2. Academic Validation
  3. Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors

Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors

  • Bioorg Med Chem. 2011 Jul 15;19(14):4220-6. doi: 10.1016/j.bmc.2011.05.060.
Shuang-Xi Gu 1,  Xuan Zhang,  Qiu-Qin He,  Liu-Meng Yang,  Xiao-Dong Ma,  Yong-Tang Zheng,  Shi-Qiong Yang,  Fen-Er Chen
Affiliations

Affiliation

  • 1 Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China.
PMID: 21689939 DOI: 10.1016/j.bmc.2011.05.060
Abstract

A novel series of naphthyl phenyl ether analogues (NPEs) have been synthesized and evaluated for their in vitro activities against HIV in C8166 cells. Most of the compounds exhibited moderate to excellent anti-HIV activities. Among them the most active compound 12o showed excellent activities against wild-type HIV-1 with an EC(50) value of 4.60 nM, along with moderate activities against the double mutant strain HIV-1(IIIB) A17 (K103N+Y181C) and HIV-2 strain ROD with an EC(50) value of 0.82 and 4.40 μM, respectively. Preliminary structure-activity relationship (SAR) among the newly synthesized NPEs was also investigated.

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