{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,23]],"date-time":"2026-09-23T11:16:09Z","timestamp":1790162169838,"version":"4.1.0"},"reference-count":76,"publisher":"MDPI AG","issue":"9","license":[{"start":{"date-parts":[[2014,9,23]],"date-time":"2014-09-23T00:00:00Z","timestamp":1411430400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/3.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>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 homology 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 \u00b5M for both 3D7 and 7G8 strains. Although, such molecules do inhibit P. falciparum growth, they require further studies to improve their selectivity for PfCDKs.<\/jats:p>","DOI":"10.3390\/molecules190915237","type":"journal-article","created":{"date-parts":[[2014,9,23]],"date-time":"2014-09-23T10:20:41Z","timestamp":1411467641000},"page":"15237-15257","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":15,"title":["Several Human Cyclin-Dependent Kinase Inhibitors, Structurally Related to Roscovitine, As New Anti-Malarial Agents"],"prefix":"10.3390","volume":"19","author":[{"given":"Sandrine","family":"Houz\u00e9","sequence":"first","affiliation":[{"name":"Laboratoire de Parasitologie, CNR du Paludisme, AP-HP, H\u00f4pital Bichat & UMR 216 IRD, Universit\u00e9 Paris Descartes, Sorbonne Paris Cit\u00e9, UFR des Sciences Pharmaceutiques,  4 avenue de l'Observatoire, Paris 75006, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Nha-Thu","family":"Hoang","sequence":"additional","affiliation":[{"name":"Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques (LCBPT),  UMR 8601 CNRS, Universit\u00e9 Paris Descartes, Sorbonne Paris Cit\u00e9, UFR Biom\u00e9dicale des Saints P\u00e8res, 45 rue des Saints-P\u00e8res, Paris 75270, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Olivier","family":"Lozach","sequence":"additional","affiliation":[{"name":"Protein Phosphorylation and Human Diseases Group, CNRS, USR 3151, Station biologique, Roscoff 29680, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jacques","family":"Le Bras","sequence":"additional","affiliation":[{"name":"Laboratoire de Parasitologie, CNR du Paludisme, AP-HP, H\u00f4pital Bichat & UMR 216 IRD, Universit\u00e9 Paris Descartes, Sorbonne Paris Cit\u00e9, UFR des Sciences Pharmaceutiques,  4 avenue de l'Observatoire, Paris 75006, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Laurent","family":"Meijer","sequence":"additional","affiliation":[{"name":"Protein Phosphorylation and Human Diseases Group, CNRS, USR 3151, Station biologique, Roscoff 29680, France"},{"name":"ManRos Therapeutics, H\u00f4tel de Recherche, Centre de Perharidy, Roscoff 29680, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Herv\u00e9","family":"Galons","sequence":"additional","affiliation":[{"name":"ManRos Therapeutics, H\u00f4tel de Recherche, Centre de Perharidy, Roscoff 29680, France"},{"name":"Laboratoire de Pharmacochimie, INSERM U 1022, Universit\u00e9 Paris Descartes, Sorbonne Paris Cit\u00e9, UFR des Sciences Pharmaceutiques, 4 avenue de l'Observatoire, Paris 75006, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Luc","family":"Demange","sequence":"additional","affiliation":[{"name":"Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques (LCBPT),  UMR 8601 CNRS, Universit\u00e9 Paris Descartes, Sorbonne Paris Cit\u00e9, UFR Biom\u00e9dicale des Saints P\u00e8res, 45 rue des Saints-P\u00e8res, Paris 75270, France"},{"name":"Institut de Chimie de Nice (ICN), UMR 7272 CNRS, Universit\u00e9 de Nice Sophia-Antipolis,  Parc Valrose, Nice 06108, France"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2014,9,23]]},"reference":[{"key":"ref_1","unstructured":"Available online:http:\/\/www.who.int."},{"key":"ref_2","first-page":"6","article-title":"Biologie de la transmission homme-moustique du plasmodium","volume":"96","author":"Robert","year":"2003","journal-title":"Bull. 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