Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540, USA.
Bioorg Med Chem Lett. 2010 Aug 1;20(15):4526-30. doi: 10.1016/j.bmcl.2010.06.030. Epub 2010 Jun 8.
A thiazolidine-2,4-dione derivative, 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione (2), was identified as a dual inhibitor of the Raf/MEK/ extracellular signal-regulated kinase (ERK) and the phosphatidylinositol 3-kinase (PI3K)/Akt signaling cascades. The discovered compound inhibited cell proliferation, induced early apoptosis, and arrested cells in G(0)/G(1) phase in human leukemia U937 cells. These results indicate its potential as a new lead compound to develop novel dual signaling pathway inhibitors and anticancer agents.
一种噻唑烷-2,4-二酮衍生物，3-(2-氨基乙基)-5-(3-苯基丙叉基)-噻唑烷-2,4-二酮（2），被鉴定为 Raf/MEK/细胞外信号调节激酶（ERK）和磷脂酰肌醇 3-激酶（PI3K）/Akt 信号通路的双重抑制剂。该发现的化合物抑制细胞增殖，诱导早期细胞凋亡，并使人类白血病 U937 细胞停滞在 G(0)/G(1)期。这些结果表明它有潜力成为开发新型双重信号通路抑制剂和抗癌药物的新先导化合物。
