Novel 5-fluorouracil derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrogen atom or methyl group, and R.sub.4 represents a straight or branched alkyl or alkenyl group, which has low toxicity and improved antitumor activity, and novel antitumor preparations containing the said 5-fluorouracil derivative.

A process for production of 5-fluorouracil and its derivatives which comprises reacting a cytosine compound of the formula: ##STR1## wherein R is a hydrogen atom or a saccharide residue with fluorine or fluorine fluorosulfonate (FOSO.sub.2 F) in an aqueous medium to give the corresponding 5-fluorouracil compound of the formula: ##STR2## wherein R is as defined above.

N.sup.1 -(2-tetrahydrofuryl)-5-fluorouracil is produced in high yield by reacting 5-fluorouracil with 2,3-dihydrofuran in the presence of trimethylsilyl chloride and a tertiary amine and treating the resultant mixture with an aqueous alkaline solution.

Process for preparing N.sub.1 -(2'-furanidyl)-5-fluorouracil having effective pharmacological activities such as anti-leukemia and anti-tumor activities comprising reacting 2,4-bis(trialkylsilyl)-5-fluorouracil with 2,3-dihydrofuran in the presence of a proton donor and a catalyst. Such process can be simply, easily conducted to give the desired product having a high purity in good yield.

A 5-fluorouracil derivative represented by the formula (1): ##STR1## wherein A represents a group represented by ##STR2## wherein R.sup.1 represents a hydrogen atom or OR.sup.5 group, R.sup.2, R.sup.3 and R.sup.5 may be the same or different and each represents a hydrogen atom or a group represented by the following formula (2): ##STR3## wherein R.sup.6 represents an acyl group, R.sup.7 represents a hydrogen atom, a straight or branched alkyl group, a cycloalkyl group, an aralkyl group, a lower ...

A combination therapy for treating cancer including administering at least one camptothecin derivative in conjunction with another anticancer agent. The combination therapy is preferably used as a first-line therapy for treating metastatic colorectal cancer and preferably involves administration of a combination of CPT-11, 5-fluorouracil and folinic acid, according to specific infusional treatment schedules which show therapeutic synergy in the treatment of cancer.

Tumor growth and metastases in cancer patients are inhibited by administration of a combination therapy including effective amounts of 5-Fluorouracil and a methylol transfer agent such as taurolidine, taurultam or mixtures thereof.

A combination therapy for treating cancer including administering at least one camptothecin derivative in conjunction with another anticancer agent. The combination therapy is preferably used as a first-line therapy for treating metastatic colorectal cancer and preferably involves administration of a combination of CPT-11, 5-fluorouracil and folinic acid, according to specific infusional treatment schedules which show therapeutic synergy in the treatment of cancer.

The present invention relates to the treatment of inflammatory skin conditions, including psoriasis, with a prodrug of 5-fluorouracil. The invention relates to methods for treatment of psoriasis with capecitabine, an oral prodrug of 5-fluorouracil.

A process for producing 5-fluorouracil or 6-mercaptopurine riboside by fermentation which comprises culturing a micro-organism belonging to Bacillus subtilis or Streptomyces fradiae in an aqueous nutrient medium under aerobic conditions. In the case of 5-fluorouracil riboside, 5-fluorouracil is added to the medium and in the case of 6-mercaptopurine riboside, 6-mercaptopurine is added to the medium. The products have been reported as being useful as antagonistic agents of nucleic acid metabolism...