Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 7, Pages 3553-3557Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm2012408
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Funding
- National Science Foundation of China [20702031]
- Ministry of Science and Technology of China [2009CB918404]
- E-Institutes of Shanghai Universities (EISU) Chemical Biology Division
- National Comprehensive Technology Platforms for Innovative Drug RD [2009ZX09301-007]
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We report the novel chalcone-benzoxaborole hybrids and their structure-activity relationship against Trypanosoma brucei parasites. The 4-NH2 derivative 29 and 3-OMe derivative 43 were found to have excellent potency. The synergistic 4-NH2-3-OMe compound 49 showed an IC50 of 0.010 mu g/mL and resulted in 100% survival and zero parasitemia in a murine infection model, which represents one of the most potent compounds discovered to date from the benzoxaborole class that inhibit T. brucei growth.
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