Hall I H, Chapman J M, Wong O T
Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina at Chapel Hill 27599.
Anticancer Drugs. 1994 Feb;5(1):75-82. doi: 10.1097/00001813-199402000-00012.
Cyclic imides such as N-substituted alkyl ethers, thioethers, sulfoxides, sulfones and related derivatives were potent agents against human single cell tumors and selected solid tumor growths, eg adenocarcinoma of the colon and glioma. These agents in the L1210 lymphoid leukemia tumor model preferentially inhibited DNA synthesis. The regulatory enzyme sites in the purine pathway were targets of the agents. Other sites of inhibition were DNA polymerase alpha and thymidylate synthetase activities. d(NTP) pool levels were also reduced by the agents over 60 min.
环状酰亚胺类化合物，如N-取代烷基醚、硫醚、亚砜、砜及相关衍生物，是抗人类单细胞肿瘤和某些实体瘤生长（如结肠癌和神经胶质瘤）的强效药物。在L1210淋巴细胞白血病肿瘤模型中，这些药物优先抑制DNA合成。嘌呤途径中的调节酶位点是这些药物的作用靶点。其他抑制位点包括DNA聚合酶α和胸苷酸合成酶活性。这些药物在60分钟内还降低了d（NTP）池水平。
