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Abstract
The series of Mannich bases and one group of related α-aminoketones which had either 1 or 2 sites for thiol alkylation were evaluated against the WiDr tumour in vitro. Maximum activity was found in the bis alkylating agents (12–64 times the activity of the reference compound, 5-fluorouracil) and one of these bis Mannich bases had confirmed activity against murine P388 lymphocytic leukemia. No correlations were found with either the rate of alkylation with glutathione or the apparent partition coefficients of selected compounds with activity against the WiDr tumour in vitro.
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