Neoflavonoids and Tetrahydroquinolones as Possible Cancer Chemopreventive Agents

作者：Luqman Suaib; Meena Abha; Singh Pragya; Kondratyuk Tamara P; Marler Laura E; Pezzuto John M; Negi Arvind S^*

来源：Chemical Biology & Drug Design, 2012, 80(4): 616-624.

DOI：10.1111/j.1747-0285.2012.01439.x

• aromatase
• cancer chemoprevention
• Neoflavonoids
• NF?B
• quinone reductase 1
• tetrahydroquinoline

Several lactone- and lactam-based neoflavonoids and tetrahydroquinolones were synthesized and evaluated for cancer chemopreventive studies using cell and molecular target-based in vitro bioassays, namely NF?B, aromatase, and quinone reductase 1. These analogs blocked TNF-a-induced NF?B activation in a dose-dependent manner with IC50 values in the range of 0.113.2 mu m. In addition, compound 8 inhibited aromatase activity with an IC50 value of 12.12 mu m, and compound 10 affected quinone reductase 1 induction (IR, 3.6; CD, 19.57 mu m). Neoflavonoids 8 and 10 exhibiting good results can further be optimized for improved therapeutic profiles. However, investigations into the actions of neoflavonoids and tetrahydroquinolones, especially those related to the NF?B signaling pathway, aromatase inhibition, induction of quinone reductase 1 expression, and in vivo studies could provide new insights into the cancer chemopreventive ability of these molecules.

• 出版日期2012-10
• 单位河北医科大学