ChemMedChem文献大全第8页

Modeling of Cdc25B dual specifity protein phosphatase inhibitors: docking of ligands and enzymatic inhibition mechanism.
abstract：:The Cdc25 dual specificity phosphatases have central roles in coordinating cellular signalling processes and cell proliferation. It has been reported that an improper amplification or activation of these enzymes is a distinctive feature of a number of human cancers, including breast cancers. Thus, the inhibition of Cd...

journal_title：ChemMedChem

pub_type： 杂志文章

doi：10.1002/cmdc.200500092

authors： Lavecchia A,Cosconati S,Limongelli V,Novellino E

更新日期：2006-05-01 00:00:00
The potential of P1 site alterations in peptidomimetic protease inhibitors as suggested by virtual screening and explored by the use of C-C-coupling reagents.
abstract：:A synthetic concept is presented that allows the construction of peptide isostere libraries through polymer-supported C-acylation reactions. A phosphorane linker reagent is used as a carbanion equivalent; by employing MSNT as a coupling reagent, the C-acylation can be conducted without racemization. Diastereoselective...

journal_title：ChemMedChem

pub_type： 杂志文章

doi：10.1002/cmdc.200500027

authors： Weik S,Luksch T,Evers A,Böttcher J,Sotriffer CA,Hasilik A,Löffler HG,Klebe G,Rademann J

更新日期：2006-04-01 00:00:00
Synthesis and preliminary biological evaluation of 2'-substituted 2-(3'-carboxybicyclo[1.1.1]pentyl)glycine derivatives as group I selective metabotropic glutamate receptor ligands.
abstract：:The first series of 2'-substituted 2-(3'-carboxybicyclo[1.1.1]pentyl)glycine derivatives, (2R)- and (2S)-(2',2'-dichloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (10) and (11), and 2-(2'-chloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (12) were synthesized and evaluated as mGluR ligands. Compounds 11 and 12 were shown to ...

journal_title：ChemMedChem

pub_type： 杂志文章

doi：10.1002/cmdc.200500071

authors： Pellicciari R,Filosa R,Fulco MC,Marinozzi M,Macchiarulo A,Novak C,Natalini B,Hermit MB,Nielsen S,Sager TN,Stensbøl TB,Thomsen C

更新日期：2006-03-01 00:00:00
Design, synthesis, biological evaluation, and molecular modeling studies of TIBO-like cyclic sulfones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
abstract：:TIBO- and TBO-like sulfone derivatives 1 and 2 were designed, synthesized, and tested for their ability to block the replication cycle of HIV-1 in infected cells. The anti-HIV-1 activities of sulfones 3, which were intermediates in the syntheses of 1 and 2, were also evaluated. Surprisingly, the sulfone analogues of T...

journal_title：ChemMedChem

pub_type： 杂志文章

doi：10.1002/cmdc.200500020

authors： Di Santo R,Costi R,Artico M,Ragno R,Lavecchia A,Novellino E,Gavuzzo E,La Torre F,Cirilli R,Cancio R,Maga G

更新日期：2006-01-01 00:00:00
The hit-to-lead process at Schering AG: strategic aspects.
abstract：:Modern organizations conducting drug-discovery programs frequently apply high-throughput screening to generate novel hit structures for the indications of interest. Systematic hit-to-lead processes have been established at most pharmaceutical companies to ensure a smooth conversion of hits into high-quality lead struc...

journal_title：ChemMedChem

pub_type： 杂志文章

doi：10.1002/cmdc.200500031

authors： Steinmeyer A

更新日期：2006-01-01 00:00:00

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