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Novel, water-soluble phosphate derivatives of 2′-ethoxy carbonylpaclitaxel as potential prodrugs of paclitaxel: Synthesis and antitumor evaluation

Authors :
Anna Maria Casazza
Yasutsugu Ueda
Vittorio Farina
William C. Rose
Amarendra B. Mikkilineni
John D. Matiskella
Jay O. Knipe
Dolatrai M. Vyas
Source :
Bioorganic & Medicinal Chemistry Letters. 5:247-252
Publication Year :
1995
Publisher :
Elsevier BV, 1995.

Abstract

Three new phosphate derivatives of paclitaxel-2′-ethylcarbonate 4a, 4b, and 4c, have been synthesized and evaluated for in vivo antitumor activity. All were soluble in water and two derivatives 4a and 4b were found to exhibit in vivo antitumor activity, comparable to paclitaxel in the M109 murine tumor model.

Details

ISSN :
0960894X
Volume :
5
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi...........f8badacaefe1c5ac0b86c528dc761fb5