Spiroindolone

The spiroindolones are a class of compounds in which an indolone ring is substituted with another ring in a spiro arrangement.

Chemical structure of cipargamin, a spiroindolone being studied as an antimalarial agent

Alkaloids in this class include horsfiline, rhynchophylline, gelsemine, carapanaubine, and maremycin E.

Spiroindolones are also an emerging class of antimalarial drugs[1] whose mode of action is to inhibit protein synthesis in the target parasite. The most advanced compound in this class in terms of drug development is cipargamin (NITD609).[2]

References

  1. Yeung, Bryan K. S.; Zou, Bin; Rottmann, Matthias; Lakshminarayana, Suresh B.; Ang, Shi Hua; Leong, Seh Yong; et al. (2010). "Spirotetrahydro β-Carbolines (Spiroindolones): A New Class of Potent and Orally Efficacious Compounds for the Treatment of Malaria". Journal of Medicinal Chemistry. 53 (14): 5155–5164. doi:10.1021/jm100410f. ISSN 0022-2623. PMID 20568778.
  2. Rottmann M, McNamara C, Yeung BK, Lee MC, Zou B, Russell B, et al. (2010). "Spiroindolones, a potent compound class for the treatment of malaria". Science. 329 (5996): 1175–80. doi:10.1126/science.1193225. PMC 3050001. PMID 20813948.


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