Synthesis and biological evaluation of deoxy-hematoxylin derivatives as a novel class of anti-HIV-1 agents.

@article{Ishii2012SynthesisAB,
  title={Synthesis and biological evaluation of deoxy-hematoxylin derivatives as a novel class of anti-HIV-1 agents.},
  author={Hideki Ishii and Hiroko Koyama and Kyoji Hagiwara and Tomoyuki Miura and Guangai Xue and Yoshie Hashimoto and Genta Kitahara and Yoko Aida and Masaaki Suzuki},
  journal={Bioorganic & medicinal chemistry letters},
  year={2012},
  volume={22 3},
  pages={
          1469-74
        }
}
SAR studies for the exploration a novel class of anti-human immunodeficiency virus type 1 (HIV-1) agents based on the hematoxylin structure (1) are described. The systematic deoxygenations of 1 including asymmetric synthesis were conducted to obtain a compound showing high potencies for inhibiting the nuclear import and viral replication as anti-HIV-1 agent. Among all, C-3-deoxygenated analog 16 exhibited most promising biological activities as anti-HIV-1 agent such as lower cytotoxicity (16:1… CONTINUE READING