Wieczorek J, Peczyńska-Czoch W, Mordarski M, Kaczmarek L, Nantka-Namirski P
Arch Immunol Ther Exp (Warsz). 1986;34(3):315-21.
alpha-Carboline and its several derivatives have been synthesized and evaluated for their antitumor activity against L1210 lymphoid leukemia, P388 lymphocytic leukemia and Sarcoma 180. It was found that of these compounds only alpha-carboline and its derivatives substituted in C-4 position with a methyl group or in 6-C position with a methyl group and fluorine or chlorine atoms caused moderate inhibition of the tumor growth of Sarcoma 180. The introduction of bromide, iodide atoms, hydroxy-, amino-groups or some other substituents in C-6 position of alpha-carboline molecule reduced significantly the biological activity of the tested compounds against Sarcoma 180. Additionally, the introduction of an ethyl or ethoxycarbonyl group to the pyrrole ring at N-9 also obliterated antitumor properties of these analogues. None of the tested compounds displayed a significant activity against murine leukemias. In the cytotoxicity test of KB cells all the compounds were inactive.
已合成了α-咔啉及其几种衍生物，并评估了它们对L1210淋巴白血病、P388淋巴细胞白血病和肉瘤180的抗肿瘤活性。结果发现，在这些化合物中，只有在C-4位被甲基取代、或在6-C位被甲基以及氟或氯原子取代的α-咔啉及其衍生物对肉瘤180的肿瘤生长有中等程度的抑制作用。在α-咔啉分子的C-6位引入溴、碘原子、羟基、氨基或其他一些取代基，会显著降低受试化合物对肉瘤180的生物活性。此外，在N-9位的吡咯环上引入乙基或乙氧羰基也会消除这些类似物的抗肿瘤特性。所有受试化合物对小鼠白血病均无显著活性。在KB细胞的细胞毒性试验中，所有化合物均无活性。
