Jurd L, Narayanan V L, Paull K D
Developmental Therapeutics Program, National Cancer Institute, Bethesda, Maryland 20892.
J Med Chem. 1987 Oct;30(10):1752-6. doi: 10.1021/jm00393a012.
A series of 6-benzyl-1,3-benzodioxoles have been synthesized and evaluated against the in vivo ip P388 murine lymphocytic leukemia. Selected activities against this system were tested against the additional in vivo systems L1210, B16, M5076, and MX1. The most active of the 6-benzyl-1,3-benzodioxoles tested were as effective as podophyllotoxin as experimental antitumor agents in vivo, but larger doses were required. Three of the P388-active series members were active against the in vitro astrocytoma assay, which detects compounds that interfere with or bind to tubulin.
已合成了一系列6-苄基-1,3-苯并二氧杂环戊烯，并对其进行了体内腹腔注射P388小鼠淋巴细胞白血病的评估。针对该系统的选定活性在另外的体内系统L1210、B16、M5076和MX1中进行了测试。所测试的6-苄基-1,3-苯并二氧杂环戊烯中最具活性的化合物作为实验性抗肿瘤药物在体内与鬼臼毒素一样有效，但需要更大的剂量。P388活性系列成员中的三种对体外星形细胞瘤试验有活性，该试验可检测干扰或结合微管蛋白的化合物。
