Uptake of acridinecarboxamide derivatives by L1210 cells

The uptake of six 9-aminoacridinecarboxamide derivatives by L1210 cells in relation to their lipophilicity and cytotoxic activity was studied. The amo unt of acridines taken up by cells was estimated by fluorimetric measuremen ts. It was found that the uptake efficiency of this class of compounds by c ells depends on the size of carboxamide residue as well as on position of t he substituent. The increase of size of carboxamide chain resulted in the l oss of capability of acridines to penetrate cell membrane. Cytotoxic effect s of acridines were well correlated with the level of drugs accumulated by cells, whereas no clear correlation between uptake and lipophilicity was ob served. It is concluded that uptake of 9-aminoacridinecarboxamides is the m ost important factor determining their antiparoliferative activity.