Laboratoire de Pharmacochimie Moléculaire et Cellulaire, Université Paris Descartes, UFR Biomédicale, 45 rue des Saints-Pères, Paris, F-75006, France; INSERM U648, Paris F-75006, France.
Eur J Med Chem. 2010 Mar;45(3):896-901. doi: 10.1016/j.ejmech.2009.11.028. Epub 2009 Dec 6.
We report herein the synthesis of 5-substituted [1]pyrindine derivatives and the evaluation of their antiproliferative properties on HeLa cells, a cervical carcinoma tumor cell line, and on the melanoma A2058 cell line. The most efficient compounds display cytotoxicity against tumor cells in the micromolar range but have interestingly no effect against the normal human fibroblasts CRL-2796. Generally, these pyrindines are active on both tumor cell lines. Compounds bearing large substituents with structural rigidity at position 5 such as phenyl-furyl show no inhibition of cell growth.
我们在此报告 5-取代的[1]吡啶并嘧啶衍生物的合成及其对宫颈癌肿瘤细胞系 HeLa 和黑色素瘤 A2058 细胞系的抗增殖活性的评价。最有效的化合物在微摩尔范围内对肿瘤细胞表现出细胞毒性，但对正常人类成纤维细胞 CRL-2796 没有影响。通常，这些吡啶并嘧啶对两种肿瘤细胞系都有活性。在 5 位具有结构刚性的大取代基如苯基-呋喃基的化合物则不抑制细胞生长。
