Development of first photoresponsive prodrug of paclitaxel |
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| Authors: | Skwarczynski Mariusz Noguchi Mayo Hirota Shun Sohma Youhei Kimura Tooru Hayashi Yoshio Kiso Yoshiaki |
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| Affiliation: | Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science and 21st Century COE Program, Kyoto Pharmaceutical University, Yamashina-ku, Japan. |
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| Abstract: | A prodrug of paclitaxel which has a coumarin derivative conjugated to the amino acid moiety of isotaxel (O-acyl isoform of paclitaxel) has been synthesized. The prodrug was selectively converted to isotaxel by visible light irradiation (430 nm) with the cleavage of coumarin. Finally, paclitaxel was released by subsequent spontaneous O-N intramolecular acyl migration. |
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