2. Academic Validation
  3. Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives

Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives

  • Bioorg Med Chem Lett. 2005 Oct 15;15(20):4451-5. doi: 10.1016/j.bmcl.2005.07.046.
Tanushree Ratan Bal 1,  Balasubramani Anand,  Perumal Yogeeswari,  Dharmarajan Sriram
Affiliations

Affiliation

  • 1 Medicinal Chemistry Research Laboratory, Pharmacy group, Birla Institute of Technology and Science, Pilani 333031, India.
PMID: 16115762 DOI: 10.1016/j.bmcl.2005.07.046
Abstract

On the basis of pharmacophoric modelling studies of existing NNRTIs, a series of isatin beta-thiosemicarbazone derivatives was synthesized and evaluated for their anti-HIV activity in HTLV-III(B) strain in the CEM cell line. Three compounds showed significant anti-HIV activity, whereupon compound 6 was found to be the most active compound with an EC(50) value of 2.62 microM and a selectivity index of 17.41, while not being cytotoxic to the cell line at a CC(50) value of 44.90 microM. Other tested compounds exhibited marked activity below their toxicity threshold.

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