16. Conformationally Constrained Tricyclic HIV Integrase Inhibitors

  1. Nouri Neamati
  1. Maria Fardis,
  2. Haolun Jin,
  3. Xiaowu Chen,
  4. Manuel Tsiang,
  5. James Chen,
  6. Choung Kim and
  7. Matthew Wright

Published Online: 28 SEP 2011

DOI: 10.1002/9781118015377.ch16

HIV-1 Integrase: Mechanism and Inhibitor Design

HIV-1 Integrase: Mechanism and Inhibitor Design

How to Cite

Fardis, M., Jin, H., Chen, X., Tsiang, M., Chen, J., Kim, C. and Wright, M. (2011) Conformationally Constrained Tricyclic HIV Integrase Inhibitors, in HIV-1 Integrase: Mechanism and Inhibitor Design (ed N. Neamati), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9781118015377.ch16

Editor Information

  1. Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, School of Pharmacy, Los Angeles, California, USA

Author Information

  1. Gilead Sciences, Inc., Foster City, California, USA

Publication History

  1. Published Online: 28 SEP 2011
  2. Published Print: 9 SEP 2011

Book Series:

  1. Wiley Series in Drug Discovery and Development

Book Series Editors:

  1. Binghe Wang

ISBN Information

Print ISBN: 9780470184745

Online ISBN: 9781118015377

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Keywords:

  • tricyclic HIV integrase inhibitors;
  • IN active site model;
  • SAR of C-5-substituted tricyclic inhibitors

Summary

This chapter contains sections titled:

  • Introduction

  • Development of Integrase Active-Site Model to Aid Inhibitor Design

  • Integrase Structure

  • Developing Active-Site Model

  • The Tetramer Model

  • Molecular Modeling Summary

  • SAR of C-5-Substituted Tricyclic Inhibitors

  • Biological Characterization of GS-9160

  • Conclusion

  • References