Peck R M, Peck E B
Cancer Res. 1980 Mar;40(3):782-5.
Carcinogenic bromomethyl- and chloromethylanthracenes and benz(a)anthracenes were found to react rapidly in vitro with DNA under physiological conditions and to varying degrees with nucleotides and nucleosides. The compounds were assayed for production of lung adenomas in strain A mice and relative carcinogenic potencies were compared with in vitro alkylation and with in vitro solvolysis rates. Success at quantitative correlation with carcinogenic potency was not obtained with either in vitro parameter. However, comparable noncarcinogenic compounds lacked their marked in vitro reactivity with DNA. Some potential polynuclear electrophiles, including chloromethyl derivatives of acridine and benz(c)acridine, a hydroxymethyl and an acetoxymethyl derivative of benz(a)anthracene, an acetoxymethylanthracene, and an acridinylglycine ester, were found not to be carcinogenic in the lung adenoma test.
致癌性溴甲基蒽和氯甲基蒽以及苯并(a)蒽在生理条件下于体外能迅速与DNA发生反应，并且与核苷酸和核苷也有不同程度的反应。对这些化合物进行了检测，观察其在A系小鼠中诱发肺腺瘤的情况，并将其相对致癌效力与体外烷基化作用及体外溶剂解速率进行了比较。无论是哪种体外参数，都未能成功实现与致癌效力的定量相关性。然而，具有可比性的非致癌化合物在体外与DNA缺乏明显的反应活性。一些潜在的多环亲电试剂，包括吖啶和苯并(c)吖啶的氯甲基衍生物、苯并(a)蒽的羟甲基和乙酰氧基甲基衍生物、乙酰氧基甲基蒽以及吖啶基甘氨酸酯，在肺腺瘤试验中被发现无致癌性。
