Explore Our Hetaryl-tethered Natural Derivatives of Chromone and Coumarin

Although combinatorial chemistry continues to play an increasing role in the drug development process, natural products and their derivatives have remained a major source for drug discovery on account of their rich structural diversity, cell permeability, and target specificity [1]. In connection with this, natural products bearing chromone 1 [2] and coumarin 2 [2] substructures possess a broad spectrum of biological activities by altering the catalytic function of numerous enzymatic reactions. The applications of chromone and coumarin scaffolds in medicine are demonstrated in many commercialized drugs. Examples of chromone-based medications are vitamin supplementation Rutin 3 and Nedocromil 4 that is used for the treatment of asthma. Acenocoumarol 5 applied for the treatment and prevention of thromboembolic diseases and anti-vitiligo drug Trioxalene 6 involve coumarin scaffold.

Figure 1. Examples of drugs bearing chromone- and coumarin-based structures

The natural chromones and Coumarins usually contain one or two points of modification, allowing their coupling with other biologically relevant fragments to give libraries of drug- and lead-like compounds for biological screening.

Such a library containing over 1000 chromone- and coumarin-based compounds is offered by Life Chemicals, with several representatives shown below. The full list of the related structures can be obtained upon request by emailing marketing@lifechemicals.com.

References

1. (a) Newman, D. J.; Cragg, G. M. J. Nat. Prod. 2020, 83, 770–803. (b) Nat. Rev. Drug Discov. 2021, 20, 200–216.
2. (a) Gaspar, A.; Matos, M. J.; Garrido, J.; Uriarte, E.; Borges, F. Chem. Rev. 2014, 114, 4960–4992. (b) Reis, J.; Gaspar, A.; Milhazes, N.; Borges, F. J. Med. Chem. 2017, 60, 7941–7957. (c) Bondarenko, S.P., Makarenko, O.G., Vinogradova, V.I. et al. Chem Nat Compd. 2020, 56, 1040–1043.
3. (a) Bourgaud, F.; Hehn, A.; Larbat, R.; Doerper, S.; Gontier, E.; Kellner, S.; Matern, U. Phytochem. Rev. 2006, 5, 293−308. (b) Venugopala, K. N.; Rashmi, V.; Odhav, B. Biomed Res Int. 2013, 963248. (с) Pinto, D. C. G. A.; Silva, A. M. S. Curr. Top. Med. Chem. 2017, 17, 3190–3198.