Neoflavonoids and tetrahydroquinolones as possible cancer chemopreventive agents.

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Luqman S, Meena A, Singh P, Kondratyuk TP, Marler LE, Pezzuto JM, Negi AS

Neoflavonoids and tetrahydroquinolones as possible cancer chemopreventive agents.

Chem Biol Drug Des. 2012 Oct;80(4):616-24. doi: 10.1111/j.1747-0285.2012.01439.x. Epub 2012 Jul 25.

PubMed ID
22726671 [ View in PubMed
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Abstract

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 NFkappaB, aromatase, and quinone reductase 1. These analogs blocked TNF-alpha-induced NFkappaB activation in a dose-dependent manner with IC(5)(0) values in the range of 0.11-3.2 muM. In addition, compound 8 inhibited aromatase activity with an IC(5)(0) value of 12.12 muM, and compound 10 affected quinone reductase 1 induction (IR, 3.6; CD, 19.57 muM). 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 NFkappaB 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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
NaringeninCytochrome P450 19A1Ki (nM)0.00109662N/AN/ADetails
NaringeninCytochrome P450 19A1IC 50 (nM)1.00E+03N/AN/ADetails