5-Fluorouracil Derivatives. IX. Synthesis and Antitumor Activities of (Alkylthio) carbonyl-5-fluorouracils

• Published in: Chemical & pharmaceutical bulletin Vol. 33; no. 7; pp. 2832 - 2837
• Main Authors: HOSHIKO, TOMONORI, OZAKI, SHOICHIRO, WATANABE, YUTAKA, OGASAWARA, TOMIO, YAMAUCHI, SHIN, FUJIWARA, KEIJI, HOSHI, AKIO, IIGO, MASAAKI
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 1985; Maruzen; Japan Science and Technology Agency
• Subjects: 1-(octylthio) carbonyl-5-fluorouracil; Animals; Antineoplastic Agents - chemical synthesis; Chemical Phenomena; Chemistry; Exact sciences and technology; Fluorouracil - analogs & derivatives; Heterocyclic compounds; Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings; Leukemia L1210 - drug therapy; Mice; Organic chemistry; Preparations and properties; Antineoplastic agent; Nitrogen heterocycle; Six membered ring; Organic thiocarbamate; Ureas; L1210-Leukemia; NMR spectrum; Biological activity
• ISSN: 0009-2363; 1347-5223
• DOI: 10.1248/cpb.33.2832

A series of 5-fluorouracil derivatives having (alkylthio) carbonyl groups at the 1-, 3-, and 1, 3-positions was synthesized and tested for antitumor activity against L-1210 leukemia in mice. Among them, 1-(octylthio) carbonyl-5-fluorouracil showed promising activity ; it gave a greater increase in life span than 1-hexylcarbamoyl-5-fluorouracil (HCFU) and 1-(2-tetrahydrofuryl)-5-fluorouracil (Tegafur), which are both in clinical use.