2. Academic Validation
  3. Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity

Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity

  • ACS Med Chem Lett. 2020 Sep 9;11(11):2290-2293. doi: 10.1021/acsmedchemlett.0c00414.
Qiang Wang 1 2 3,  Yujiang Li 1,  Liyun Zheng 3,  Xiaowan Huang 3,  Yanli Wang 2,  Chin-Ho Chen 4,  Yung-Yi Cheng 5,  Susan L Morris-Natschke 5,  Kuo-Hsiung Lee 5 6
Affiliations

Affiliations

  • 1 High & New Technology Research Center of Henan Academy of Sciences, Zhengzhou 450002, China.
  • 2 National Health Commission Key Laboratory of Birth Defect Prevention, Zhengzhou 450002, China.
  • 3 Institute of Medical and Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450052, China.
  • 4 Surgical Science, Department of Surgery, Duke University Medical Center, Durham, North Carolina 27710, United States.
  • 5 Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599-7568, United States.
  • 6 Chinese Medicine Research and Development Center, China Medical University and Hospital, Taichung 40402, Taiwan.
PMID: 33214842 DOI: 10.1021/acsmedchemlett.0c00414
Abstract

Novel betulinic/betulonic acid-nucleoside hybrids were synthesized as possible new anti-HIV agents. Among the synthesized hybrids, two compounds were highly effective against HIV. Compared with AZT and DSB, compounds 10a (IC50 = 0.0078 μM, CC50 = 9.6 μM) and 10b (IC50 = 0.020 μM, CC50 = 23.8 μM) showed more potent or equipotent, respectively, anti-HIV activity but displayed lower cytotoxicity.

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