The Scripps Research Institute

Brunswick Corporation

Biotechnetics

Wolfgang A Wrasidlo

Kyriacos Costa Nicolaou

Peter Emmanuel Maligres

John H Norman

Karol J Mysels

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. A contemplated chemotherapeutic agent is a daunomycin derivative whose structure corresponds to structural Formula I, wherein Ar is phenyl, 1-naphthyl or 2-naphthyl ##STR1##

Daunomycin derivative with reduced cytotoxicity toward normal cells

The invention provides for antinomycin D derivatives and methods of producing antinomycin D derivatives. Such derivatives include isocyanate, thioisocyanate, carboxylic acid, bromide, aldehyde and sulfonic acid derivatives. The invention also provides for actinomycin D derivatives conjugated to target cell binding proteins. Methods are provided to make such conjugates through attachment of the derivatized moiety to a reactive group on a target cell binding protein or on a spacer. The conjugates can be administered to an animal and produce localized cytotoxic effects on target cells.

Methods of conjugating actinomycin D

A method and generator for preparing the radioisotope of lead, .sup.212 Pb, whereby .sup.228 Th, in a closed chamber, is allowed to decay to gaseous .sup.220 Rn which is then readily separated from the thorium and other decay products by diffusing the .sup.220 Rn gas into a second chamber, where it decays to .sup.212 Pb which can then be collected from the second chamber. The .sup.228 Th preferably is amorphous, such as thorium stearate. Collection of .sup.212 Pb occurs in a medium of high and open porosity into which the .sup.220 Rn diffuses so that the decay products recoil into the medium. The .sup.212 Pb can be recovered from this medium by dissolving the medium or by reacting it with an antibody-chelating complex solution to entrap it in the antibody-chelating complex.

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La Jolla, CA, United States of America

Wolfgang A Wrasidlo