Journal
CHEMMEDCHEM
Volume 5, Issue 10, Pages 1760-1769Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201000252
Keywords
cancer; dihydropyrimidines; kinesin inhibitors; molecular docking; multicomponent reactions
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Funding
- Cancer Research UK
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Dihydropyrimidine-based compounds belong to the first discovered inhibitors of the human mitotic kinesin Eg5. Although they are used by many research groups as model compounds for chemical genetics, considerably less emphasis has been placed on the improvement of this type of inhibitor, with the exception of two recent studies. Dihydropyrimidines can be divided into class I (analogues that bind in the S configuration) and class II type inhibitors, which bind in the R configuration. Herein we report the synthesis and optimization of novel class II type dihydropyrimidines using a combination of in vitro and docking techniques.
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