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

Xuan Li, Isabel Barasoain, Ruth Matesanz, J. Fernando Díaz, Wei-Shuo Fang, Xuan Li, Isabel Barasoain, Ruth Matesanz, J. Fernando Díaz, Wei-Shuo Fang

Index: Bioorg. Med. Chem. Lett. 19(3) , 751-4, (2009)

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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.