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Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Journal of medicinal chemistry - 22 Jul 2021

Nardella F, Halby L, Dobrescu I, Viluma J, Bon C, Claes A, Cadet-Daniel V, Tafit A, Roesch C, Hammam E, Erdmann D, Mairet-Khedim M, Peronet R, Mecheri S, Witkowski B, Scherf A, Arimondo PB,

Link to Pubmed [PMID] – 34185525

Link to DOI – 10.1021/acs.jmedchem.1c00821

J Med Chem 2021 Jul; 64(14): 10403-10417

Epigenetic post-translational modifications are essential for human malaria parasite survival and progression through its life cycle. Here, we present new functionalized suberoylanilide hydroxamic acid (SAHA) derivatives that chemically combine the pan-histone deacetylase inhibitor SAHA with the DNA methyltransferase inhibitor procainamide. A three- or four-step chemical synthesis was designed starting from cheap raw materials. Compared to the single drugs, the combined molecules showed a superior activity in Plasmodium and a potent inhibition against human HDAC6, exerting no cytotoxicity in human cell lines. These new compounds are fully active in multidrug-resistant Plasmodium falciparum Cambodian isolates. They target transmission of the parasite by inducing irreversible morphological changes in gametocytes and inhibiting exflagellation. The compounds are slow-acting and have an additive antimalarial effect in combination with fast-acting epidrugs and dihydroartemisinin. The lead compound decreases parasitemia in mice in a severe malaria model. Taken together, this novel fused molecule offers an affordable alternative to current failing antimalarial therapy.

https://pubmed.ncbi.nlm.nih.gov/34185525