Medicinal chemistry progression of antimalarial hits from phenotypic whole cell screening of SoftFocus libraries

被引：4
|
作者：
Cheuka, Peter M. [1 ,2 ]
Mayoka, Godfrey [1 ,3 ]
Okombo, John [4 ]
Chibale, Kelly [1 ,5 ,6 ,7 ]
机构：
[1] Univ Cape Town, Dept Chem, Cape Town, South Africa
[2] Univ Zambia, Dept Chem, Lusaka, Zambia
[3] Jomo Kenyatta Univ Agr & Technol, Sch Pharm, Dept Pharmacol & Pharmacognosy, Nairobi, Kenya
[4] Columbia Univ, Dept Microbiol & Immunol, New York, NY USA
[5] Univ Cape Town, Drug Discovery & Dev Ctr H3D, Cape Town, South Africa
[6] Univ Cape Town, Inst Infect Dis & Mol Med, Cape Town, South Africa
[7] Univ Cape Town, South African Med Res Council, Drug Discovery & Dev Res Unit, Cape Town, South Africa
来源：
MEDICINAL CHEMISTRY APPROACHES TO MALARIA AND OTHER TROPICAL DISEASES | 2019年 / 53卷
关键词：
ANTIPLASMODIAL IMIDAZOPYRIDAZINE HITS; HUMAN MALARIA PARASITE; PLASMODIUM-FALCIPARUM; PROTEIN-KINASE; SUBSTITUTED IMIDAZOPYRIDAZINES; POTENT INHIBITORS; OPTIMIZATION; IDENTIFICATION; DERIVATIVES; SOLUBILITY;
D O I：
10.1016/bs.armc.2019.04.001
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
引用
收藏
页码：25 / 71
页数：47
相关论文
共 50 条
  • [41] A Whole-Cell Phenotypic Screening Platform for Identifying Methylerythritol Phosphate Pathway-Selective Inhibitors as Novel Antibacterial Agents
    Testa, Charles A.
    Johnson, L. Jeffrey
    ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2012, 56 (09) : 4906 - 4913
  • [42] Locating Sweet Spots for Screening Hits and Evaluating Pan-Assay Interference Filters from the Performance Analysis of Two Lead-like Libraries
    Mok, N. Yi
    Maxe, Sara
    Brenk, Ruth
    JOURNAL OF CHEMICAL INFORMATION AND MODELING, 2013, 53 (03) : 534 - 544
  • [43] Identification of antimalarial phytoconstituents from Tinospora sinensis (Lour.) Merr. Stem by in vitro whole cell assay and multiple targets directed in silico screening against Plasmodium falciparum
    Gogoi, Neelutpal
    Gogoi, Bhaskarjyoti
    Kaishap, Partha Pratim
    Chetia, Dipak
    JOURNAL OF ETHNOPHARMACOLOGY, 2025, 338
  • [44] Capillary electrophoresis chips for screening of endotoxin chemotypes from whole-cell lysates
    Kilar, Aniko
    Peterfi, Zoltan
    Csorba, Eszter
    Kilar, Ferenc
    Kocsis, Bela
    JOURNAL OF CHROMATOGRAPHY A, 2008, 1206 (01) : 21 - 25
  • [45] A Rapid Phenotypic Whole-Cell Screening Approach for the Identification of Small-Molecule Inhibitors That Counter β-Lactamase Resistance in Pseudomonas aeruginosa
    Collia, Deanna
    Bannister, Thomas D.
    Tan, Hao
    Jin, Shouguang
    Langaee, Taimour
    Shumate, Justin
    Scampavia, Louis
    Spicer, Timothy P.
    SLAS DISCOVERY, 2018, 23 (01) : 55 - 64
  • [46] Sensitive screening of antifungal compounds from acetone extracts of medicinal plants with a Bio-Cell Tracer
    Iida, Y
    Yonemura, H
    Oh, KB
    Saito, M
    Matsuoka, H
    YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 1999, 119 (12): : 964 - 971
  • [47] Toward performance-diverse small-molecule libraries for cell-based phenotypic screening using multiplexed high-dimensional profiling
    Wawer, Mathias J.
    Li, Kejie
    Gustafsdottir, Sigrun M.
    Ljosa, Vebjorn
    Bodycombe, Nicole E.
    Marton, Melissa A.
    Sokolnicki, Katherine L.
    Bray, Mark-Anthony
    Kemp, Melissa M.
    Winchester, Ellen
    Taylor, Bradley
    Grant, George B.
    Hon, C. Suk-Yee
    Duvall, Jeremy R.
    Wilson, J. Anthony
    Bittker, Joshua A.
    Dancik, Vlado
    Narayan, Rajiv
    Subramanian, Aravind
    Winckler, Wendy
    Golub, Todd R.
    Carpenter, Anne E.
    Shamji, Alykhan F.
    Schreiber, Stuart L.
    Clemons, Paul A.
    PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2014, 111 (30) : 10911 - 10916
  • [48] Multiple-targets Directed Screening of Flavonoid Compounds from Citrus Species to find out Antimalarial Lead with Predicted Mode of Action: An in silico and Whole Cell-based in vitro Approach
    Gogoi, Neelutpal
    Chetia, Dipak
    Gogoi, Bhaskarjyoti
    Das, Aparoop
    CURRENT COMPUTER-AIDED DRUG DESIGN, 2021, 17 (01) : 69 - 82
  • [49] Diverse antimalarials from whole-cell phenotypic screens disrupt malaria parasite ion and volume homeostasis
    Adelaide S. M. Dennis
    James E. O. Rosling
    Adele M. Lehane
    Kiaran Kirk
    Scientific Reports, 8
  • [50] Diverse antimalarials from whole-cell phenotypic screens disrupt malaria parasite ion and volume homeostasis
    Dennis, Adelaide S. M.
    Rosling, James E. O.
    Lehane, Adele M.
    Kirk, Kiaran
    SCIENTIFIC REPORTS, 2018, 8
12345