2. Academic Validation
  3. Synthesis and biological activities of high affinity taxane-based fluorescent probes

Synthesis and biological activities of high affinity taxane-based fluorescent probes

  • Bioorg Med Chem Lett. 2009 Feb 1;19(3):751-4. doi: 10.1016/j.bmcl.2008.12.018.
Xuan Li 1,  Isabel Barasoain,  Ruth Matesanz,  J Fernando Díaz,  Wei-Shuo Fang
Affiliations

Affiliation

  • 1 Key Lab of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine (PUMC), Ministry of Education, Beijing 100050, China.
PMID: 19128972 DOI: 10.1016/j.bmcl.2008.12.018
Abstract

Three fluorescent probes 3a,3b, and 4 have been synthesized through conjugation of fluorescein and difluorescein groups to the 7-OH of C-2 modified paclitaxel and cephalomannine derivatives with very high affinity to microtubules. All these probes exhibited potent tubulin assembly promotion and tumor cell killing activities, thus may be useful as tools for the determination of thermodynamic parameters and exploration of ligand-microtubule interactions.

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