2. Academic Validation
  3. Synthesis of a highly active new anti-HIV agent 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine

Synthesis of a highly active new anti-HIV agent 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine

  • Bioorg Med Chem Lett. 2003 Nov 3;13(21):3775-7. doi: 10.1016/j.bmcl.2003.07.009.
Kazuhiro Haraguchi 1,  Shingo Takeda,  Hiromichi Tanaka,  Takao Nitanda,  Masanori Baba,  G E Dutschman,  Yung-Chi Cheng
Affiliations

Affiliation

  • 1 School of Pharmaceutical Sciences, Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, Japan.
PMID: 14552777 DOI: 10.1016/j.bmcl.2003.07.009
Abstract

Compounds having methyl, vinyl, and ethynyl groups at the 4'-position of stavudine (d4T: 2',3'-didehydro-3'-deoxythymidine) were synthesized. The compounds were assayed for their ability to inhibit the replication of HIV in Cell Culture. The 4'-ethynyl analogue (15) was found to be more potent and less toxic than the parent compound stavudine.

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