High-Throughput Screening of the ReFRAME Library Identifies Potential Drug Repurposing Candidates for Trypanosoma cruzi
Abstract
:1. Introduction
2. Materials and Methods
2.1. Cells
2.2. Phenotypic Imaging Assay
2.3. Software
3. Results
3.1. Primary Screening of the ReFRAME Library against T. cruzi Using a High-Content Imaging Assay
3.2. Counter-Screen of 238 Hits in Dose Response
4. Discussion
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
References
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Compound Name | EC50 CA-I/72 T. cruzi (nM) | CC50 C2C12 (nM) | Selectivity Index (SI) |
---|---|---|---|
NSC-706744 | 0.44 +/− 0.08 | 94 +/− 56 | 214 |
348U87 | 0.63 +/− 0.45 | 815 +/− 215 | 1294 |
ASP-8273 | 2.7 +/− 1.9 | 515 +/− 280 | 191 |
XR 5944 | 3.5 +/− 6.8 | 46 +/− 21 | 13 |
Prenyl-IN-1 | 18 +/− 12 | 182 +/− 90 | 10 |
3-[4-[4-(2-Methoxyphenyl)piperazine-1-yl]butyl]-6-[2-[4-(4-fluorobenzoyl)piperidine-1-yl]ethyl]benzothiazole-2(3H)-one | 22 +/− 23 | 3190 +/− 1202 | 145 |
Incadronate Disodium | 480 +/− 385 | >10,000 | >20 |
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Bernatchez, J.A.; Chen, E.; Hull, M.V.; McNamara, C.W.; McKerrow, J.H.; Siqueira-Neto, J.L. High-Throughput Screening of the ReFRAME Library Identifies Potential Drug Repurposing Candidates for Trypanosoma cruzi. Microorganisms 2020, 8, 472. https://doi.org/10.3390/microorganisms8040472
Bernatchez JA, Chen E, Hull MV, McNamara CW, McKerrow JH, Siqueira-Neto JL. High-Throughput Screening of the ReFRAME Library Identifies Potential Drug Repurposing Candidates for Trypanosoma cruzi. Microorganisms. 2020; 8(4):472. https://doi.org/10.3390/microorganisms8040472
Chicago/Turabian StyleBernatchez, Jean A., Emily Chen, Mitchell V. Hull, Case W. McNamara, James H. McKerrow, and Jair L. Siqueira-Neto. 2020. "High-Throughput Screening of the ReFRAME Library Identifies Potential Drug Repurposing Candidates for Trypanosoma cruzi" Microorganisms 8, no. 4: 472. https://doi.org/10.3390/microorganisms8040472