2. Academic Validation
  3. Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport

Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport

  • Bioorg Med Chem Lett. 2011 Aug 15;21(16):4852-6. doi: 10.1016/j.bmcl.2011.06.034.
Xi Xiao 1,  Ju Wu,  Chiara Trigili,  Hui Chen,  Joseph W K Chu,  Ying Zhao,  Peihua Lu,  Li Sheng,  Yan Li,  Frances J Sharom,  Isabel Barasoain,  J Fernando Diaz,  Wei-shuo Fang
Affiliations

Affiliation

  • 1 State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, China.
PMID: 21764308 DOI: 10.1016/j.bmcl.2011.06.034
Abstract

Some C-7 modified analogs of 3, a taxane with high affinity for binding to microtubules, were prepared through multistep transformations. Most of the analogs, bearing less lipophilic C-7 substituents than propionyl in 3, exhibited comparable binding affinities to microtubules but less cytotoxicity against drug-sensitive as well as multidrug-resistant tumor cells overexpressing P-glycoprotein. In addition, these C7 modifications increased P-glycoprotein-mediated drug transport in both directions in a Caco-2 cell assay.

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