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你正在浏览MedChemComm期刊下所有文献
  • Novel sphingosine-containing analogues selectively inhibit sphingosine kinase (SK) isozymes, induce SK1 proteasomal degradation and reduce DNA synthesis in human pulmonary arterial smooth muscle cells.

    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

    pub_type： 杂志文章

    doi：10.1039/C3MD00201B

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

    更新日期：2013-01-01 00:00:00

  • Developing novel C-4 analogues of pyrrole-based antitubulin agents: weak but critical hydrogen bonding in the colchicine site.

    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

    pub_type： 杂志文章

    doi：10.1039/C2MD20320K

    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

  • Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance().

    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

    pub_type： 杂志文章

    doi：10.1039/C2MD20203D

    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

  • Design, synthesis and initial biological evaluation of a novel pladienolide analog scaffold.

    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

    pub_type： 杂志文章

    doi：10.1039/C1MD00040C

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

    更新日期：2011-01-01 00:00:00

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