2. Academic Validation
  3. Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: selection of the scaffold

Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: selection of the scaffold

  • Bioorg Med Chem Lett. 2010 Oct 1;20(19):5913-7. doi: 10.1016/j.bmcl.2010.07.079.
Eric D Jones 1,  Nick Vandegraaff,  Giang Le,  Neil Choi,  William Issa,  Katherine Macfarlane,  Neeranat Thienthong,  Lisa J Winfield,  Jonathan A V Coates,  Long Lu,  Xinming Li,  Xiao Feng,  Changjiang Yu,  David I Rhodes,  John J Deadman
Affiliations

Affiliation

  • 1 Avexa Ltd, 576 Swan Street, Richmond, Victoria 3121, Australia.
PMID: 20727748 DOI: 10.1016/j.bmcl.2010.07.079
Abstract

HIV Integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization of the 6:6 core giving compound 48 with an EC(50) of 3 nM against wild type HIV infected T-cells.

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