Abstract: Methods and compositions are provided which include use of lymphotoxin (LT) and one or more other anti-cancer therapies for treating cancer in vivo or ex vivo. LT can be employed, for instance, with chemotherapy or radiation therapy to provide improved anti-cancer therapy.

Abstract: The present invention provides the new use in the manufacture of a medicament for use in the treatment of amyloidosis of an anthracycline of formula A: wherein R1, R2, R3 and X are appropriate substituents. Novel compounds of the formula A, processes for their production and pharmaceutical compositions containing them are also described.

Abstract: This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.

Abstract: A compound of hyaluronic acid and a medicinal ingredient produced by the convalent bonding (preferably amide bonding) of hyaluronic acid and the medicinal ingredient, and a process for preparing the same.The hyaluronic acid portion is completely decomposed by metabolism in the action region, whereby the medicinal ingredient is gradually and quantitatively released.

Abstract: Provided are enteric coating compositions which utilize a low viscosity cellulose acetate phthalate polymer as a film former. The cellulose acetate phthalates have an inherent viscosity of about 0.2 to 0.6 dL/g and phthalyl values of from 30 to 40% and can be applied to solid oral medicaments with less solvent than conventional cellulose acetate phthalate polymers. Also provided is a process for preparing the low viscosity cellulose acetate phthalate polymers.

Abstract: A method for treating cellulose with cellulose ester for use in various paper products involves reacting cellulose and an acid anhydride to form a cellulose ester-carboxylic acid solution. Acetic anhydride may be used as the acid anhydride, and a cellulose acetate-acetic acid solution may formed as the resulting cellulose ester-acetic acid solution. The cellulose acetate-acetic acid solution is diluted in a mixer, with additional acetic acid. Bulk cellulose is milled into cellulose fibers, and the diluted cellulose acetate-acetic acid solution diluted is combined with the cellulose fibers to achieve a treated fiber. Excess cellulose acetate-acetic acid solution is removed from the treated fiber and recycled to the mixer used in dilution. The treated fiber is water washed followed by removing water from the washed treated fiber. This product can then be used in paper making to produce a sheet for circuit boards, laminated products, and various paper products.

Abstract: Novel anthracycline derivatives have now been produced, which exhibit higher antitumor activities and lower toxicities than those of daunomycin, adriamycin etc. that have been clinically used as anticancer agents. That is, a daunomycinone or adriamycinone derivative represented by the general formula (I): ##STR1## wherein R is a hydrogen atom or a hydroxyl group.

Abstract: The present invention relates to thermoplastic and biodegradable polysaccharide esters/polysaccharide ether esters, which are characterised in that they can be represented by the general structure ##STR1## wherein Polysaccharide-O represents the substituted OH groups of a polymeric saccharide unit and wherein A is a linear polyether chain of the following structureA=(E--O)nwherein E signifies a linear aliphatic or aromatic branched or unbranched chain having 2 to 11 C atoms, n is an integer equal to or greater than 0 and both B and D are a maleic acid addition product of the following structure ##STR2## wherein F is an aliphatic, saturated, monounsaturated or polyunsaturated carbon skeleton, which may optionally be provided with further substituents and wherein C can be a hydrogen atom, one or more substituents from the group dihydroxyethyl, hydroxypropyl, hydroxybutyl, methyl, ethyl, benzyl, dihydroxypropyl, carboxyalkyl, sulphoalkyl or cyanoethyl.

Abstract: Anthracycline derivatives are disclosed which are coupled to an enzymatically cleavable N-phenyl-O-glycosyl carbamate spacer group, which derivatives are represented by the formula ##STR1## as well as the acid addition salts thereof. Further the synthesis of these derivatives and their use, alone or in combination with enzymes or antibody enzyme conjugates are disclosed.

Abstract: The invention relates to a combination of substances (component I) inducing necrosis in tumors or inflamed tissue with other nontoxic substances ("prodrugs", component II). The enzymes set free by necrotic processes then cleave the nontoxic "prodrug" into the toxic "drug", which leads to massive tumor cell death and/or remission of inflammation.

