Abstract: Phosphate derivatives of 4'-demethylepipodophyllotoxin glucosides are novel antitumor agents and the salts thereof offer the pharmaceutical advantage of high water solubility.

Abstract: This invention relates to a novel method for the delivery of cytotoxic drugs to tumor cells by the administration of a tumor-specific antibody-enzyme conjugate that binds to the tumor cells, and the additional administration of a prodrug that is converted at the tumor site, in the presence of the antibody-bound enzyme, to an active cytotoxic drug. According to preferred embodiments of this invention, antibody-enzyme conjugates containing the enzyme, alkaline phosphatase ("AP"), have been used in conjunction with the novel prodrug, etoposide-4'-phosphate or 7-(2'-aminoethyl phosphate)mitomycin or a combination thereof, to effect killing of tumor cells. According to another embodiment of the invention, an antibody-enzyme conjugate containing the enzyme, penicillin V amidase ("PVA"), has been used in conjunction with a novel prodrug, N-(p-hydroxyphenoxyacetyl)adriamycin to effect killing of tumor cells.

Abstract: There is disclosed a drug-monoclonal antibody conjugate wherein the antibody is linked to a antitumor drug using disulfide benzyl carbamate or carbonate as the linker. Also disclosed is a method of delivering an active antitumor drug to the site of tumor cells in a mammal by administering the drug-monoclonal antibody conjugate.

Abstract: Phosphate derivatives of 4'-demethylepipodophyllotoxin glucosides are novel antitumor agents and the salts thereof offer the pharmaceutical advantage of high water solubility.

Abstract: Immunotoxins having improved toxic activity have the composition ##STR1## wherein Toxin-NH is a ribosome-inactivating protein containing no accessible sulfhydryl groups, n is an integer from 1 to 5, m is an integer from 1 to 5, and NH-Antibody is a monoclonal antibody specific to eucaryotic cells or antigens associated therewith. The immunotoxins are made by reacting the Toxin-NH with an iminothiolester salt to form a first conjugate, reacting the NH-Antibody with N-succinimidyl-3-(2-pyridyldithio) propionate to form a second conjugate, and reacting the two conjugates to form the immunotoxin.

Abstract: Disclosed herein are N.sup.7 -alkylphosphate derivatives of mitomycin C and porfiromycin showing antitumor activity against transplanted human tumor and reduced toxicity relative to the parent N.sup.7 -alkanol mitomycin compounds.

Abstract: A photo-cleavable compound for delivery and release of a biologically active substance to selected target cells; the compound includes a binding partner for a specific cell-surface receptor of those target cells, the biologically active substance to be delivered, and a photo-cleavable bridge between the binding partner and the biologically active substance. When the compound is exposed to a heterogeneous population of target and non-target cells, it binds selectively to the receptors on the surface of the target cells. Exposing the compound to light of selected wave length cleaves it, yielding the active substance.

Abstract: Amino-sulfhydryl cross-linking reagents that are cleavable under mildly acidic conditions are disclosed. Also disclosed are methods of making the cross-linkers, as well as methods of using the cross-linkers, e.g., to deliver a biologically active substance across the membranes of selected cells in a heterogeneous cell population; once inside the cell the active substance is released, intact, by the transient, mild acidity of certain cell structure. Finally, a method of characterizing complex multi-chain protein structures is disclosed.

Abstract: Amino-sulfhydryl cross-linking reagents that are cleavable under mildly acidic conditions are disclosed. Also disclosed are methods of making the cross-linkers, as well as methods of using the cross-linkers, e.g., to deliver a biologically active substance across the membranes of selected cells in a heterogeneous cell population; once inside the cell the active substance is released, intact, by the transient, mild acidity of certain cell structures. Finally, a method of characterizing complex multi-chain protein structures is disclosed.

Abstract: Amino-sulfhydryl cross-linking reagents that are cleavable under mildly acidic conditions are disclosed. Also disclosed are methods of making the cross-linkers, as well as methods of using the cross-linkers, e.g., to deliver a biologically active substance across the membranes of selected cells in a heterogeneous cell population; once inside the cell the active substance is released, intact, by the transient, mild acidity of certain cell structures. Finally, a method of characterizing complex multi-chain protein structures is disclosed.