N-Glycosyl-thiophene-2-carboxamides: Effects on endothelial cell growth in the presence and absence of bFGF - A significant increase in potency using per-O-acetylated sugar analogues

Sarah L. Rawe; Violeta Zaric; Kathy M. O'Boyle; Paul V. Murphy

doi:10.1016/j.bmcl.2005.11.058

N-Glycosyl-thiophene-2-carboxamides: Effects on endothelial cell growth in the presence and absence of bFGF - A significant increase in potency using per-O-acetylated sugar analogues

Sarah L. Rawe
, Violeta Zaric
, Kathy M. O'Boyle
, Paul V. Murphy

University College Dublin

Research output: Contribution to a Journal (Peer & Non Peer) › Article › peer-review

9 Citations (Scopus)

Abstract

Inhibitors of endothelial cell proliferation are of interest in development of therapies for angiogenesis related disease. N-Glucosyl-thiophene-2- carboxamides have been synthesized and evaluated for their effects on proliferation in bovine aortic endothelial cells. Per-O-acetylated-N-glucosyl- thiophene-2-carboxamides showed improved inhibition of both serum and bFGF stimulated uptake of [³H]thymidine, when compared to non-acetylated analogues.

Original language	English
Pages (from-to)	1316-1319
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	5
DOIs	https://doi.org/10.1016/j.bmcl.2005.11.058
Publication status	Published - 1 Mar 2006
Externally published	Yes

Keywords

Angiogenesis
Endothelial cell proliferation
Glycoconjugates
Glycosyl amides
Thiophene-2-carboxamides
bFGF

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10.1016/j.bmcl.2005.11.058

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title = "N-Glycosyl-thiophene-2-carboxamides: Effects on endothelial cell growth in the presence and absence of bFGF - A significant increase in potency using per-O-acetylated sugar analogues",

abstract = "Inhibitors of endothelial cell proliferation are of interest in development of therapies for angiogenesis related disease. N-Glucosyl-thiophene-2- carboxamides have been synthesized and evaluated for their effects on proliferation in bovine aortic endothelial cells. Per-O-acetylated-N-glucosyl- thiophene-2-carboxamides showed improved inhibition of both serum and bFGF stimulated uptake of [3H]thymidine, when compared to non-acetylated analogues.",

keywords = "Angiogenesis, Endothelial cell proliferation, Glycoconjugates, Glycosyl amides, Thiophene-2-carboxamides, bFGF",

author = "Rawe, \{Sarah L.\} and Violeta Zaric and O'Boyle, \{Kathy M.\} and Murphy, \{Paul V.\}",

year = "2006",

month = mar,

day = "1",

doi = "10.1016/j.bmcl.2005.11.058",

language = "English",

volume = "16",

pages = "1316--1319",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "5",

}

N-Glycosyl-thiophene-2-carboxamides: Effects on endothelial cell growth in the presence and absence of bFGF - A significant increase in potency using per-O-acetylated sugar analogues. / Rawe, Sarah L.; Zaric, Violeta; O'Boyle, Kathy M. et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 5, 01.03.2006, p. 1316-1319.

Research output: Contribution to a Journal (Peer & Non Peer) › Article › peer-review

TY - JOUR

T1 - N-Glycosyl-thiophene-2-carboxamides

T2 - Effects on endothelial cell growth in the presence and absence of bFGF - A significant increase in potency using per-O-acetylated sugar analogues

AU - Rawe, Sarah L.

AU - Zaric, Violeta

AU - O'Boyle, Kathy M.

AU - Murphy, Paul V.

PY - 2006/3/1

Y1 - 2006/3/1

N2 - Inhibitors of endothelial cell proliferation are of interest in development of therapies for angiogenesis related disease. N-Glucosyl-thiophene-2- carboxamides have been synthesized and evaluated for their effects on proliferation in bovine aortic endothelial cells. Per-O-acetylated-N-glucosyl- thiophene-2-carboxamides showed improved inhibition of both serum and bFGF stimulated uptake of [3H]thymidine, when compared to non-acetylated analogues.

AB - Inhibitors of endothelial cell proliferation are of interest in development of therapies for angiogenesis related disease. N-Glucosyl-thiophene-2- carboxamides have been synthesized and evaluated for their effects on proliferation in bovine aortic endothelial cells. Per-O-acetylated-N-glucosyl- thiophene-2-carboxamides showed improved inhibition of both serum and bFGF stimulated uptake of [3H]thymidine, when compared to non-acetylated analogues.

KW - Angiogenesis

KW - Endothelial cell proliferation

KW - Glycoconjugates

KW - Glycosyl amides

KW - Thiophene-2-carboxamides

KW - bFGF

UR - https://www.scopus.com/pages/publications/31344435142

U2 - 10.1016/j.bmcl.2005.11.058

DO - 10.1016/j.bmcl.2005.11.058

M3 - Article

SN - 0960-894X

VL - 16

SP - 1316

EP - 1319

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 5

ER -

N-Glycosyl-thiophene-2-carboxamides: Effects on endothelial cell growth in the presence and absence of bFGF - A significant increase in potency using per-O-acetylated sugar analogues

Abstract

Keywords

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