ICI D1694, an inhibitor of thymidylate synthase for clinical study.
The TS inhibitor, ICI D1694, is a highly potent inhibitor of tumour growth in vitro and in vivo. Uptake via the RFC and rapid metabolism to polyglutamate forms appear to be responsible for potency. Antiproliferative toxicity in mice was evident although the dose-limiting renal toxicity experienced with CB3717 was not apparent.
Jackman
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Drug Development Section, Institute of Cancer Research, Sutton, Surrey, UK.
Jodrell
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Gibson
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Stephens
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TC
D000818:Animals; D001943:Breast Neoplasms; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D005260:Female; D005493:Folic Acid Antagonists / Q000633:toxicity*; D006801:Humans; D007939:Leukemia L1210; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D011799:Quinazolines / Q000494:pharmacology / Q000627:therapeutic use / Q000633:toxicity*; D013876:Thiophenes / Q000494:pharmacology / Q000627:therapeutic use / Q000633:toxicity*; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors*; D014407:Tumor Cells, Cultured
D005493:Folic Acid Antagonists; D011799:Quinazolines; D013876:Thiophenes; D013940:Thymidylate Synthase; C068874:raltitrexed