A number of modifications have been made in the formyl thiosemicarbazone side chain of 1-formylisoquinoline thiosemicarbazone to ascertain the importance of this part of the molecule for antineoplastic activity; tumorinhibitory potency and host toxicity of these compounds were assessed in mice bearing Sarcoma 180 ascites cells. Substitutions made on the different positions of the side chain resulted in either a diminution or a total loss of tumor-inhibitory activity, indicating that the intactness of this portion of the molecule was essential for 1-formvlisoquinoline thiosemicarbazone to function as an inhibitor of the growth of malignant cells. © 1969, American Chemical Society. All rights reserved.