Abstract: A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.

Abstract: A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.

Abstract: Quinone- and hydroquinone-containing cyclic enediyneols and enediyneones having 10-carbon atoms in the enediyne-containing ring that cleave DNA are disclosed, as are methods of making and using the same.

Abstract: Chimeric analogs of calicheamicin that include an analog of calicheamicinone linked to an ester or glycoside, (-)-calicheamicinone and its analogs are disclosed.

Abstract: The synthesis of stable, ten-membered, cyclic conjugated enediynes is described. Said compounds were successfully employed to cleave double-stranded DNA spontaneously at ambient temperatures.

Abstract: Phosphine oxide-terminated allene-ene-yne compounds are disclosed that possess DNA-cleaving, antimicobial and tumor growth-inhibiting properties. Methods of making and using those compounds are also disclosed.

Abstract: Macrocyclic enediynediols and enediynediones having a ten carbon ring and open chain enediyne dihydroperoxides having eight carbons between the hydroperoxide groups that cleave DNA are disclosed, as are methods of making and using the same.

Abstract: 5-Hydroxy-benzo-(1',2')-cyclodeca-2,7-diyne-1-one and derivatives thereof and related fused ring diyneone macrocyclic compounds are disclosed. The compounds possess DNA-cleaving, antibiotic and tumor growth-inhibiting properties. Methods of making and using the same are also disclosed.

Abstract: An improved method for synthesizing leukotriene B.sub.4 and derivatives thereof is disclosed, as are novel intermediates used in the process. Unlike prior art processes, the method of this invention involves a step in which 2(R)-[[(1,1-dimethylethyl)diphenylsilyl]oxy]dec-4 (Z)-ene-1-ol or a related compound is coupled with methyl-[5(S)-[[1,1dimethylethyl)-diphenylsilyl]oxy]-dec-8 (E)-10-(dimethylphosphono)-6-ynoate.

Abstract: The synthesis of stable, ten-membered cyclic conjugated enediynes is described. Said compounds were successfully employed to cleave double-stranded DNA spontaneously at ambient temperatures.

Abstract: The novel sesquiterpene epoxides trans-(Z)-1-methyl-4-(1,5-dimethyl-1,4-hexadienyl)-1,2-epoxycyclohexane and cis-(z)-1-methyl-4-(1,5-dimethyl-1,4-hexadienyl)-1,2-expoxycyclohexane have been isolated from N. viridula adult males, and have been successfully synthesized. The compounds are useful for the production of synthetic sex attractants for N. viridula and its parasitoids.

Abstract: Novel, optically active azido alcohols are synthesized from N-haloacetyl oxazolidinone and are coupled with protected, activated carbohydrate residues in stereoselective glycosidic fashion to provide glycolipids in substantially pure stereochemical form. In accordance with certain preferred embodiments, the glycosphingolipids globotriaosylceramide, lactosyl ceramide, and galactosyl ceramide are synthesized in substantially pure stereochemical form from alkenyl, C-18 azido alcohols and protected fluoroglycosides and are employed as antigens in the production of antibodies useful, for example, in the treatment of disease.

Abstract: A series of alkanoarachidonic acids have been prepared as modulators of the arachidonic acid cascade to increase the production of biologically desirable compounds and minimize the production of biologically undesirable compounds. Examples of desirable compounds in this respect comprise postaglandins and thromboxanes whereas undesirable compounds comprise the mono- and polyhydroxyarachidonic acids and leukotrienes. The alkanoarachidonic acids and their intermediates are of the general formula: ##STR1## and at least one of X, Y, and Z is lower alkano and is hydrogen when not lower alkano; the esters and salts of the acids are also prepared. The acids, esters and salts may be used as anti-anaphylaxis or anti-thrombosis agents.

Abstract: A compound of the formula ##STR1## wherein n is an integer from 2 to 4;m is an integer from 3 to 5;R is OM, OR.sub.1 or NR.sub.2 R.sub.3 where M is a pharmaceutically acceptable cation;R.sub.1, R.sub.2 and R.sub.3 are the same or different and selected from the group consisting of hydrogen, C.sub.1 -C.sub.2 branched, unbranched or cyclic alkyl aryl and aralkyl; or R.sub.2 and R.sub.3 taken together from a group of the formula ##STR2## can be used as an inhibitor of the lipoxygenase pathway of the arachidonic acid cascade in animals.

Abstract: A compound of the formula ##STR1## wherein n is an integer from 2 to 4; m is an integer from 3 to 5; R is OM, OR.sub.1 or NR.sub.2 R.sub.3 where M is a pharmaceutically acceptable cation;R.sub.1, R.sub.2 and R.sub.3 are the same or different and selected from the group consisting of hydrogen, C.sub.1 -C.sub.12 branched, unbranched or cyclic alkyl, aryl and aralkyl; or R.sub.2 and R.sub.3 taken together form a group of the formula ##STR2## can be used as an inhibitor of the lipoxygenase pathway of the arachidonic acid cascade in animals.

Abstract: Stable biologically active thromboxane A.sub.2 analogues having the formula: ##STR1## wherein R.sup.1 is OR.sup.3, where R.sup.3 represents hydrogen or a pharmaceutically acceptable cation or lower alkyl group; orR.sup.1 is NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are the same or different substituents selected from the group consisting of hydrogen and lower alkyl group; andR.sup.2 is hydrogen or an --OH group.The thromboxane analogues are potent thrombotic agents, useful in cardiovascular treatment.

Abstract: Stable biologically active thromboxane A.sub.2 analogues having the formula: ##STR1## wherein R.sup.1 is OR.sup.3, where R.sup.3 represents hydrogen or a pharmaceutically acceptable cation or lower alkyl group; orR.sup.1 is NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are the same or different substituents selected from the group consisting of hydrogen and lower alkyl group; andR.sup.2 is hydrogen or an -OH group.The thromboxane analogues are potent thrombotic agents, useful in cardiovascular treatment.

Abstract: Stable biologically active thromboxane A.sub.2 analogues having the formula ##STR1## wherein R.sup.1 is OR.sup.3, where R.sup.3 represents hydrogen or a pharmaceutically acceptable cation or lower alkyl group; orR.sup.1 is NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are the same or different substituents selected from the group consisting of hydrogen and lower alkyl group; andR.sup.2 is hydrogen or an --OH group.

Abstract: Stable biologically active 6,9 .alpha.-thiaprostacyclin derivatives having the formula ##STR1## wherein X represents >S, >SO or >SO.sub.2 ;Y represents (E) and(Z)-->C.dbd.CH--CH.sub.2 CH.sub.2 CH.sub.2 COOR,(E)-->CH--CH.dbd.CH--CH.sub.2 CH.sub.2 COOR or >CH--CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 COOR; andR represents hydrogen, a pharmaceutically acceptable cation or a pharmaceutically acceptable lower alkyl group.

Abstract: Stable biologically active thromboxane A.sub.2 analogues having the formula: ##STR1## wherein R.sup.1 is OR.sup.3, where R.sup.3 represents hydrogen or a pharmaceutically acceptable cation or lower alkyl group; orR.sup.1 is NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are the same or different substituents selected from the group consisting of hydrogen and lower alkyl group; andR.sup.2 is hydrogen or an --OH group.The thromboxane analogues are potent thrombotic agents, useful in cardiovascular treatment.