Several human cyclin-dependent kinase inhibitors, structurally related to roscovitine, as new anti-malarial agents was written by Houze, Sandrine;Hoang, Nha-Thu;Lozach, Olivier;Le Bras, Jacques;Meijer, Laurent;Galons, Herve;Demange, Luc. And the article was included in Molecules in 2014.Synthetic Route of C8H8Cl2N4 This article mentions the following:
In Africa, malaria kills one child each minute. It is also responsible for about one million deaths worldwide each year. Plasmodium falciparum, is the protozoan responsible for the most lethal form of the disease, with resistance developing against the available anti-malarial drugs. Among newly proposed anti-malaria targets, are the P. falciparum cyclin-dependent kinases (PfCDKs). There are involved in different stages of the protozoan growth and development but share high sequence homol. with human cyclin-dependent kinases (CDKs). We previously reported the synthesis of CDKs inhibitors that are structurally-related to (R)-roscovitine, a 2,6,9-trisubstituted purine, and they showed activity against neuronal diseases and cancers. In this report, we describe the synthesis and the characterization of new CDK inhibitors, active in reducing the in vitro growth of P. falciparum (3D7 and 7G8 strains). Six compounds are more potent inhibitors than roscovitine, and three exhibited IC50 values close to 1 μM for both 3D7 and 7G8 strains. Although, such mols. do inhibit P. falciparum growth, they require further studies to improve their selectivity for PfCDKs. In the experiment, the researchers used many compounds, for example, 2,6-Dichloro-9-isopropyl-9H-purine (cas: 203436-45-7Synthetic Route of C8H8Cl2N4).
2,6-Dichloro-9-isopropyl-9H-purine (cas: 203436-45-7) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Synthetic Route of C8H8Cl2N4
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics