A Novel series of G-quadruplex ligands with selectivity for HIF-expressing osteosarcoma and renal cancer cell lines

Caterina M. Lombardo; Sarah J. Welsh; Sandra J. Strauss; Aaron G. Dale; Alan K. Todd; Rupesh Nanjunda; W. David Wilson; Stephen Neidle

doi:10.1016/j.bmcl.2012.07.009

A Novel series of G-quadruplex ligands with selectivity for HIF-expressing osteosarcoma and renal cancer cell lines

Caterina M. Lombardo, Sarah J. Welsh, Sandra J. Strauss, Aaron G. Dale, Alan K. Todd, Rupesh Nanjunda, W. David Wilson, Stephen Neidle

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

29 Citations (Scopus)

Abstract

A series of naphthalene derivatives with disubstituted triazole side-arms have been assembled by click chemistry. Lead compounds show a high level of selectivity for renal, osteo- and Ewing's sarcomas that express the HIF-1∝ transcription factor. They also interact selectively with the quadruplex DNAs located in the promoter of the HIF genes and it is suggested that the mechanism of action involves inhibition of transcription by drug-mediated quadruplex stabilization in these regions.

Original language	English
Pages (from-to)	5984-5988
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	22
Issue number	18
DOIs	https://doi.org/10.1016/j.bmcl.2012.07.009
Publication status	Published - 2012
Externally published	Yes

Keywords

HIF
Quadruplex
Renal cancer
Sarcomas
Small molecule

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10.1016/j.bmcl.2012.07.009

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title = "A Novel series of G-quadruplex ligands with selectivity for HIF-expressing osteosarcoma and renal cancer cell lines",

abstract = "A series of naphthalene derivatives with disubstituted triazole side-arms have been assembled by click chemistry. Lead compounds show a high level of selectivity for renal, osteo- and Ewing's sarcomas that express the HIF-1∝ transcription factor. They also interact selectively with the quadruplex DNAs located in the promoter of the HIF genes and it is suggested that the mechanism of action involves inhibition of transcription by drug-mediated quadruplex stabilization in these regions.",

keywords = "HIF, Quadruplex, Renal cancer, Sarcomas, Small molecule",

author = "Lombardo, {Caterina M.} and Welsh, {Sarah J.} and Strauss, {Sandra J.} and Dale, {Aaron G.} and Todd, {Alan K.} and Rupesh Nanjunda and Wilson, {W. David} and Stephen Neidle",

year = "2012",

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language = "English",

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pages = "5984--5988",

journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - A Novel series of G-quadruplex ligands with selectivity for HIF-expressing osteosarcoma and renal cancer cell lines

AU - Lombardo, Caterina M.

AU - Welsh, Sarah J.

AU - Strauss, Sandra J.

AU - Dale, Aaron G.

AU - Todd, Alan K.

AU - Nanjunda, Rupesh

AU - Wilson, W. David

AU - Neidle, Stephen

PY - 2012

Y1 - 2012

N2 - A series of naphthalene derivatives with disubstituted triazole side-arms have been assembled by click chemistry. Lead compounds show a high level of selectivity for renal, osteo- and Ewing's sarcomas that express the HIF-1∝ transcription factor. They also interact selectively with the quadruplex DNAs located in the promoter of the HIF genes and it is suggested that the mechanism of action involves inhibition of transcription by drug-mediated quadruplex stabilization in these regions.

AB - A series of naphthalene derivatives with disubstituted triazole side-arms have been assembled by click chemistry. Lead compounds show a high level of selectivity for renal, osteo- and Ewing's sarcomas that express the HIF-1∝ transcription factor. They also interact selectively with the quadruplex DNAs located in the promoter of the HIF genes and it is suggested that the mechanism of action involves inhibition of transcription by drug-mediated quadruplex stabilization in these regions.

KW - HIF

KW - Quadruplex

KW - Renal cancer

KW - Sarcomas

KW - Small molecule

U2 - 10.1016/j.bmcl.2012.07.009

DO - 10.1016/j.bmcl.2012.07.009

M3 - Article

C2 - 22889802

VL - 22

SP - 5984

EP - 5988

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 18

ER -

A Novel series of G-quadruplex ligands with selectivity for HIF-expressing osteosarcoma and renal cancer cell lines

Abstract

Keywords

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