Abstract: Provided are drug/ligand compounds of Formula (I): ##STR1## (I) in whichD is a drug moiety;n is an integer from 1 to 10;p is an integer from 1 to 6;Y is O or NH.sub.2.sup.+ C1.sup.- ;z is 0 or 1;q is about 1 to about 10;X is a ligand; and,A is a Michael Addition Adduct.In a preferred embodiment, the ligand is an immunoglobulin, preferably a chimeric antibody or fragment thereof. Also provided are formulations comprising as an active ingredient a compound of Formula (I), intermediates useful for preparing the compounds of Formula (I), processes for preparing the compounds of Formula (I), and methods for using the compounds of the invention.

Abstract: The invention relates to methods that permit the rapid construction of oligosaccharides and other glycoconjugates. Methods for forming multiple glycosidic linkages in solution in a single step are disclosed. The invention takes advantage of the discovery that the relative reactivity of glycoside residues containing anomeric sulfoxides and nucleophilic functional groups can be controlled. In another aspect of the invention, the reactivity of activated anomeric sugar sulfoxides is utilized in a solid phase method for the formation of glycosidic linkages. The methods disclosed may be applied to the preparation of specific oligosaccharides and other glycoconjugates, as well as to the preparation of glycosidic libraries comprising mixtures of various oligosaccharides, including glycoconjugates, which can be screened for biological activity.

Abstract: A substance IT-62-B represented by the following formula (1): ##STR1## a production process thereof, a medicinal composition comprising the compound as an active component, and methods of treating an infectious disease caused by bacteria and a tumor, in which such a substance is administered.The compound according to the invention has good antibacterial activities against gram-positive bacteria and some of gram-negative bacteria, and also possesses excellent antitumor activities against tumors such as human nasopharyngeal carcinoma, and is hence useful as a medicine.

Abstract: The present invention relates to new antifungal compounds having the formula ##STR1## wherein R.sup.1 is hydrogen, methyl, or hydroxymethyl; R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen and C.sub.1-5 alkyl; and R.sup.4 is selected from the group consisting of .beta.-L-xylosyl, .beta.-D-ribosyl, .alpha.-L-arabinosyl, .beta.-D-chinovosyl, .beta.-D-fucosyl, and .beta.-D-glucosyl; with the proviso that when R.sup.1 is methyl or hydroxymethyl, and one of R.sup.2 or R.sup.3 is methyl, R.sup.4 is not .beta.-D-glucosyl; or a pharmaceutically acceptable salt thereof.

Abstract: Desalaninebenanomicin A has been synthesized by chemical conversion of benanomicin A. Amino acid derivatives of desalaninebenanomicin A having the general formula (Ia): ##STR1## where R.sup.a represents a hyhrogen atom, a C.sub.1-5 alkyl group, a C.sub.1-5 hydroxyalkyl group, carboxyl group or a lower alkoxycarbonyl group have been synthesized by condensing the 2-carboxyl group of desalaninebenanomicin A with a variety of amino acids. Among the derivatives of the formula (Ia) having antifungal activities, such desalaninebenanomicin A derivatives in which R.sup.a is a C.sub.2-5 alkyl group, a C.sub.2-5 hydroxyalkyl group, carboxyl group or a lower alkoxycarbonyl group are novel semi-synthetic antibiotics having antifungal activities.

Abstract: This invention is a water-soluble high molecular polymerized drug comprising a water-soluble clock copolymer having a hydrophilic segment and a hydrophobic pharmacological-functioning segment to side chain of which a drug is bonded.The hydrophilic first segments of the present invention include polyethylene glycol, polysaccharides, polyacrylamide, and so on.The hydrophobic segments being attached to a drug include polyaspartic acid, polyglutamic acid, polylysine, or derivatives thereof.Drugs to be attached to the hydrophobic segment include anti-cancer drugs, drugs for central nerve, drugs for circulatory organs, and so on.

Abstract: An improved process for surface treating water soluble cellulosic polymers with crosslinking agents to provide products which are more readily dispersible in cold water, and have longer viscosity delay times than can be achieved with polymers treated in low intensity mixers, such as ribbon blenders, comprising distributing the crosslinking agent using a continuous, high intensity mixer, followed by heating to facilitate surface crosslinking. This process also allows for a reduced level of crosslinking chemicals to be used.

Abstract: Immunoconjugates of antibodies or antigen-recognizing fragments of antibodies and monovalent cytotoxic drug derivatives make use of .beta.-alanine derived linkers wherein the antibody or fragment thereof is attached to the linker's carboxy group via an ester or amide group and the drug is attached through the linker's 2-position methylene group. Intermediates, compositions and methods of use also are provided.

