Journal
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
Volume 108, Issue 17, Pages 6775-6780Publisher
NATL ACAD SCIENCES
DOI: 10.1073/pnas.1017666108
Keywords
chemical biology; organocatalytic; polycyclic ketal
Categories
Funding
- NIGMS CMLD Initiative [P50 GM067041]
- Divisions of Intramural Research at the National Institute of Allergy and Infectious Diseases
- National Human Genome Research Institute
- NIH Roadmap for Medical Research
- National Institutes of Health
Ask authors/readers for more resources
In an effort to expand the stereochemical and structural complexity of chemical libraries used in drug discovery, the Center for Chemical Methodology and Library Development at Boston University has established an infrastructure to translate methodologies accessing diverse chemotypes into arrayed libraries for biological evaluation. In a collaborative effort, the NIH Chemical Genomics Center determined IC(50)'s for Plasmodium falciparum viability for each of 2,070 members of the CMLD-BU compound collection using quantitative high-throughput screening across five parasite lines of distinct geographic origin. Three compound classes displaying either differential or comprehensive antimalarial activity across the lines were identified, and the nascent structure activity relationships (SAR) from this experiment used to initiate optimization of these chemotypes for further development.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available