Claims
- 1. An aminopropylaminobleomycin represented by the following general formula or a salt thereof:
- [BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.3 --B
- wherein
- [BX] represents the bleomycin acid acyl group;
- A is ##STR17## R.sub.1 and R.sub.2 are independently lower alkyl or benzyl; R is lower alkylene;
- n is the integer 0 or 1; and
- B has the formula ##STR18## wherein (i) R.sub.3 is hydrogen and R.sub.4 is
- (a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.1 is lower alkyl,
- (b) benzyl substituted by cyano, two or more alkoxy groups or two or more benzyloxy groups,
- (c) lower alkyl substituted by cycloalkyl or anthranyl,
- (d) phenylethyl substituted by one or more halogen atoms, or
- (e) diphenylethyl; or
- (ii) both R.sub.3 and R.sub.4 are benzyl which may be substituted by one or more
- (a) benzyloxy groups,
- (b) ring substituted benzyloxy groups in which the ring substituents may be one or more halogen atoms, lower alkoxy groups or benzyloxy groups, or
- (c) cycloalkylmethoxy groups;
- 2. An aminopropylaminobleomycin or a salt thereof according to claim 1, wherein ##STR19## R.sub.1 is lower alkyl; R.sub.2 is a lower alkyl or benzyl;
- n is the integer 0 or 1; and
- (i) R.sub.3 is hydrogen and R.sub.4 is
- (a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogens when R.sub.1 is lower alkyl,
- (b) benzyl substituted by cyano, two or more C.sub.1 -C.sub.4 alkoxy groups or two or more benzyloxy groups,
- (c) methyl substituted by a C.sub.8 -C.sub.13 cycloalkyl group, or
- (d) diphenylmethyl; or
- (ii) both R.sub.3 and R.sub.4 are benzyl optionally substituted by one or more
- (a) benzyloxy groups which may contain one or more ring substituents selected from halogen atoms, C.sub.1 -C.sub.4 alkoxy or benzyloxy, or
- (b) C.sub.8 -C.sub.13 cycloalkylmethoxy groups.
- 3. An aminopropylaminobleomycin or a salt thereof according to claim 1, wherein
- A is ##STR20## R.sub.3 is benzyl, substituted benzyl having one or more substituents selected from benzyloxy, cycloalkylmethyl having 11 to 13 carbon atoms in the cycloalkyl group, and
- R.sub.4 is a hydrogen atom, a benzyl group, or a benzyl group substituted by one or more benzyloxy groups.
- 4. The compound of claim 1 which is 3-{N-Methyl-N-[3'-(cycloundecanylmethylamino)propyl]amino}propylaminobleomycin.
- 5. The compound of claim 1 which is 3-{N-Methyl-N-[3'-(bis(m,p-dibenzyloxybenzyl)amino)priopyl]amino}propylaminobleomycin.
- 6. The compound of claim 1 which is 3-[4'-(3"-dibenzylaminopropyl)piperazin-1-yl]propylaminobleomycin.
- 7. The compound of claim 1 which is 3-{N,N-dimethyl-N-[3'-(dibenzylamino)propyl]amino}propylaminobleomycin.
- 8. The compound of claim 1 which is 3-{N,N-dimethyl-N-[3'-(N,N-dimethyl-N-(3"-dibenzylaminopropyl)amino)propyl]amino}propylaminobleomycin.
- 9. The compound of claim 1 which is 3-{N,N-dimethyl-N-[3'-(N,N-dimethyl-N-(3"-cyclooctylmethylaminopropyl)amino)propyl]amino}propylaminobleomycin.
- 10. The method for inhibiting an experimental mammalian tumor which comprises systemically administering to a mammal bearing a tumor a non-toxic anti-tumor effective amount of a Compound of claim 1.
Priority Claims (1)
Number |
Date |
Country |
Kind |
56-210449 |
Dec 1981 |
JPX |
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CROSS-REFERENCE TO RELATED APPLICATION
This is a continuation-in-part of our copending application Ser. No. 453,254 filed Dec. 27, 1982, and now abandoned.
US Referenced Citations (3)
Number |
Name |
Date |
Kind |
RE30451 |
Umezawa et al. |
Dec 1980 |
|
3922262 |
Umezawa et al. |
Nov 1975 |
|
3929993 |
Tomohisa et al. |
Dec 1975 |
|
Non-Patent Literature Citations (2)
Entry |
J. of Antibiotics, Umezawa, Maeda, et al., 19A, pp. 200-209 (1966). |
J. of Antibiotics, Umezawa, Suhara, et al., 19A, pp. 210-215 (1966). |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
453254 |
Dec 1982 |
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