Abstract: The present invention relates to the compound UCH9 represented by the following formula: ##STR1## which has antibacterial and anti-tumor activity, and pharmaceutically acceptable salts thereof.

Abstract: Immunoconjugates of antibodies or antigen-recognizing fragments of antibodies and monovalent cytotoxic drug derivatives make use of .beta.-alanine derived linkers wherein the antibody or fragment thereof is attached to the linker's carboxy group via an ester or amide group and the drug is attached through the linker's 2-position methylene group. Intermediates, compositions and methods of use also are provided.

Abstract: Hayumicin compounds, obtainable by cultivation of a strain of Actinomadura sp. designated ATCC 55432, and analogs of these compounds. The novel compounds have antitumor as well as antibiotic, particularly antibacterial, activity.

Abstract: The use of 4'-iodo-4'-deoxydoxorubicin and its pharmaceutically acceptable salts in the treatment of amyloidosis is described.

Abstract: The invention relates to methods that permit the rapid construction of oligosaccharides and other glycoconjugates. Methods for forming multiple glycosidic linkages in solution in a single step are disclosed. The invention takes advantage of the discovery that the relative reactivity of glycoside residues containing anomeric sulfoxides and nucleophilic functional groups can be controlled. In another aspect of the invention, the reactivity of activated anomeric sugar sulfoxides is utilized in a solid phase method for the formation of glycosidic linkages. The methods disclosed may be applied to the preparation of specific oligosaccharides and other glycoconjugates, as well as to the preparation of glycosidic libraries comprising mixtures of various oligosaccharides, including glycoconjugates, which can be screened for biological activity.

Abstract: The present disclosure details novel modified anthracyclines, the synthesis thereof, and their use in treating patients with tumors. Preferred aspects of the disclosure involve modified anthracyclines which have an O-substituted aromatic ring on their sugar moiety. Other preferred aspects of the disclosure involve synthesis steps wherein a hydroxyl group on a sugar moiety to be added is blocked with a halo-substituted alkyl group during the process of adding it to an anthracycline ring compound.

Abstract: Provided are drug/ligand compounds of Formula (I): ##STR1## in which D is a drug moiety;n is an integer from 1 to 10;p is an integer from 1 to 6;Y is O or NH.sub.2.sup.+ C1.sup.- ;z is 0 or 1;q is about 1 to about 10;X is a ligand; and,A is a Michael Addition Adduct.In a preferred embodiment, the ligand is an immunoglobulin, preferably a chimeric antibody or fragment thereof. Also provided are formulations comprising as an active ingredient a compound of Formula (I), intermediates useful for preparing the compounds of Formula (I), processes for preparing the compounds of Formula (I), and methods for using the compounds of the invention.

Abstract: The present invention relates to intermediates, pradimic acids and pradimic acid amides of the formula (II) ##STR1## wherein R is OH or NH.sub.2 ; R.sup.1 is hydrogen or a group of the formula ##STR2## with the proviso that when R is OH, R.sup.1 is not hydrogen; Y is OH or NR.sup.2 R.sup.3 ; R.sup.2 is hydrogen or methyl; R.sup.3 is hydrogen, C.sub.1-5 alkyl, or an amino protecting group; R.sup.4 is hydrogen, hydroxy protecting group, or .beta.-D-xylosyl.The invention relates also to novel processes for the preparation of pradimic acids and pradimic acid amides, as well as novel pradimicin derivatives prepared therefrom.

Abstract: This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.

Abstract: Provided are drug/ligand compounds of Formula (I): ##STR1## in which D is a drug moiety;n is an integer from 1 to 10;p is an integer from 1 to 6;Y is O or NH.sub.2.sup.+ Cl.sup.- ;z is 0 or 1;q is about 1 to about 10;X is a ligand; and,A is a Michael Addition Adduct.In a preferred embodiment, the ligand is an immunoglobulin, preferably a chimeric antibody or fragment thereof. Also provided are formulations comprising as an active ingredient a compound of Formula (I), intermediates useful for preparing the compounds of Formula (I), processes for preparing the compounds of Formula (I), and methods for using the compounds of the invention.

