摘要
一系列 1,4 代用品 phthalazine 衍生物被设计并且综合。所有准备混合物在 vitro 对 A549， HT-29 和 MDA-MB-231 房间线为他们的细胞毒素的活动被屏蔽。在他们之中，混合物 7a 鈥 ? h 从 1 nmol/L 与 IC50 价值为 MDA-MB-231 房间线显示出优秀选择到 0.92 渭 m ol/L。这些衍生物的初步的 SAR 研究被执行。
A series of 1,4-substituted phthalazine derivatives were designed and synthesized.All the prepared compounds were screened for their cytotoxic activities against A549.HT-29 and MDA-MB-231 cell lines in vitro.Among them,compounds 7a-7h showed excellent selectivity for MDA-MB-231 cell line with IC50 values from 1 nmol/L to 0.92μmol/L.A preliminary SAR study of these derivatives was performed.
