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Characterization of a human squamous carcinoma cell line resistant to cis-diamminedichloroplatinum(II).
TLDR
The mechanism of resistance of the SCC-25/CP cell line to CDDP is multifactorial, involving plasma membrane changes, increased cytosolic binding, and decreased DNA cross-linking.
Carrier- and receptor-mediated transport of folate antagonists targeting folate-dependent enzymes: correlates of molecular-structure and biological activity.
TLDR
This folate antagonist structure-activity relationship can be of value for predicting drug sensitivity and resistance of tumor cells or drug-related toxicity to normal cells and for the rational design and development of novel antifolates.
A clinical-pharmacological evaluation of hepatic arterial infusions of 5-fluoro-2'-deoxyuridine and 5-fluorouracil.
TLDR
Hepatic arterial infusion is supported as a means to improve the therapeutic index of FdUrd and fluorouracil in the treatment of cancer in the liver and this type of analytical approach should prove valuable in the evaluation of other agents for liver cancer treatment.
Cyclophosphamide pharmacokinetics: correlation with cardiac toxicity and tumor response.
TLDR
These pharmacokinetic data support the premise that enhancement of cyclophosphamide activation may lead to both greater tumor cytotoxicity and increased but reversible end-organ toxicity.
Biochemical studies on PT523, a potent nonpolyglutamatable antifolate, in cultured cells.
TLDR
Inhibition of H35 cell growth by PT523 was associated with a concentration- and time-related decrease in de novo dTMP and purine biosynthesis, suggesting that penetration of the cell probably involves, at least in part, active transport by the MTX/reduced folate carrier.
Comparison of pharmacokinetics of 5-fluorouracil and 5-fluorouracil with concurrent thymidine infusions in a Phase I trial.
The serum half-life of 5-fluorouracil (5-FUra) in humans is best described as a biexponential decay function, with t1/2 alpha = 7.8 +/- 2.6 (S.E.) min and t1/2 beta = 36.8 +/- 13.5 min during initial
Methotrexate analogues. 33. N delta-acyl-N alpha-(4-amino-4-deoxypteroyl)-L-ornithine derivatives: synthesis and in vitro antitumor activity.
TLDR
N delta-Acylation of APA-L-Orn markedly enhanced toxicity to cultured tumor cells, however, N delta-acyl derivatives also containing an N10-formyl substituent were less cytotoxic than the corresponding N 10-unsubstituted analogues even though their anti-DHFR activity was the same, suggesting that N10 -formylation may be unfavorable for transport.
Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium
Six previously undescribed N-(2,4-diaminopteridin-6-yl)methyldibenz[b,f]azepines with water-solubilizing O-carboxyalkyloxy or O-carboxybenzyloxy side chains at the 2'-position were synthesized and
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