Abstract: The inventive compounds are analogues of sialyl Le.sup.x that inhibit cellular adhesion between a selectin and cells that express sialyl Le.sup.x on their surfaces, and their synthetic intermediates. An inventive compound has structure A, ##STR1## wherein Z is hydrogen, C.sub.1 -C.sub.6 acyl or ##STR2## Y is C(O), SO.sub.2, HNC(O), OC(O) or SC(O); R.sup.1 is an aryl, a substituted aryl or a phenyl C.sub.1 -C.sub.3 alkylene group, wherein an aryl group has one five- or six-membered aromatic ring, a fused five/six-membered aromatic ring, or two fused six-membered aromatic rings, which rings are hydrocarbyl, monooxahydrocarbyl, monothiahydrocarbyl, monoazahydrocarbyl or diazahydrocarbyl rings, and a substituted aryl group is an aryl group having a halo, trifluoromethyl, nitro, C.sub.1 -C.sub.18 alkyl, C.sub.1 -C.sub.18 alkoxy, amino, mono-C.sub.1 -C.sub.18 alkylamino, di-C.sub.1 -C.sub.18 alkylamino, benzylamino, C.sub.1 -C.sub.18 alkylbenzylamino, C.sub.1 -C.sub.18 thioalkyl or C.sub.1 -C.sub.

Abstract: Semisynthetic diastereomerically pure N-glycidylanthracyclines, a process for the stereoselective preparation thereof and the use thereof as cytostatics. The invention relates to anthracyclines having cytostatic activity and the formula I, which are, where appropriate, in the form of a salt with an inorganic or organic acid, ##STR1## in which R.sup.1 is hydrogen or a hydroxyl group,R.sup.2 is hydrogen, a hydroxyl group or an alkyloxy group (C.sub.1 -C.sub.4),R.sup.3 is hydrogen, a hydroxyl group or a structure of the formula II ##STR2## R.sup.4 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH,R.sup.5 is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula II,R.sup.6 is hydrogen, an alkyl group (C.sub.1 -C.sub.4), an allyl group, a benzyl group or mono- or di-methyloxy-substituted benzyl group, a tetrahydropyranyl group,R.sup.7 is hydrogen, an alkyl group (C.sub.1 -C.sub.

Abstract: Novel pyrano heterocyclic anthracycline derivatives are described, which are useful in the treatment of cancer and tumors, such as breast cancer, leukemia, lung cancer, colon cancer, ovarian cancer, renal cancer, and melanoma. As well, these compounds may be used ex vivo for the treatment of cancerous bone marrow before retransplanting said marrow in a patient. Pharmaceutical compositions and methods of preparing the compounds are also described.

Abstract: The present invention provides polymer-bound anthracyclines of formula A which consists essentially of three units represented by formulae 1, 2 and 3: ##STR1## wherein: Gly represents glycine;n is 0 or 1;x is from 70 to 98 mol %,y is from 1 to 29 mol %,z is from 1 to 29 mol %,R.sub.1 is a C.sub.1 -C.sub.6 alkyl group substituted by one or more hydroxy groups;Y is an amino acid residue or a peptide spacer;[NH--D] is the residue of an anthracycline aminoglycoside [NH.sub.2 --D]; andZ is a hydroxy group or a residue of formula --NHR.sub.1 wherein R.sub.1 is as defined above. Methods for their preparation and pharmaceutical compositions containing them are also provided.

Abstract: Glycosylated prodrugs, a preparation method therefor, and their use with tumor-specific immunoenzymatic conjugates for the treatment of cancer, are described. These anthracycline prodrugs have formula (I).

Abstract: Immunoconjugates of antibodies or antigen-recognizing fragments of antibodies and monovalent cytotoxic drug derivatives make use of .beta.-alanine derived linkers wherein the antibody or fragment thereof is attached to the linker's carboxy group via an ester or amide group and the drug is attached through the linker's 2-position methylene group. Intermediates, compositions and methods of use also are provided.

Abstract: Conjugates of general formula 1:[A--O--W--Z].sub.a --T 1wherein the moiety A--O-- is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula 2: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.

Abstract: The present invention provides novel lipophilic drug derivatives which are capable of being formulated in liposomes or micelles. These drug derivatives are known therapeutic agents which are covalently attached to a fatty acid chain of a phospholipid, glyceride, ceramide or 1,2-diacyloxypropane-3-amine. The linkage between the therapeutic agent and the lipid is one which can be cleaved in vivo, allowing the therapeutic agent to be separated from the micellar or liposomal formulation.

