TY - JOUR
T1 - Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1
T2 - Selection of the scaffold
AU - Jones, Eric D.
AU - Vandegraaff, Nick
AU - Le, Giang
AU - Choi, Neil
AU - Issa, William
AU - MacFarlane, Katherine
AU - Thienthong, Neeranat
AU - Winfield, Lisa J.
AU - Coates, Jonathan A.V.
AU - Lu, Long
AU - Li, Xinming
AU - Feng, Xiao
AU - Yu, Changjiang
AU - Rhodes, David I.
AU - Deadman, John J.
PY - 2010/10/1
Y1 - 2010/10/1
N2 - 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 EC50 of 3 nM against wild type HIV infected T-cells.
AB - 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 EC50 of 3 nM against wild type HIV infected T-cells.
KW - 3-Hydroxy-pyrido[12-a]pyrimidin-4-one
KW - Inhibitor
KW - Integrase
KW - Synthesis
UR - http://www.scopus.com/inward/record.url?scp=77957555860&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2010.07.079
DO - 10.1016/j.bmcl.2010.07.079
M3 - Article
C2 - 20727748
AN - SCOPUS:77957555860
VL - 20
SP - 5913
EP - 5917
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 19
ER -
