Flavonoid Derivatives

Flavonoids make one of the most preferred groups of natural chemotypes tested for various biological activities. Flavonoids have low toxicity and are widely available in plants, including edible.

This group of compounds provides a good example of “natural fit” holding leading performance in anti-inflammatory, anticancer, anti-oxidant activities.

9 Core Flavonoid structures are used to assemble TimTec small collection of 500 Flavonoids Derivatives.

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9 Core Flavonoid structures

Chalcone	Flavanone	Flavone
Dihydroflavonol	Flavonol	Flavan
Stilbene	Isoflavonoid	Neoflavonoid

Following the screens of TimTec compounds and compound collections involving flavonoids:

Narwal M, Haikarainen T, et.al. Screening and structural analysis of flavones inhibiting tankyrases. J Med Chem. 2013 May 9;56(9):3507-17. doi: 10.1021/jm3018783

Holder S., et al., Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinase. Mol Cancer Ther. Jan. 2007, 6(1), 163-172

Bullock A.N., et al. Structural Basis of Inhibitor Specificity of the Human Protooncogene Proviral Insertion Site in Moloney Murine Leukemia Virus (PIM-1) Kinase. J. Med. Chem., 2005, 48 (24), pp 7604–7614

Auld, D. S., Characterization of Chemical Libraries for Luciferase Inhibitory Activity. J. Med. Chem., 2008, 51 (8), pp 2372–2386

Selected references highlighting flavonoids therapeutic benefits:

Cushnie TP, Lamb AJ. Recent advances in understanding the antibacterial properties of flavonoids. Int J Antimicrob Agents. 2011 Aug;38(2):99-107.

Nishiumi S, Miyamoto S, et.al. Dietary flavonoids as cancer-preventive and therapeutic biofactors.Front Biosci (Schol Ed). 2011 Jun 1;3:1332-62.

González R, Ballester I, et.al. Effects of flavonoids and other polyphenols on inflammation.Crit Rev Food Sci Nutr. 2011 Apr;51(4):331-62.