lah H,Rather MA,Maqbool M,Ara T,Ahmad Z,Yousuf SK

更新日期：2017-12-06 00:00:00

abstract：:Classical aminoglycoside antibiotics are obsolete or hampered by the emergence of drug resistant bacteria. Recent discoveries of antifungal amphiphilic kanamycins offer new strategies for reviving and repurposing these old drugs. A simple structural modification turns the clinically obsolete antibacterial kanamycin in...

journal_title：MedChemComm

authors： Subedi YP,AlFindee MN,Takemoto JY,Chang CT

更新日期：2018-04-17 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 cyclic peptides were designed and prepared to investigate the physicochemical properties that affect oral bioavailabilty of this chemotype in rats. In particular, the ionization state of the peptide was examined by the incorporation of naturally occurring amino acid residues that are charged in differing r...

journal_title：MedChemComm

authors： Rand AC,Leung SS,Eng H,Rotter CJ,Sharma R,Kalgutkar AS,Zhang Y,Varma MV,Farley KA,Khunte B,Limberakis C,Price DA,Liras S,Mathiowetz AM,Jacobson MP,Lokey RS

更新日期：2012-10-01 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：: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：:The high storage capacities and excellent biocompatibilities of zinc(ii) metal-organic frameworks (Zn-MOFs) have made them outstanding candidates as drug delivery carriers. Recent studies on the pH-responsive processes based on carrier-drug interactions have proven them to be the most efficient and effective way to co...

journal_title：MedChemComm

authors： Liu W,Pan Y,Xiao W,Xu H,Liu D,Ren F,Peng X,Liu J

更新日期：2019-10-17 00:00:00

abstract：:Recognition of nucleosides at adenosine receptors (ARs) is supported by multiple X-ray structures, but the structure of an adenine complex is unknown. We examined the selectivity of predicted A1AR and A3AR adenine antagonists that incorporated known agonist affinity-enhancing N6 and C2 substituents. Adenines with A1AR...

journal_title：MedChemComm

authors： Yu J,Mannes P,Jung YH,Ciancetta A,Bitant A,Lieberman DI,Khaznadar S,Auchampach JA,Gao ZG,Jacobson KA

更新日期：2018-10-18 00:00:00

abstract：:N-Myristoyltransferase (NMT) represents an attractive drug target in parasitic infections such as malaria due to its genetic essentiality and amenability to inhibition by drug-like small molecules. Scaffold simplification from previously reported inhibitors containing bicyclic cores identified phenyl derivative 3, pro...

journal_title：MedChemComm

authors： Yu Z,Brannigan JA,Rangachari K,Heal WP,Wilkinson AJ,Holder AA,Leatherbarrow RJ,Tate EW

更新日期：2015-10-08 00:00:00

abstract：:The introduction of proteins into dendritic cells (DCs) ex vivo is a critical step for the DC-based immunotherapy of cancer. Here, we developed a biotin-modified polymer with multiple hydrophobic membrane anchors for cells that functions as a synthetic receptor for an antigen protein, ovalbumin (OVA), to introduce it ...

journal_title：MedChemComm

authors： Li C,Takeo M,Matsuda M,Nagai H,Xizheng S,Hatanaka W,Kishimura A,Inoue H,Tani K,Mori T,Katayama Y

更新日期：2017-05-12 00:00:00

abstract：:In this review, we have focused on the recent progress in metal complexes that are able to bind to β-amyloid (Aβ) species. We have discussed various radioactive complexes of 99mTc, 68Ga, 64Cu, 89Zr, and 111In, which were designed as Aβ imaging agents for positron emission tomography (PET) and single photon emission co...

journal_title：MedChemComm

authors： Chen K,Cui M

更新日期：2017-05-16 00:00:00

abstract：:In this paper, synthesis and characterization of metal complexes [Cu2(L)3]ClO4 (1), [Ga(L)2]NO3·2H2O (2) and [In(L)2]NO3·H2O (3) (HL = 2-acetylpyridine N(4)-phenylthiosemicarbazone) was carried out, including elemental analysis, spectral analysis (IR, UV-vis, NMR), and X-ray crystallography. Complex 1 contains one S-b...

journal_title：MedChemComm

authors： Wang YT,Fang Y,Zhao M,Li MX,Ji YM,Han QX

更新日期：2017-10-09 00:00:00

abstract：:Sphingosine 1-phosphate (S1P) is involved in hyper-proliferative diseases such as cancer and pulmonary arterial hypertension. We have synthesized inhibitors that are selective for the two isoforms of sphingosine kinase (SK1 and SK2) that catalyze the synthesis of S1P. A thiourea adduct of sphinganine (F02) is selectiv...

