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Anticancer Activity of Bisthiosemicarbazones of Methylglyoxal¹

Laboratories of the Medical Research Council of Ireland, Trinity College, Dublin, Ireland

Methylglyoxal-1-thiosemicarbazone-2-N⁴-substituted thiosemicarbazones (A isomers) and the isomeric 1-N⁴-substituted thiosemicarbazones-2-thiosemicarbazone (B isomers) have been synthesized as anticancer agents. A number of these compounds show high antitumor activity against Sarcoma 180 in the mouse. The most active compounds are those in which the N⁴-substitutent is methyl, ethyl, or n-propyl. The antiumor activity is not antagonized by pyridoxine.

¹ This work was supported financially by May and Baker Ltd., Dagenham, Essex; Arthur Guinness Son & Co. (Dublin) Ltd.; Irish Hospital Sweepstakes Ltd.; Irish Hospitals Trust Ltd.; The Children's Cancer Research Foundation Inc., Boston; Conquer Cancer Campaign (Ireland); Southern Chemicals Ltd., Askeaton; Roadstone Ltd.; Carbide Ltd., Collooney; Rathdrum Parish Church (per Canon R. K. W. Lowe); T. W. Breaden, F.I.C.I.

Received 2/14/66.