Flavonoids

Flavonoids make one of the most preferred groups of natural chemotypes tested for various biological activities. Flavonoids have low toxicity and are found in a variety of plants such as fruits, vegetables and flowers. Specific sources include Citrus, Garlic, Teas, and certain berries. Flavonoids are also known as bioflavonoids or Vitamin P/citrin.

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
Anthocyanin	Isoflavonoid	Neoflavonoid

Selected Reference:

Watternberg, L. W., et al. Inhibition of carcinogen-induced pulmonary and mammary carcinogenesis by chalcone administered subsequent to carcinogen exposure. Cancer Lett. 1994, 83, 165-169

Lo Piparo E., et al. Flavonoids for Controlling Starch Digestion: Structural Requirements for Inhibiting Human a-Amylase. J. Med. Chem., 2008, 51 (12), pp 3555–3561

Daskiewicz J-B., et al. Effects of Flavonoids on Cell Proliferation and Caspase Activation in a Human Colonic Cell Line HT29:  An SAR Study. J. Med. Chem., 2005, 48 (8), pp 2790–2804

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

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