The antifolate compounds IOdeazaaminopterin (lOdAM) and IO-ethyl-IOdeazaaminopterin ( IO-EdAM) are therapeutically superior to methotrexate in transplanted murine tumor systems and in human tumor xenografts growing in immunodeficient "nude" mice. The increased therapeutic index of these analogs corr
Synthesis of the 7-hydroxy metabolites of methotrexate and 10-ethyl-10-deazaaminopterin
β Scribed by Marcia I. Dawson; David O'Krongly; Peter D. Hobbs; Jose R. Barrueco; Frank M. Sirotnak
- Book ID
- 102408837
- Publisher
- John Wiley and Sons
- Year
- 1987
- Tongue
- English
- Weight
- 416 KB
- Volume
- 76
- Category
- Article
- ISSN
- 0022-3549
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π SIMILAR VOLUMES
vevsi ty o f South A1 abama Mobile, AL 36688 SUMARY 10-Deazaaminopterin (1) and 10-Ethyl-10-deazaaminopterin ( 2 ) labeled uniformly w i t h 14C a t the glutamate moiety were prepared by the following procedure. Uniformly labeled L-glutamic acid was converted t o i t s dimethyl ester (3). -4-Amino-
lo-ethyl-1 0-deazaaminopterin (1 0-EDAM) is a rationally designed derivative of the antifolate. methotrexate (MTX). In a number of tumor models these design features have resulted in an improved spectrum of antiproliferative activity as compared with the parent compound. Using an MTT growth assay, w