Literature DB >> 18774709

Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7.

Nathalie Bouloc1, Jonathan M Large, Ela Smiljanic, David Whalley, Keith H Ansell, Christopher D Edlin, Justin S Bryans.   

Abstract

A high-throughput screening campaign identified a number of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. Further synthetic chemistry efforts enabled the preparation of a number of analogues with promising in vitro potencies. Although these compounds show likely broad spectrum inhibitory activity, they represent a useful starting point for further chemical optimisation.

Entities:  

Mesh:

Substances:

Year:  2008        PMID: 18774709     DOI: 10.1016/j.bmcl.2008.08.043

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

Review 1.  Malaria biology and disease pathogenesis: insights for new treatments.

Authors:  Louis H Miller; Hans C Ackerman; Xin-zhuan Su; Thomas E Wellems
Journal:  Nat Med       Date:  2013-02-06       Impact factor: 53.440

2.  Expanding the Antimalarial Drug Arsenal-Now, But How?

Authors:  Brian T Grimberg; Rajeev K Mehlotra
Journal:  Pharmaceuticals (Basel)       Date:  2011-05-01

3.  Potent inhibitors of malarial P. Falciparum protein kinase G: Improving the cell activity of a series of imidazopyridines.

Authors:  Jonathan M Large; Kristian Birchall; Nathalie S Bouloc; Andy T Merritt; Ela Smiljanic-Hurley; Denise J Tsagris; Mary C Wheldon; Keith H Ansell; Peter J Coombs; Catherine A Kettleborough; David Whalley; Lindsay B Stewart; Paul W Bowyer; David A Baker; Simon A Osborne
Journal:  Bioorg Med Chem Lett       Date:  2018-11-20       Impact factor: 2.823

4.  Potent bicyclic inhibitors of malarial cGMP-dependent protein kinase: approaches to combining improvements in cell potency, selectivity and structural novelty.

Authors:  Jonathan M Large; Kristian Birchall; Nathalie S Bouloc; Andy T Merritt; Ela Smiljanic-Hurley; Denise J Tsagris; Mary C Wheldon; Keith H Ansell; Peter J Coombs; Catherine A Kettleborough; David Whalley; Lindsay B Stewart; Paul W Bowyer; David A Baker; Simon A Osborne
Journal:  Bioorg Med Chem Lett       Date:  2019-08-09       Impact factor: 2.823

5.  Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1).

Authors:  Timothy M Chapman; Simon A Osborne; Nathalie Bouloc; Jonathan M Large; Claire Wallace; Kristian Birchall; Keith H Ansell; Hayley M Jones; Debra Taylor; Barbara Clough; Judith L Green; Anthony A Holder
Journal:  Bioorg Med Chem Lett       Date:  2013-03-21       Impact factor: 2.823

6.  Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.

Authors:  Gregory J Crowther; Heidi K Hillesland; Katelyn R Keyloun; Molly C Reid; Maria Jose Lafuente-Monasterio; Sonja Ghidelli-Disse; Stephen E Leonard; Panqing He; Jackson C Jones; Mallory M Krahn; Jack S Mo; Kartheek S Dasari; Anna M W Fox; Markus Boesche; Majida El Bakkouri; Kasey L Rivas; Didier Leroy; Raymond Hui; Gerard Drewes; Dustin J Maly; Wesley C Van Voorhis; Kayode K Ojo
Journal:  PLoS One       Date:  2016-03-02       Impact factor: 3.240

Review 7.  An Update on Development of Small-Molecule Plasmodial Kinase Inhibitors.

Authors:  Chantalle Moolman; Rencia van der Sluis; Richard M Beteck; Lesetja J Legoabe
Journal:  Molecules       Date:  2020-11-07       Impact factor: 4.411

  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.