journal_title：MedChemComm

authors： Byun HS,Pyne S,Macritchie N,Pyne NJ,Bittman R

更新日期：2013-01-01 00:00:00

abstract：:Human African trypanosomiasis (HAT), also known as African sleeping sickness, is caused by parasitic protozoa of the genus Trypanosoma. As the disease progresses, the parasites cross the blood brain barrier and are lethal for the patients if the disease is left untreated. Current therapies suffer from several drawback...

journal_title：MedChemComm

authors： Berninger M,Schmidt I,Ponte-Sucre A,Holzgrabe U

更新日期：2017-07-31 00:00:00

abstract：:A library of 33 compounds was screened for potentiation of the antibiotic FR 900098 against the Francisella tularensis surrogate Francisella novicida. From the screen a highly potent 2-oxazoline adjuvant was discovered capable of potentiating FR 900098 with a 1000-fold reduction in MIC against the Francisella sub-spec...

journal_title：MedChemComm

authors： Stephens MD,Yodsanit N,Melander C

更新日期：2016-01-01 00:00:00

abstract：:The type III secretion system injectisome is a syringe-like multimembrane spanning nanomachine that is essential to the pathogenicity but not viability of many clinically relevant Gram-negative bacteria, such as enteropathogenic Escherichia coli, Salmonella enterica and Pseudomonas aeruginosa. Due to the rise in antib...

journal_title：MedChemComm

authors： Lyons BJE,Strynadka NCJ

更新日期：2019-06-20 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 synthesis, biological evaluation and molecular modeling of a series of pyrrole compounds related to 3,5-dibromo-4-(3,4-dimethoxyphenyl)-1H-pyrrole-2-carboxylic acid that evaluates and optimizes C-4 substituents are reported. The key factor for microtubule depolymerization activity appears to be the presence of an ...

journal_title：MedChemComm

authors： Da C,Telang N,Hall K,Kluball E,Barelli P,Finzel K,Jia X,Gupton JT,Mooberry SL,Kellogg GE

更新日期：2013-01-01 00:00:00

abstract：:In the present work, coumarin based pyrazolines (7a-g) have been synthesized and investigated for their in vitro and in vivo anti-inflammatory potential. Amongst the synthesized compounds, compounds 7a, 7d and 7f exhibited significant in vitro anti-inflammatory activity as compared to the standard etoricoxib. Keeping ...

journal_title：MedChemComm

authors： Chandel P,Kumar A,Singla N,Kumar A,Singh G,Gill RK

更新日期：2019-01-23 00:00:00

abstract：:Twenty-four 14-sulfonamide-tetrandrine derivatives as potential anti-cancer agents were synthesized. The synthetic derivatives were investigated for their cytotoxic activity against human cancer cell lines MDA-MB-231, PC3, WM9, HEL and K562. Initially, the IC50 values (50% inhibitory concentrations) of all of the comp...

journal_title：MedChemComm

authors： Song J,Lan J,Chen C,Hu S,Song J,Liu W,Zeng X,Lou H,Ben-David Y,Pan W

更新日期：2018-05-04 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：:A series of novel indazole-pyrone hybrids were synthesized by a one pot reaction between N-alkyl-6(5)-nitroindazoles and 2-pyrone (4-hydroxy-6-methyl-2H-pyran-2-one) using indium or stannous chloride as the reducing system in the presence of acetic acid in tetrahydrofuran. The hybrid molecules were obtained in good to...

journal_title：MedChemComm

authors： El Ghozlani M,Bouissane L,Berkani M,Mojahidi S,Allam A,Menendez C,Cojean S,Loiseau PM,Baltas M,Rakib EM

更新日期：2018-11-19 00:00:00

abstract：:Malaria is a serious tropical disease that kills thousands of people every year, mainly in Africa, due to Plasmodium falciparum infections. Salirasib is a promising cancer drug candidate that interferes with the post-translational modification of Ras. This S-farnesyl thiosalicylate inhibits isoprenylcysteine carboxyl ...

journal_title：MedChemComm

authors： Porta EOJ,Bofill Verdaguer I,Perez C,Banchio C,Ferreira de Azevedo M,Katzin AM,Labadie GR

更新日期：2019-06-21 00:00:00