Journal
MEDCHEMCOMM
Volume 4, Issue 2, Pages 417-421Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2md20320k
Keywords
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Funding
- NIH [R01 CA135043, R15 CA067236]
- President's Council Research Excellence Award
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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 Cys241 beta in the otherwise hydrophobic subpocket A.
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