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Literature DB >> 11597420

Design and synthesis of Pfmrk inhibitors as potential antimalarial agents.

Z Xiao¹, N C Waters, C L Woodard, Z Li, P K Li.

Abstract

The synthesis and inhibitory activities of 10 potential inhibitors of Pfmrk, a Plasmodium falciparum cyclin-dependent protein kinase, are described. The most potent inhibitor is a 3-phenyl-quinolinone compound with an IC(50) value of 18 microM. It is the first compound reported to inhibit Pfmrk at the micro molar range.

Entities: Chemical Species

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Year: 2001 PMID： 11597420 DOI： 10.1016/s0960-894x(01)00578-9

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

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Cited

14 in total

1. Synthesis and pharmacological evaluation of some new pyrimidine derivatives containing 1,2,4-triazole.

Authors: Shantaram Gajanan Khanage; S Appala Raju; Popat Baban Mohite; Ramdas Bhanudas Pandhare
Journal: Adv Pharm Bull Date: 2012-08-15

2. Analgesic activity of some 1,2,4-triazole heterocycles clubbed with pyrazole, tetrazole, isoxazole and pyrimidine.

Authors: Shantaram Gajanan Khanage; Appala Raju; Popat Baban Mohite; Ramdas Bhanudas Pandhare
Journal: Adv Pharm Bull Date: 2013-02-07

3. A Plasmodium falciparum transcriptional cyclin-dependent kinase-related kinase with a crucial role in parasite proliferation associates with histone deacetylase activity.

Authors: Jean Halbert; Lawrence Ayong; Leila Equinet; Karine Le Roch; Mary Hardy; Dean Goldring; Luc Reininger; Norman Waters; Debopam Chakrabarti; Christian Doerig
Journal: Eukaryot Cell Date: 2010-03-19

Review 4. 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

5. Characterization of a UBC13 kinase in Plasmodium falciparum.

Authors: Nisha Philip; Timothy A Haystead
Journal: Proc Natl Acad Sci U S A Date: 2007-04-23 Impact factor: 11.205

6. Microwave Assisted Synthesis of 1-[5-(Substituted Aryl)-1H-Pyrazol-3-yl]-3,5-Diphenyl-1H-1,2,4-Triazole as Antinociceptive and Antimicrobial Agents.

Authors: Shantaram Gajanan Khanage; Popat Baban Mohite; Ramdas Bhanudas Pandhare; S Appala Raju
Journal: Adv Pharm Bull Date: 2013-12-24

Design and synthesis of Pfmrk inhibitors as potential antimalarial agents.

1. Synthesis and pharmacological evaluation of some new pyrimidine derivatives containing 1,2,4-triazole.

2. Analgesic activity of some 1,2,4-triazole heterocycles clubbed with pyrazole, tetrazole, isoxazole and pyrimidine.

3. A Plasmodium falciparum transcriptional cyclin-dependent kinase-related kinase with a crucial role in parasite proliferation associates with histone deacetylase activity.

Review 4. Malaria biology and disease pathogenesis: insights for new treatments.

5. Characterization of a UBC13 kinase in Plasmodium falciparum.

6. Microwave Assisted Synthesis of 1-[5-(Substituted Aryl)-1H-Pyrazol-3-yl]-3,5-Diphenyl-1H-1,2,4-Triazole as Antinociceptive and Antimicrobial Agents.

7. Antimalarial activity of kinase inhibitor, nilotinib, in vitro and in vivo.

8. 1-{6-Chloro-2-[(2-chloro-6-methyl-quinolin-3-yl)meth-oxy]-4-phenyl-quinolin-3-yl}ethanone.

9. 1-{6-Chloro-2-[(2-chloro-8-methyl-3-quinol-yl)meth-oxy]-4-phenyl-quinolin-3-yl}ethanone.

10. 1-{6-Chloro-2-[(2-chloro-3-quinol-yl)meth-oxy]-4-phenyl-3-quinol-yl}ethan-1-one.