Dipartimento Farmacochimico, Tossicologico e Biologico, Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Bioorg Med Chem. 2010 Jun 15;18(12):4524-9. doi: 10.1016/j.bmc.2010.04.061. Epub 2010 Apr 28.
A series of novel 2,5-bis(3'-indolyl)furans and 3,5-bis(3'-indolyl)isoxazoles were synthesized as antitumor agents. The antiproliferative activity was evaluated in vitro toward diverse human tumor cell lines. Initially 5 isoxazoles and 3 furan derivatives were tested against a panel of 10 human tumor cell lines and the most active derivatives 3c and 4a were selected to be evaluated in an extended panel of 29 cell lines. By exhibiting mean IC(50) values of 17.4 microg/mL (3a) and 20.5 microg/mL (4c), in particular 4c showed a high level of tumor selectivity toward the 29 cell lines.
一系列新型 2,5-双(3'-吲哚基)呋喃和 3,5-双(3'-吲哚基)异恶唑被合成作为抗肿瘤剂。在体外对多种人肿瘤细胞系进行了抗增殖活性评估。最初，5 个异恶唑和 3 个呋喃衍生物对 10 个人类肿瘤细胞系进行了测试，最活跃的衍生物 3c 和 4a 被选择在 29 个细胞系的扩展面板中进行评估。通过表现出平均 IC(50)值为 17.4μg/mL(3a)和 20.5μg/mL(4c)，特别是 4c 对 29 个细胞系显示出高水平的肿瘤选择性。
