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AssigneeKirin Beer Kabushiki Kaisha
InventorsNoboru Otake, Hiroyuki Kawai, Tomiko Kawasaki, Atsuo Odagawa, Masaru Kamishohara, Teruyuki Sakai
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Disclosed is a novel spicamycin derivative represented by the formula (I) or a salt thereof: ##STR1## wherein R represents an alkenyl having a given number of carbon atoms, a haloalkyl having a given number of carbon atoms, CH.sub.3 (CH.sub.2).sub.n CH(OH)-- or CH.sub.3 (CH.sub.2).sub.n-1 CH(OH)--CH.sub.2 -- (wherein n denotes an integer of 9-13), an alkyl with a certain group and a given number of carbon atoms, ##STR2## (wherein a denotes 2, and b denotes an integer of 10-15), CH.sub.3 (CH.sub.2).sub.c SO.sub.2 O(CH.sub.2).sub.d --, ##STR3## (wherein c denotes an integer of 0-3 and d denotes an integer of 10-15), (CH.sub.3).sub.3 Si(CH.sub.2).sub.10 --, (CH.sub.3).sub.3 Si--C.tbd.C--(CH.sub.2).sub.8 --, ##STR4## (wherein X represents O or S), and R.sub.1 and R.sub.2 are different from each other and each represents H or OH, which exhibits an excellent antitumor effect and has a high therapeutic index. An antitumor agent containing at least one of the above-described compounds in an effective amount is also disclosed.
A method of treating cancer comprising administering to a patient in need of such treatment an effective amount of a spicamycin derivative represented by the formula (I) or a salt thereof:
A method of treating cancer comprising administering to a patient in need of such treatment an effective amount of a spicamycin derivative which is selected from the group consisting of the following compounds:
A process for producing a spicamycin derivative, which comprises condensing 6-(4'-N-glycyl-spicaminyl-amino) purine of formula (IIIa) or a salt thereof ##STR60## with a carboxylic acid of the formula RCOOH or an active ester thereof to give a spicamycin derivative of formula (I) or a salt thereof ##STR61## where R.sub.1 is H and R.sub.2 is OH;
A process for producing a spicamycin derivative, which comprises condensing 6-(4''-N-glycyl-septaminyl-amino) purine of formula (IIIb) or a salt thereof ##STR67## with a carboxylic acid of the formula RCOOH or an active ester thereof to give a spicamycin derivative of formula (I) or a salt thereof ##STR68## where R.sub.1 is OH and R.sub.2 is H;
A spicamycin derivative 6-(4'-N-glycyl-spicaminyl-amino) purine represented by the following formula (IIIa) or a salt thereof:
A spicamycin derivative 6-(4'-N-glycyl-septaminyl-amino) purine represented by the following formula (IIIb) or a salt thereof:
Dependencies are inferred from the claim text.