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Transport and Accumulation of Triazenoimidazoles by L1210 Cells¹

Department of Pharmacology, University of Rochester School of Medicine, Rochester, New York 14620

Transport of 5-(dimethyltriazeno)imidazole-4-carboxamide (NSC 45388) and the 3,3-bis(2-chloroethyl) derivative (NSC 82196) was studied in vitro in L1210 cells and in drug-resistant sublines. Uptake of both compounds was temperature sensitive and apparently nonsaturable. Accumulated NSC 45388 could be removed from the cells by brief suspension in buffer at 37°. In contrast, accumulated NSC 82196 was not readily washed out. Under ultraviolet irradiation, NSC 45388 dissociates to form an unstable compound, presumably 5-diazoimidazole-4-carboxamide. The latter was extensively bound to L1210 cells, even at 0°. Sublines of L1210 selected for resistance to NSC 45388 and NSC 82196 showed no impairment in capacity for drug accumulation; retention of accumulated NSC 82196 labeled in the bis(chloroethyl) side chain was impaired in L1210/82196.

¹ Supported by Contract NIH 69-39 with Chemotherapy, National Cancer Institute, NIH, Grant CA 11198-01 from the NIH, an institutional grant (GRSG), and funds from the Monroe Country Cancer and Leukemia Association.

Received 4/23/70. Accepted 9/29/70.