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Developing novel C-4 analogues of pyrrole-based antitubulin agents: weak but critical hydrogen bonding in the colchicine site.
Da, Chenxiao; Telang, Nakul; Hall, Kayleigh; Kluball, Emily; Barelli, Peter; Finzel, Kara; Jia, Xin; Gupton, John T; Mooberry, Susan L; Kellogg, Glen E.
Affiliation
  • Da C; Department of Medicinal Chemistry & Institute for Structural Biology and Drug Discovery, Virginia Commonwealth University, Richmond, Virginia, USA 23298-0540.
  • Telang N; Department of Chemistry, Gottwald Center for the Sciences, University of Richmond, Richmond, Virginia, USA 23173.
  • Hall K; Department of Chemistry, Gottwald Center for the Sciences, University of Richmond, Richmond, Virginia, USA 23173.
  • Kluball E; Department of Chemistry, Gottwald Center for the Sciences, University of Richmond, Richmond, Virginia, USA 23173.
  • Barelli P; Department of Chemistry, Gottwald Center for the Sciences, University of Richmond, Richmond, Virginia, USA 23173.
  • Finzel K; Department of Chemistry, Gottwald Center for the Sciences, University of Richmond, Richmond, Virginia, USA 23173.
  • Jia X; Department of Chemistry, Gottwald Center for the Sciences, University of Richmond, Richmond, Virginia, USA 23173.
  • Gupton JT; Department of Chemistry, Gottwald Center for the Sciences, University of Richmond, Richmond, Virginia, USA 23173.
  • Mooberry SL; Department of Pharmacology, University of Texas Health Science Center at San Antonio, San Antonio, Texas, USA 78229-3900.
  • Kellogg GE; Department of Medicinal Chemistry & Institute for Structural Biology and Drug Discovery, Virginia Commonwealth University, Richmond, Virginia, USA 23298-0540.
Medchemcomm ; 4(2): 417-421, 2013.
Article in En | MEDLINE | ID: mdl-23457660
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 appropriately positioned acceptor for Cys241ß in the otherwise hydrophobic subpocket A.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Type of study: Prognostic_studies Language: En Journal: Medchemcomm Year: 2013 Document type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Type of study: Prognostic_studies Language: En Journal: Medchemcomm Year: 2013 Document type: Article