Abstract: Anthracycline glycosides of general formula 1 and 2: ##STR1## wherein R.sub.1 is hydrogen or a methoxy group; R.sub.2 is hydrogen, a hydroxy group or represents an acyloxy residue of formula 3 --O--COR.sub.5 wherein R.sub.5 is a linear or branched C.sub.1 -C.sub.8 alkyl, an aryl group or a heterocyclic mono or bicyclic ring, each of which may be unsubstituted or substituted with (a) an amino group NR.sub.6 R.sub.7 in which R.sub.6 and R.sub.7 are independently hydrogen or C.sub.1 -C.sub.4 alkyl or (b) a carboxy group; R.sub.3 and R.sub.4 both represent hydrogen or one of R.sub.3 and R.sub.4 is hydrogen and the other is hydroxy group or a group of formula --OSO.sub.2 R.sub.8 in which R.sub.

Abstract: The invention is directed to the formation of cellulose derivatives using homogenous phase reaction conditions. Cellulose is dissolved using DMAc/LiCl and a reagent system is added to promote the acylation of an appropriate acid anhydride or free carboxylic acid. One reagent system includes N,N-dicyclohexylcarbodiimide (DCC) and 4-pyrrolidinopyridine (PP). Another reagent system includes p-toluene sulfonyl chloride (TsCl) and pyridine (Py).

Abstract: Water soluble or water-dispersible cellulose acetoacetate esters are prepared by contacting a cellulose material with diketene, an alkyl acetoacetate, 2,2,6-trimethyl-4H-1,3-dioxin-4-one or a mixture thereof and a carboxylic anhydride in a solvent system comprising lithium chloride plus a carboxamide. Compositions containing the cellulose acetoacetate esters are useful for coatings applications.

Abstract: Anthracycline glycosides of formula 1: ##STR1## wherein R.sub.1 is hydrogen or methoxy group; R.sub.2 is hydrogen or hydroxy; both R.sub.3 and R.sub.4 represent hydrogen or one of R.sub.3 and R.sub.4 is hydroxy and the other of R.sub.3 and R.sub.4 a represents hydrogen; R.sub.5 represents hydrogen atom or an acyl residue--COX in which X is a C.sub.1 -C.sub.8 linear or branched alkyl chain, an aryl, an aryl lower alkyl, or a 5- or 6-membered heteroaromatic group are anti-tumour agents.

Abstract: An anthracycline glycoside of general formula 1: ##STR1## wherein R.sub.1 is hydrogen or methoxy group; R.sub.2 is hydrogen or hydroxy group, A and B both represent hydrogen or one of A and B is hydrogen and the other is hydroxy or a group of formula --OSO.sub.2 R.sub.5 in which R.sub.5 is C1-C4 alkyl or aryl optionally substituted by C1-C4 alkyl, nitro, amino, methoxy or halogen; R.sub.3 is a hydrogen atom or a group of formula 2 and R.sub.4 is a group of formula 2--(CH.sub.2).sub.n --X 2in which n is 2 or 3 and X is hydroxy group, a halogen or a group of formula --OSO.sub.2 R.sub.5 in which R.sub.5 is as defined above and with the proviso that if R.sub.2, X and A are an hydroxy group and R.sub.3 .dbd.H, n must be 3; or a pharmaceutically acceptable salt thereof.Compounds of the invention have activity as antitumor agents. Processes for their preparation and pharmaceutical composition containing them are also disclosed.

Abstract: Compounds of formulae I and IaR--Y--CO--R.sub.3 --CO--O--A (I),R--Y--CO--R.sub.3 --CO--O--CH.sub.2 --A.sub.1 (Ia),whereinR is a radically polymerisable hydrocarbon group,R.sub.3 is a direct bond, linear or branched C.sub.1 -C.sub.22 alkylene, C.sub.3 -C.sub.8 cycloalkylene or C.sub.6 -C.sub.14 arylene,A is the radical, reduced by a hydroxy group in a 2- or 3position, of a cyclic-oligomeric carbohydrate or of a derivative of such a carbohydrate,A.sub.1 is the radical, reduced by a hydroxymethyl group, of a monomeric or linear oligomeric carbohydrate or of a derivative of such a carbohydrate, andY is --O--, --NH-- or --N(C.sub.1 -C.sub.6 alkyl)-.Homo- and co-polymers having those monomers have, depending upon their composition, hydrophilic, amphiphilic or hydrophobic properties and are able to form hydrogels. The polymers can be used, for example, as surfactants, thickeners, carriers for biologically active ingredients or in the manufacture of contact lenses.

