Dipartimento di Scienze Farmaceutiche, Universita di Bologna, Bologna, Italy.
J Med Chem. 2010 Aug 12;53(15):5567-75. doi: 10.1021/jm1007165.
The synthesis of new substituted E-3-(3-indolylmethylene)-1,3-dihydroindol-2-ones is reported. The antitumor activity was evaluated according to protocols available at the National Cancer Institute (NCI), Bethesda, MD. Structure-activity relationships are discussed. The action of selected compounds was investigated in MCF-7 breast cancer cells. The ability of these derivatives to inhibit cellular proliferation was accompanied by increased level of p53 and its transcriptional targets p21 and Bax, interference in the cell cycle progression with cell accumulation in the G2/M phase, and activation of apoptosis.
报告了新型取代的 E-3-(3-吲哚亚甲基)-1,3-二氢吲哚-2-酮的合成。根据马里兰州贝塞斯达的国家癌症研究所 (NCI) 的可用方案评估了抗肿瘤活性。讨论了结构-活性关系。在 MCF-7 乳腺癌细胞中研究了选定化合物的作用。这些衍生物抑制细胞增殖的能力伴随着 p53 及其转录靶标 p21 和 Bax 的水平升高，细胞周期进展受阻，细胞在 G2/M 期积累，以及凋亡激活。
