Synthesis and TNF expression inhibitory properties of new thalidomide analogues derived via Heck cross coupling

Scott Stewart; Daniel Spagnolo; Marta Polomska; M. Sin; Mahdad Karimi; Lawrence Abraham

doi:10.1016/j.bmcl.2007.08.042

Synthesis and TNF expression inhibitory properties of new thalidomide analogues derived via Heck cross coupling

Scott Stewart
, Daniel Spagnolo
, Marta Polomska
, M. Sin
, Mahdad Karimi
, Lawrence Abraham

School of Molecular Sciences

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

49 Citations (Scopus)

Abstract

A library of new thalidomide analogues containing an olefin functionality were synthesised using a Heck cross coupling reaction from their aryl halogenated precursor. All analogues were tested for their ability to inhibit the synthesis of the proinflammatory cytokine Tumour Necrosis Factor (TNF). Compounds 22, 29, 33 and 37 were the most effective in this assay inhibiting TNF expression 50%, 69%, 52% and 50%, respectively. Crown copyright (c) 2007 Published by Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	5819-5824
Journal	Bioorganic & medicinal chemistry letters
Volume	17
Issue number	21
DOIs	https://doi.org/10.1016/j.bmcl.2007.08.042
Publication status	Published - 2007

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10.1016/j.bmcl.2007.08.042

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title = "Synthesis and TNF expression inhibitory properties of new thalidomide analogues derived via Heck cross coupling",

abstract = "A library of new thalidomide analogues containing an olefin functionality were synthesised using a Heck cross coupling reaction from their aryl halogenated precursor. All analogues were tested for their ability to inhibit the synthesis of the proinflammatory cytokine Tumour Necrosis Factor (TNF). Compounds 22, 29, 33 and 37 were the most effective in this assay inhibiting TNF expression 50\%, 69\%, 52\% and 50\%, respectively. Crown copyright (c) 2007 Published by Elsevier Ltd. All rights reserved.",

author = "Scott Stewart and Daniel Spagnolo and Marta Polomska and M. Sin and Mahdad Karimi and Lawrence Abraham",

year = "2007",

doi = "10.1016/j.bmcl.2007.08.042",

language = "English",

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journal = "Bioorganic \& medicinal chemistry letters",

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AU - Spagnolo, Daniel

AU - Polomska, Marta

AU - Sin, M.

AU - Karimi, Mahdad

AU - Abraham, Lawrence

PY - 2007

Y1 - 2007

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AB - A library of new thalidomide analogues containing an olefin functionality were synthesised using a Heck cross coupling reaction from their aryl halogenated precursor. All analogues were tested for their ability to inhibit the synthesis of the proinflammatory cytokine Tumour Necrosis Factor (TNF). Compounds 22, 29, 33 and 37 were the most effective in this assay inhibiting TNF expression 50%, 69%, 52% and 50%, respectively. Crown copyright (c) 2007 Published by Elsevier Ltd. All rights reserved.

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DO - 10.1016/j.bmcl.2007.08.042

M3 - Article

SN - 0960-894X

VL - 17

SP - 5819

EP - 5824

JO - Bioorganic & medicinal chemistry letters

JF - Bioorganic & medicinal chemistry letters

IS - 21

ER -

Synthesis and TNF expression inhibitory properties of new thalidomide analogues derived via Heck cross coupling

Abstract

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