A new prodrug of paclitaxel: synthesis of Protaxel

Anti-cancer Drugs
A L SeligsonMilos Sovak

Abstract

2' and 7 Polyol carbonates of paclitaxel were synthesized and screened as potential paclitaxel prodrugs. Paclitaxel is released from 7-(2",3"-dihydroxypropylcarbonato) paclitaxel (Protaxel) at rates inversely proportional to pH, by an intramolecular cyclization. Compared to paclitaxel, maximum tolerated i.v. or i.p. doses (MTD) of Protaxel are about 2.5- to 3-fold higher; its efficacy is substantially higher in human cancer line xenografts in athymic mice, especially in prostate PC-3, breast MDA-MB 468 and ovary OVCAR-1.

References

Apr 13, 1995·The New England Journal of Medicine·E K Rowinsky, R C Donehower
Jan 30, 1999·Bioorganic & Medicinal Chemistry Letters·T TakahashiH Yamada
Dec 2, 1999·Journal of Medicinal Chemistry·A SafavyJ A Bonner
Jun 15, 2000·Cancer Chemotherapy and Pharmacology·K MrossH Maier-Lenz

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Citations

Dec 4, 2003·Bioorganic & Medicinal Chemistry Letters·Mariusz SkwarczynskiYoshiaki Kiso
Aug 27, 2005·Mitochondrion·Volkmar WeissigGerard G M D'Souza
Mar 8, 2008·Journal of Biomaterials Science. Polymer Edition·Beom-Young RyuByung-Wook Jo
Nov 2, 2011·EuroIntervention : Journal of EuroPCR in Collaboration with the Working Group on Interventional Cardiology of the European Society of Cardiology·Ulrich SpeckVerena Stangl
Aug 30, 2008·Expert Opinion on Drug Metabolism & Toxicology·Jason M HatfieldPhilip M Potter
Aug 28, 2009·Expert Opinion on Drug Delivery·Gerard G M D'Souza, Volkmar Weissig
Nov 22, 2005·Expert Opinion on Drug Delivery·Volkmar Weissig
May 24, 2007·British Journal of Pharmacology·J S Armstrong
Dec 8, 2006·Journal of Medicinal Chemistry·Mariusz SkwarczynskiYoshiaki Kiso

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