Synthesis and biological evaluation of non-peptidic cyclophilin ligands

Yong Qian Wu; Sergei Belyakov; Chi Choi; David Limburg; Bert E. Thomas IV; Mark Vaal; Ling Wei; Douglas E. Wilkinson; Agnes Holmes; Mike Fuller; Jocelyn McCormick; Maureen Connolly; Tim Moeller; Joseph Steiner; Gregory S. Hamilton

doi:10.1021/jm020409u

Synthesis and biological evaluation of non-peptidic cyclophilin ligands

Yong Qian Wu, Sergei Belyakov, Chi Choi, David Limburg, Bert E. Thomas IV, Mark Vaal, Ling Wei, Douglas E. Wilkinson, Agnes Holmes, Mike Fuller, Jocelyn McCormick, Maureen Connolly, Tim Moeller, Joseph Steiner, Gregory S. Hamilton

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

24 Scopus citations

Abstract

Peptidylprolyl isomerase cyclophilins play critical roles in a variety of biological processes. Recent findings that cyclophilins are present at high levels in the CNS and that cyclosporin A may possess neuroprotective/neurotrophic effects have prompted us to search for nonimmunosuppressant small molecule cyclophilin ligands. To this end, we report the lead identification through "virtual screening" and the synthesis of our first series of non-peptidic cyclophilin ligands, along with the preliminary biological results.

Original language	English (US)
Pages (from-to)	1112-1115
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	46
Issue number	7
DOIs	https://doi.org/10.1021/jm020409u
State	Published - Mar 27 2003
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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title = "Synthesis and biological evaluation of non-peptidic cyclophilin ligands",

abstract = "Peptidylprolyl isomerase cyclophilins play critical roles in a variety of biological processes. Recent findings that cyclophilins are present at high levels in the CNS and that cyclosporin A may possess neuroprotective/neurotrophic effects have prompted us to search for nonimmunosuppressant small molecule cyclophilin ligands. To this end, we report the lead identification through {"}virtual screening{"} and the synthesis of our first series of non-peptidic cyclophilin ligands, along with the preliminary biological results.",

author = "Wu, {Yong Qian} and Sergei Belyakov and Chi Choi and David Limburg and {Thomas IV}, {Bert E.} and Mark Vaal and Ling Wei and Wilkinson, {Douglas E.} and Agnes Holmes and Mike Fuller and Jocelyn McCormick and Maureen Connolly and Tim Moeller and Joseph Steiner and Hamilton, {Gregory S.}",

year = "2003",

month = mar,

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doi = "10.1021/jm020409u",

language = "English (US)",

volume = "46",

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TY - JOUR

T1 - Synthesis and biological evaluation of non-peptidic cyclophilin ligands

AU - Wu, Yong Qian

AU - Belyakov, Sergei

AU - Choi, Chi

AU - Limburg, David

AU - Thomas IV, Bert E.

AU - Vaal, Mark

AU - Wei, Ling

AU - Wilkinson, Douglas E.

AU - Holmes, Agnes

AU - Fuller, Mike

AU - McCormick, Jocelyn

AU - Connolly, Maureen

AU - Moeller, Tim

AU - Steiner, Joseph

AU - Hamilton, Gregory S.

PY - 2003/3/27

Y1 - 2003/3/27

N2 - Peptidylprolyl isomerase cyclophilins play critical roles in a variety of biological processes. Recent findings that cyclophilins are present at high levels in the CNS and that cyclosporin A may possess neuroprotective/neurotrophic effects have prompted us to search for nonimmunosuppressant small molecule cyclophilin ligands. To this end, we report the lead identification through "virtual screening" and the synthesis of our first series of non-peptidic cyclophilin ligands, along with the preliminary biological results.

AB - Peptidylprolyl isomerase cyclophilins play critical roles in a variety of biological processes. Recent findings that cyclophilins are present at high levels in the CNS and that cyclosporin A may possess neuroprotective/neurotrophic effects have prompted us to search for nonimmunosuppressant small molecule cyclophilin ligands. To this end, we report the lead identification through "virtual screening" and the synthesis of our first series of non-peptidic cyclophilin ligands, along with the preliminary biological results.

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DO - 10.1021/jm020409u

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JO - Journal of medicinal chemistry

JF - Journal of medicinal chemistry

IS - 7

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Synthesis and biological evaluation of non-peptidic cyclophilin ligands

Abstract

ASJC Scopus subject areas

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