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1. An aldol-based build/couple/pair-strategy for the synthesis of medium- and large-sized rings: discovery of macrocyclic histone deacetylase inhibitors

Author

Marcaurelle, Lisa A., Haggarty, Stephen J., Palmer, Michelle, Foley, Michael A., Yan-Ling Zhang, Fass, Daniel M., Reis, Surya A., Wen-Ning Zhao, Young, Damian W., Akella, Lakshmi B., Ross, Nathan T., Rowley, Ann, Ryba, Troy D., Byung-Chul Suh, Jiangqiang Wei, Marie, Jean-Charles, Mulrooney, Carol A., Pandya, Bhaumik A., Kesavan, Sarathy, Lee, Maurice D., IV, Haibo Liu, Lowe, Jason T., Dandapani, Sivaraman, Duvall, Jeremy R., Gerard, Baudouin, and Comer, Eamon

Subjects
Macrocycles -- Research, Fructosediphosphate aldolase -- Research, Chemistry
Abstract

An aldol-based build/couple/pair (B/C/P) strategy is used for generating a collection of stereochemically and skeletally diverse small molecules. The screening of the library of macrolactams has led to the discovery of a novel class of histone deacetylase inhibitors, which has displayed mixed enzyme inhibition, and has led to increased levels of acetylation in a primary mouse neuron culture.

Published
2010

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