Abstract: Disclosed herein are a novel strain of Streptomyces and a method for the production of aclacinomycins A, B, Y and aglycone thereof by cultivating the same. Streptomyces lavendofoliae DKRS(KCTC 0092BP) of the present invention is capable of producing aclacinomycins A, B, Y and aglycone with higher yield. Further, it is possible to selectively produce aclacinomycin A or Y by adjusting pH of the cultured broth of Streptomyces lavendofoliae DKRS to 4.4 or 4.6 with acetate buffer or hydrochloric acid, respectively.

Abstract: This invention discloses new targeted conjugates for the delivery of a compound, and particularly, a steroid, to vascular endothelial cells. The conjugates comprise two components, preferably linked by a selectively-hydrolyzable bond, such as an acid-labile bond or enzyme-sensitive bond. The first component, a polyanionic polymer, and preferably, a polysulphated polymer such as a heparin-derivative, specifically directs the conjugate to vascular endothelial cells. The second component is a selected agent, such as asteroid, which exerts a specific effect on the target cell following its release. In particular, the present invention provides novel conjugated angiogenesis inhibitors, for use in the treatment of pathogenic conditions including cancer, arthritis, and diabetic blindness.

Abstract: A phenylalanine-glycine derivative of the general formula (I): ##STR1## wherein R represents a residue of an antitumor substance, or a salt or ester thereof, a process for preparation thereof, and a pharmaceutical composition containing the same are described.The novel conjugate of the phenylalanine-glycine derivative and the antitumor substance exhibits superior antitumor activity in comparison with the case wherein an antitumor substance is administered singly or as a mixture with phenylalanine.

Abstract: Disclosed herein are a novel strain of Streptomyces and a method for the production of aclacinomycins A, B, Y and aglycone thereof by cultivating the same. Streptomyces lavendofoliae DKRS (KCTC 0092BP) of the present invention is capable of producing aclacinomycins A, B, Y and aglycone with higher yield. Further, it is possible to selectively produce aclacinomycin A or Y by adjusting pH of the cultured broth of Streptomyces lavendofoliae DKRS to 4.4 or 4.6 with acetate buffer or hydrochloric acid, respectively.

Abstract: A method for site-specific in-vivo activation of a prodrug in an animal using an activator-targeting moiety conjugate to localize an activator at a predetermined site of use and a prodrug compound that is converted to an active drug in the presence of the activator. In the preferred embodiment, the targeting moiety, the activator, and the prodrug demonstrate little or no immunogenicity in the animal being treated. The targeting moiety is relatively specific for binding to the target tissue than to non-target tissue. The activator is not found or present in only small amounts in circulation or in non-target tissue, does not have a substrate for its activity in circulation or in non-target tissue, can be linked to the targeting moiety, and is capable of converting the prodrug to an active drug. The prodrug is selected for its ability to exert a cytotoxic activity on the target tissue after conversion by the activator.

Abstract: Two novel glycosides of 3'-deoxyaquayamycin isolated from an antimicrobial complex produced in fermentation under controlled conditions using a biologically pure culture of the microorganism Streptomyces sp. SCC 2136, ATCC 55186 are disclosed.

Abstract: The present invention relates to intermediates, pradimic acids and pradimic acid amides of the formula (II) ##STR1## wherein R is OH or NH.sub.2 ; R.sup.1 is hydrogen or a group of the formula ##STR2## with the proviso that when R is OH, R.sup.1 is not hydrogen; Y is OH or NR.sup.2 R.sup.3 ; R.sup.2 is hydrogen or methyl; R.sup.3 is hydrogen, C.sub.1-5 alkyl, or an amino protecting group; R.sup.4 is hydrogen, hydroxy protecting group, or .beta.-D-xylosyl. The invention relates also to novel processes for the preparation of pradimic acids and pradimic acid amides, as well as novel pradimicin derivatives prepared therefrom.

Abstract: Chemotherapeutic agents that exhibit cytotoxicity similar to that of daunomycin against cancer cells, but exhibit lessened cytotoxicity against normal, non-transformed cells are disclosed, as are compositions, processes for making and using the same.