Premium
Neoflavonoids and Tetrahydroquinolones as Possible Cancer Chemopreventive Agents
Author(s) -
Luqman Suaib,
Meena Abha,
Singh Pragya,
Kondratyuk Tamara P.,
Marler Laura E.,
Pezzuto John M.,
Negi Arvind S.
Publication year - 2012
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2012.01439.x
Subject(s) - aromatase , reductase , chemistry , quinone , enzyme , in vivo , in vitro , biochemistry , pharmacology , cancer , stereochemistry , biology , breast cancer , genetics
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 NFκB, aromatase, and quinone reductase 1. These analogs blocked TNF‐α‐induced NFκB activation in a dose‐dependent manner with IC 50 values in the range of 0.11–3.2 μ m . In addition, compound 8 inhibited aromatase activity with an IC 50 value of 12.12 μ m , and compound 10 affected quinone reductase 1 induction (IR, 3.6; CD, 19.57 μ 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 NFκB 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.