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

Eric D. Jones; 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

doi:10.1016/j.bmcl.2010.07.079

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

Eric D. Jones, 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

Research output: Contribution to journal › Article › Research › peer-review

37 Citations (Scopus)

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 EC₅₀ of 3 nM against wild type HIV infected T-cells.

Original language	English
Pages (from-to)	5913-5917
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2010.07.079
Publication status	Published - 1 Oct 2010
Externally published	Yes

Keywords

3-Hydroxy-pyrido[12-a]pyrimidin-4-one
Inhibitor
Integrase
Synthesis

Access to Document

10.1016/j.bmcl.2010.07.079

Link to publication in Scopus

Cite this

Jones, E. D., Vandegraaff, N., Le, G., Choi, N., Issa, W., MacFarlane, K., Thienthong, N., Winfield, L. J., Coates, J. A. V., Lu, L., Li, X., Feng, X., Yu, C., Rhodes, D. I., & Deadman, J. J. (2010). Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold. Bioorganic and Medicinal Chemistry Letters, 20(19), 5913-5917. https://doi.org/10.1016/j.bmcl.2010.07.079

Jones, Eric D. ; Vandegraaff, Nick ; Le, Giang ; Choi, Neil ; Issa, William ; MacFarlane, Katherine ; Thienthong, Neeranat ; Winfield, Lisa J. ; Coates, Jonathan A.V. ; Lu, Long ; Li, Xinming ; Feng, Xiao ; Yu, Changjiang ; Rhodes, David I. ; Deadman, John J. / Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1 : Selection of the scaffold. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 19. pp. 5913-5917.

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title = "Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold",

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 EC50 of 3 nM against wild type HIV infected T-cells.",

keywords = "3-Hydroxy-pyrido[12-a]pyrimidin-4-one, Inhibitor, Integrase, Synthesis",

author = "Jones, {Eric D.} and Nick Vandegraaff and Giang Le and Neil Choi and William Issa and Katherine MacFarlane and Neeranat Thienthong and Winfield, {Lisa J.} and Coates, {Jonathan A.V.} and Long Lu and Xinming Li and Xiao Feng and Changjiang Yu and Rhodes, {David I.} and Deadman, {John J.}",

year = "2010",

month = oct,

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doi = "10.1016/j.bmcl.2010.07.079",

language = "English",

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Jones, ED, Vandegraaff, N, Le, G, Choi, N, Issa, W, MacFarlane, K, Thienthong, N, Winfield, LJ, Coates, JAV, Lu, L, Li, X, Feng, X, Yu, C, Rhodes, DI & Deadman, JJ 2010, 'Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold', Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 19, pp. 5913-5917. https://doi.org/10.1016/j.bmcl.2010.07.079

Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1 : Selection of the scaffold. / Jones, Eric D.; Vandegraaff, Nick; Le, Giang; Choi, Neil; Issa, William; MacFarlane, Katherine; Thienthong, Neeranat; Winfield, Lisa J.; Coates, Jonathan A.V.; Lu, Long; Li, Xinming; Feng, Xiao; Yu, Changjiang; Rhodes, David I.; Deadman, John J.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 19, 01.10.2010, p. 5913-5917.

Research output: Contribution to journal › Article › Research › peer-review

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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.

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KW - 3-Hydroxy-pyrido[12-a]pyrimidin-4-one

KW - Inhibitor

KW - Integrase

KW - Synthesis

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