5-Fluorouracil derivatives. IX. Synthesis and antitumor activities of (alkylthio)carbonyl-5-fluorouracils.
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چکیده
منابع مشابه
Synthesis and bioevaluation of 5-fluorouracil derivatives.
A series of six novel 5-fluorouracil derivatives 1-6 were synthesized and their structures confirmed by (1)H- and (13)C-NMR, MS and elemental analysis. The preliminary in vitro antitumor activities against B16, K562 and CHO cells and the in vivo inhibitions of liver cancer H(22) demonstrated that some of these compounds effectively inhibit the growth of tumor cells, but the in vivo trials in mi...
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A series of amino acid ester derivatives containing 5-fluorouracil were synthesized using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC*HCl) and N-hydroxybenzotriazole (HOBt) as a coupling agent. The structures of the products were assigned by NMR, MS, IR etc. The in vitro antitumor activity tests against leukaemia HL-60 and liver cancer BEL-7402 indicated that (R)-ethyl 2-(2...
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Three new antitumour drugs containing two 5-fluorouracil moieties at both ends of the structure and a two amide bond linker were synthesized. Appropriated bis-acetal were reacted with two equivalents of 5-FU to afford the desired compounds. These drugs were evaluated for their ability to induce myogenic maturation in vitro on human rhabdomyosarcoma cells in an experimental model. Compounds 5 an...
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Starting from milbemycin D (1), milbemycin A4 (2) and milbemycin A3 (3), a series of 5-keto-5-oxime derivatives were synthesized by selective oximation at the alpha,beta-conjugated carbonyl function of the 5-ketomilbemycins (4-6). The activities of the synthesized compounds were studied in dogs naturally infested with microfilariae of Dirofilaria immitis. The 5-keto-5-oximes of milbemycin D (7)...
متن کاملSchedule-dependent antitumor effects of methotrexate and 5-fluorouracil.
The antitumor effects of methotrexate with 5-fluorouracil against the Sarcoma 180 mouse tumor model were found to be schedule dependent. Pretreatment of tumor-bearing animals with methotrexate significantly enhanced the antitumor activity of the combination relative to simultaneous treatment or to those with methotrexate following 5-fluorouracil. These studies indirectly support the hypothesis ...
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ژورنال
عنوان ژورنال: Chemical and Pharmaceutical Bulletin
سال: 1985
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.33.2832