Literature DB >> 22472

Comparative studies on the metabolism of 2-(tetrahydrofuryl)-5-fluorouracil and 5-fluorouracil.

H Toide, H Akiyoshi, Y Minato, H Okuda, S Fujii.   

Abstract

5=Fluorouracil inhibited DNA synthesis markedly using various DNA precursors such as deoxyuridine, orotic acid, uracil, and uridine except for thymidine. 2-(Tetrahydrofury)-5-fluorouracil (FT-207) did not inhibit DNA synthesis with any of the precursors tested. The metabolisms of 5-fluorouracil and FT-207 in mice and rats were studied. When administered intravenously 5-fluorouracil was rapidly degraded to fluoro-beta-alanine in both mice and rats, while at most 70% of FT-207 was slowly degraded after a prolonged period. The metabolites of FT-207 were found to be 5-fluorouracil and fluoro-beta-alanine in both species of animals. In vitro degradation of FT-207 into 5-fluorouracil was observed mainly in the microsomal fraction in the presence of NADPH. This result suggested that microsomal electron-transport system was concerned with the degradation of FT-207.

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Year:  1977        PMID: 22472

Source DB:  PubMed          Journal:  Gan        ISSN: 0016-450X


  19 in total

1.  Potentiation of the chemotherapeutic action of tegafur against solid adenocarcinoma 755 by combination with L-cystine.

Authors:  M Iigo; A Hoshi; H Kitagawa
Journal:  J Cancer Res Clin Oncol       Date:  1986       Impact factor: 4.553

2.  An Unusual Case of Acute Liver Failure Caused by Adjuvant Oral Tegafur-Uracil with Folinate Therapy for Colon Cancer Patient: a Case Report.

Authors:  Masatsugu Hiraki; Toshiya Tanaka; Futa Koga; Akimasa Saito; Noriko Oza; Osamu Ikeda; Tatsuya Manabe; Atsushi Miyoshi; Kenji Kitahara; Seiji Sato; Hirokazu Noshiro
Journal:  J Gastrointest Cancer       Date:  2020-03

3.  Hepatic conversion of 1-(tetrahydro-2-furanyl)-5-fluorouracil into 5-fluorouracil in patients with hepatocellular carcinoma.

Authors:  S Kawata; S Noda; Y Imai; S Tamura; R Saitoh; S Miyoshi; Y Minami; S Tarui
Journal:  Gastroenterol Jpn       Date:  1987-02

Review 4.  Conceptual changes in cancer chemotherapy: from an oral fluoropyrimidine prodrug, UFT, to a novel oral fluoropyrimidine prodrug, S-1, and low-dose FP therapy in Japan.

Authors:  T Shirasaka; S Yamamitsu; A Tsuji; T Taguchi
Journal:  Invest New Drugs       Date:  2000-11       Impact factor: 3.850

Review 5.  Therapeutic usefulness of postoperative adjuvant chemotherapy with Tegafur-Uracil (UFT) in patients with breast cancer: focus on the results of clinical studies in Japan.

Authors:  Takahiro Nakayama; Shinzaburo Noguchi
Journal:  Oncologist       Date:  2010-01-15

Review 6.  S-1 in gastric cancer: a comprehensive review.

Authors:  Yoshihiko Maehara
Journal:  Gastric Cancer       Date:  2003       Impact factor: 7.370

7.  Antitumor activity of 1-alkylcarbamoyl derivatives of 5-fluorouracil in a variety of mouse tumors.

Authors:  M Iigo; A Hoshi; A Nakamura; K Kuretani
Journal:  Cancer Chemother Pharmacol       Date:  1978       Impact factor: 3.333

8.  5-Fluorouracil incorporated into the tissue RNA of human and rat bladder carcinoma after administration of 1-(2-tetrahydrofuryl)-5-fluorouracil combined with uracil.

Authors:  Shigehiro Tsujimoto; Kiyohide Fujimoto; Eijiro Okajima; Seiichiro Ozono; Eigoro Okajima; Yoshihiko Hirao
Journal:  Int J Clin Oncol       Date:  2008-05-08       Impact factor: 3.402

9.  Effect of gastrectomy on the pharmacokinetics of tegafur, uracil, and 5-fluorouracil after oral administration of a 1:4 tegafur and uracil combination.

Authors:  Y Maehara; H Takeuchi; T Oshiro; I Takahashi; S Inutsuka; H Baba; S Kohnoe; K Sugimachi
Journal:  Cancer Chemother Pharmacol       Date:  1994       Impact factor: 3.333

10.  Noninvasive direct detection of ocular mucositis by in vivo confocal microscopy in patients treated with S-1.

Authors:  Tai-ichiro Chikama; Norihisa Takahashi; Makiko Wakuta; Teruo Nishida
Journal:  Mol Vis       Date:  2009-12-26       Impact factor: 2.367

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