Kirin Beer Kabushiki Kaisha

Tomiko Kawasaki

Noboru Otake

Teruyuki Sakai

Hiroyuki Kawai

Atsuo Odagawa

Masaru Kamishohara

Kazuyoshi Adachi

Hiroyuki Tanba

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 --,

Spicamycin derivatives and the use thereof

Spicamycin derivative represented by the formula (I) or a salt thereof: ##STR1## wherein R represents specific diverse substituents, for example, a linear alkadienyl having from 11 to 13 carbon atoms, and R.sub.1 and R.sub.2 respectively represent H or OH. Examples of specific compounds are 6-[4'-N-(N'-trans,trans 2,4-tridecadienoylglycyl)spicaminyl-amino]purine, and 6-[4'-N-(N'-trans,trans-2,4 dodecadienyoly glycyl) spicaminyl-amino]purine. Comopunds according to this invention are useful as a pharmaceutical for inhibition of a tumor, for example, human colon cancer.

Spicamycin derivatives and their use as anticancer agents

Disclosed is a novel macrolide antibiotic, M 119, of the formula (A): ##STR1## wherein the substituent R designates either (a) or (d): (a) R: H

Macrolide antibiotic M 119

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Takasaki, Japan

Tomiko Kawasaki