Abstract: Compounds of the formula ##STR1## wherein R is --COCH.sub.3, --CHOHCH.sub.3, --COCH.sub.2 OH, or --CHOHCH.sub.2 OH; hydrogen; hydroxyl; a 1 to 3 carbon alkyl; a 1 to 3 carbon .omega.-hydroxyalkyl; a 2 to 7 carbon organic acid ester or diester of --COCH.sub.2 OH, --CHOHCH.sub.2 OH, or --CHOHCH.sub.3 ; or the groups --COCH.sub.2 OH, --CHOHCH.sub.2 OH, or --CHOHCH.sub.3 having a 1 to 6 carbon alkyl or aryl ether replacement of one or more hydroxyls; or 13-ketimine derivatives of --COCH.sub.3 or --COCH.sub.2 OH;Y is methoxy, hydroxy, or hydrogen; and X is O or NH, but when Y is hydroxy or hydrogen, X must be O;and wherein R' is a 1 to 3 carbon alkyl; andor wherein Z is O, S, CH.sub.2 or CHOR' wherein R' is 1 to 3 carbon alkyl,and the pharmaceutically acceptable acid additive salts thereof; are useful for retarding tumor proliferation.

Abstract: Disclosed herein is a new procedure for preparing the C.1-2,4-pentadienyl derivatives of 2-deoxyhexopyranoses, as well as a new procedure for allylation of daunosamine. These methods are particularly useful for the preparation of intermediates in the synthesis of adriamycin C-glycosidic analogs which are useful anti-tumor agents. These methods provide the first enabling disclosure of methods to prepare these desired adriamycin and anthrocyclinone C-glycosidic analogs.

Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein R is: --CO--CH.sub.3, --CHOH--CH.sub.3, --CO--CH.sub.2 OH, --CHOH--CH.sub.2 OH, hydrogen, hydroxy, 1 to 3 carbon alkyl, 1 to 3 carbon terminal hydroxyalkyl; or,a 2 to 7 carbon ester or diester of said --CO--CH.sub.2 OH, --CHOH--CH.sub.2 OH, --CHOH--CH.sub.3 or of said 1 to 3 carbon terminal hydroxyalkyl; orsaid --CO--CH.sub.2 OH, --CHOH--CH.sub.2 OH, or --CHOH--CH.sub.3 or said 1 to 3 C-terminal hydroxyalkyl having 1 to 6 carbon alkyl or aryl ether replacements of one or more of the hydroxyls; orthe 13-ketimine derivatives of --CO--CH.sub.3 and --CO--CH.sub.2 OH;Y is hydrogen, hydroxy, or methoxy,X is O or NH, but when Y is hydrogen or hydroxy, X must be O;at least one of R.sup.1 and R.sup.

Abstract: A group of new daunorubicin and doxorubicin derivatives is disclosed. Included in this group are 3'-deamino-3'(3"-cyano-4"-morpholinyl doxorubicin; 3'-deamino-3'-(3"-cyano-4"-morpholinyl)-13-dihydoxorubicin; (3'-deamino-3'-(3"-cyano-4"-morpholinyl) daunorubicin; 3'-deamino-3'-(3"-cyano-4"-morpholinyl)-3-dihydrodaunorubicin; and 3'-deamino-3'-(4"-morpholinyl-5-iminodoxorubicin and derivatives thereof which have excellent activity as antitumor agents.

Abstract: A group of new daunorubicin and doxorubicin derivatives is disclosed. These materials have the formula ##STR1## wherein R is CO--CH.sub.3 or CHOH--CH.sub.3 in the case of daunorubicin derivatives or CO--CH.sub.2 OH or CHOH--CH.sub.2 OH in the case of doxorubicin derivatives; X is O or NH; and A is either a cyano group (CN) or a hydrogen, subject to the limitation that when X is O, A must be a cyano group. When A is hydrogen, these compounds can exist as acid addition salts, as well. Derivatives of these compounds are disclosed as well.

Abstract: 5-Iminodoxorubicin and its pharmaceutically acceptable acid addition salts having good antitumor activity.

Abstract: Described are 3'-deamino-3'-(4-methoxy-1-piperidinyl) derivatives of daunorubicin and doxorubicin having the formula ##STR1## wherein R is COCH.sub.3 or --CHOHCH.sub.3 in the case of daunorubicin derivatives, or is COCH.sub.2 OH or --CHOH--CH.sub.2 OH in the case of doxorubicin derivatives together with their pharmaceutically acceptable acid salts. The compounds have utility as antitumor agents.

Abstract: Described are 3'-deamino-3'-(4-morpholinyl) derivatives of daunorubicin and doxorubicin having the formula ##STR1## wherein R is COCH.sub.3 or --CHOHCH.sub.3 in the case of daunorubicin derivatives, or is --COCH.sub.2 OH or --CHOHCH.sub.2 OH in the case of doxorubicin derivatives together with their pharmaceutically acceptable acid addition salts. The compounds have utility as antitumor agents.

Abstract: Septacidin analogs, useful as antitumor agents, having the structure ##STR1## where R is a branched or straight chain alkanoyl group of from 12 to 16 carbon atoms. A preferred compound is 6-[4,6-dideoxy-4-(isopalmitoylglycyl)-amino-.beta.-L-glucopyranosylamino]- 9H-purine.

Abstract: New compounds 4-methyl-1,4-cyclohexadiene-1-carboxaldehyde syn-oxime, 4-methoxymethyl-1,4-cyclohexadiene-1-carboxaldehyde syn-oxime, and 4-(1-methoxyethyl)-1,4-cyclohexadiene-1-carboxaldehyde syn-oxime, as well as the compound 1,4-cyclohexadiene-1-carboxaldehyde syn-oxime, are found to have a high degree of sweetness which is accompanied by very little off-taste. The compounds have good stability even in acid solution. They give no evidence of toxicity and can be employed in foods and beverages as synthetic sweetening ingredients.

Abstract: New 3-methyl-3-nitrosoureido derivatives of the following amino sugars were prepared as analogs of streptozotocin with the anomeric carbon protected, by nitrosating the methylureas in water with N.sub.2 O.sub.3 : 3-amino-3-deoxy-1,2-O-isopropylidene-.alpha.-D-ribofuranose; methyl 3-amino-3-deoxy-.beta.-D-xylopyranoside; methyl 3-amino-3-deoxy-.alpha.-D-altropyranoside; methyl 3-amino-3-deoxy-.alpha.-D-glucopyranoside; and methyl 3-amino-2,3,6-trideoxy-.alpha.-L-lyxohexopyranoside. Tests against murine leukemia L1210 show that the anticancer activity of streptozotocin not only was retained but was enhanced in most of these derivatives.