Preclinical Pharmacology Studies and the Clinical Development of a Novel Multitargeted Antifolate, MTA (LY231514)
作者： Chuan Shih , Donald E. Thornton
DOI: 10.1007/978-1-59259-725-3_8
关键词:
摘要: Since the early 1950s, extensive research efforts have been devoted to discovery and development of antifolate antimetabolites as chemotherapeutic agents for management neoplastic diseases. However, it was only in last 10–15 yr, because rapid advances medicinal chemistry, X-ray protein crystallography, molecular biology, pharmacology, clinical medicine, that a significant number new generation antifolates were brought forward development. Several folate-based are currently being investigated trials. These include lometrexol (6R-5,10-dideazatetrahydrofolic acid) (1–3) LY309887 (4) AG2034 (5) which potent selective inhibitors glycinamide ribonucleotide formyltransferase (GARFT), an enzyme purine de novo biosynthetic pathway; trimetrexate (6) edatrexate (7,8) PT523 (9) act on dihydrofolate reductase (DHFR); raltitrexed (10,11) AG337 (12) BW1843U89 (13) ZD933 (14) specifically target thymidylate synthase (TS) involved pyrimidine biosynthesis.
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