Synthesis and antitumor evaluation of paclitaxel phosphonooxymethyl ethers: A novel class of water soluble paclitaxel pro-drugs

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 15, 1996, Pages 1837-1842

  Golik, Jerzy ^a   Wong, Henry S L ^a   Chen, Shu Hui ^b   Doyle, Terrence W ^b   Wright, J J Kim ^a   Knipe, Jay ^a   Rose, William C ^a   Casazza, Anna Maria ^a   Vyas, Dolatrai M ^a  

^a BRISTOL MYERS SQUIBB PHARMACEUTICAL RESEARCH INSTITUTE   (United States)

^b OncoRx Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALKALINE PHOSPHATASE; ANTINEOPLASTIC AGENT; ETHER DERIVATIVE; PACLITAXEL; PACLITAXEL DERIVATIVE; PRODRUG;

ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER; CATTLE; CONTROLLED STUDY; CYTOTOXICITY; DRUG BLOOD LEVEL; DRUG DESIGN; DRUG RELEASE; DRUG SOLUBILITY; DRUG STABILITY; DRUG SYNTHESIS; DRUG TISSUE LEVEL; INTRAPERITONEAL DRUG ADMINISTRATION; INTRAVENOUS DRUG ADMINISTRATION; LIVER; MOUSE; NONHUMAN;

ANIMALIA; BOS TAURUS;

EID: 0030572491     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00321-6     Document Type: Article

References (20)

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19. 16. Compounds 8 and 11 were administered iv to mice bearing sc-implanted M109 tumors. At intervals after dosing, plasma, liver and tumor samples were obtained. Concentrations of paclitaxel (1), 8, 11, and 20 were determined in these samples using a specific HPLC-UV ( 227 nm) assay following solid-phase extraction. Additional details will be published in a separate paper.
20. 17. Compounds were administered ip on days 5 and 8 post-tumor implant; paclitaxel was evaluated concomitantly in each experiment. All compounds were evaluated at several dose levels in a vehicle consisting of 10% ethanol/10% Cremophor/80% water (or 0.9% NaCl for paclitaxel). For additional details related to this antitumor test see: Rose, W. C. Cancer Treat. Repts. 1981, 65, 299.