Kaolin alleviates the toxicity of graphene oxide for mammalian cells.

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：: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：:We previously reported that troponoid compounds profoundly inhibit replication of herpes simplex virus (HSV)-1 and HSV-2 in cell culture, including acyclovir-resistant mutants. Synthesis of 26 alpha-hydroxylated tropolones (αHTs) led to a preliminary structure-activity relationship highlighting the potency of bi-pheny...

journal_title：MedChemComm

authors： Berkowitz AJ,Franson AD,Gazquez Cassals A,Donald KA,Yu AJ,Garimallaprabhakaran AK,Morrison LA,Murelli RP

更新日期：2019-05-30 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 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 benzisoxazole analogs represent one of the privileged structures in medicinal chemistry and there has been an increasing number of studies on benzisoxazole-containing compounds. The unique benzisoxazole scaffold also exhibits an impressive potential as antimicrobial, anticancer, anti-inflammatory, anti-glycation a...

journal_title：MedChemComm

authors： Rakesh KP,Shantharam CS,Sridhara MB,Manukumar HM,Qin HL

更新日期：2017-10-31 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：: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：: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：:Three series of compounds were designed, synthesized and evaluated for their in vitro anticancer activity against a procaspase-3 over-expression cancer cell line (U937) and a procaspase-3 no-expression cancer cell line (MCF-7) to rule out off-target effects. Biological evaluation led to the identification of a series ...

journal_title：MedChemComm

authors： Ma J,Ni X,Gao Y,Huang K,Liu J,Wang Y,Chen R,Wang C

更新日期：2019-02-25 00:00:00

abstract：:Tetrahydroisoquinoline (THIQ) is a key structural component in many biologically active molecules including natural products and synthetic pharmaceuticals. Here, we report on the use of transition-metal mediated [2 + 2 + 2] cyclotrimerisation of alkynes to generate tricyclic THIQs with potential to selectively inhibit...

journal_title：MedChemComm

authors： Santos ARN,Sheldrake HM,Ibrahim AIM,Danta CC,Bonanni D,Daga M,Oliaro-Bosso S,Boschi D,Lolli ML,Pors K

更新日期：2019-06-27 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：: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 combinatorial library of 6 × 106 cyclic peptides was synthesized in the one bead-two compound format, with each bead displaying a unique cyclic peptide on its surface and a linear peptide encoding tag in its interior. Screening of the library against K-Ras identified compounds that bound K-Ras with submicromolar aff...

journal_title：MedChemComm

authors： Wu X,Upadhyaya P,Villalona-Calero MA,Briesewitz R,Pei D

更新日期：2013-02-01 00:00:00

abstract：:A new iron(iii) complex with 5,7-dichloro-2-methyl-8-quinolinol (HClMQ) as ligands, i.e., [Fe(ClMQ)2Cl] (1), was synthesized and evaluated for its anticancer activity. Compared to the HClMQ ligand, complex 1 showed a higher cytotoxicity towards a series of tumor cell lines, including Hep-G2, BEL-7404, NCI-H460, A549, ...

journal_title：MedChemComm

authors： Zou BQ,Qin QP,Bai YX,Cao QQ,Zhang Y,Liu YC,Chen ZF,Liang H

更新日期：2017-02-01 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：:We used quantum mechanics/molecular mechanics calculations to test if antimalarial primaquine (PQ) and its derivatives aid the conversion of hemoglobin to methemoglobin by binding to hemoglobin and merely lowering hemoglobin's ionization potential (IP). Our results showed that PQ and its derivatives do not significant...

journal_title：MedChemComm

authors： Liu H,Ding Y,Walker LA,Doerksen RJ

更新日期：2013-08-01 00:00:00

abstract：:Rigidification of the isobutyl side chain of drug-like AT2 receptor agonists and antagonists that are structurally related to the first reported selective AT2 receptor agonist 1 (C21) delivered bioactive indane derivatives. Four enantiomer pairs were synthesized and the enantiomers were isolated in an optical purity >...

journal_title：MedChemComm

authors： Wallinder C,Sköld C,Sundholm S,Guimond MO,Yahiaoui S,Lindeberg G,Gallo-Payet N,Hallberg M,Alterman M

更新日期：2019-11-18 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：:[This corrects the article DOI: 10.1039/C7MD00637C.]. ...

journal_title：MedChemComm

authors： Okombo J,Chibale K

更新日期：2018-03-02 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

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：: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：: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：: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：:Based on structure modification and a high-throughput Jurkat-Lat cell screening model, we found that GIBH-LRA002, ethyl-2-amino-3-cyano-9-methyl-4-(trifluoromethyl)-4,9-dihydropyrano[2,3-b]indole-4-carboxylate, effectively reactivated the latent proviruses in a Jurkat-Lat cell line and primary CD4+ T cells from both c...

journal_title：MedChemComm

authors： Yang Q,Ding Y,Feng F,Pan E,Fan X,Ma X,Chen L,Zhao J,Sun C

更新日期：2017-07-25 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 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：: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