Journal of pharmaceutical sciences

Protection of murine L1210 leukemia and bone marrow progenitor cells against mechlorethamine and inhibition of choline uptake as a structure-activity relationship of 2-dimethylaminoethanol and its analogues.

PMID 6694079


The structure-activity relationships of 2-dimethylaminoethanol and its analogues as protectors against mechlorethamine cytotoxicity and as inhibitors of choline uptake were evaluated. Of a series of inhibitors and protectors, 2-dimethylaminoethanol was the most potent inhibitor of choline uptake and the most potent protector of both hematopoietic progenitor cells and murine L1210 leukemia cells. Two analogues that exhibited both potent protection and inhibition were 1-dimethylamino-2-propanol and 2-ethylmethylaminoethanol. 2-Di-n-butylaminoethanol, while protecting against mechlorethamine cytotoxicity, was not an inhibitor of choline uptake. 2-n-Butylmethylaminoethanol, while an inhibitor of choline uptake, was not a protector against mechlorethamine cytotoxicity. Addition of 2-dimethylaminoethanol to mechlorethamine in a mole ratio of 1000:1 did not improve survival of tumor-bearing mice beyond that of mice treated with mechlorethamine alone.

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