Tetracycline analogues with a selective inhibitory effect on HIF-1α

Yassine Bendiabdellah; Khondaker Rahman; B Uranchimeg; Kazi Nahar; Dyeison Antonow; R.H. Shoemaker; G. Melillo; Giovanna Zinzalla; David E Thurston

doi:10.1039/C4MD00111G

Tetracycline analogues with a selective inhibitory effect on HIF-1α

Yassine Bendiabdellah
, Khondaker Rahman
, B Uranchimeg
, Kazi Nahar
, Dyeison Antonow
, R.H. Shoemaker
, G. Melillo
, Giovanna Zinzalla
, David E Thurston

Institute of Pharmaceutical Science

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

3 Citations (Scopus)

Abstract

As part of a programme to discover novel transcription factor inhibitors, a 40-membered library of tetracycline analogues was screened to identify potential HIF-1 inhibitors. Two novel analogues (5b and 5c) with significant HIF-1 modulation properties were identified. These molecules possess good cellular penetration properties, and provide significant down-regulation of VEGF in U251 cells.

Original language	English
Pages (from-to)	923-926
Number of pages	4
Journal	MedChemComm
Volume	5
Issue number	7
DOIs	https://doi.org/10.1039/C4MD00111G
Publication status	Published - Jul 2014

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title = "Tetracycline analogues with a selective inhibitory effect on HIF-1α",

abstract = "As part of a programme to discover novel transcription factor inhibitors, a 40-membered library of tetracycline analogues was screened to identify potential HIF-1 inhibitors. Two novel analogues (5b and 5c) with significant HIF-1 modulation properties were identified. These molecules possess good cellular penetration properties, and provide significant down-regulation of VEGF in U251 cells.",

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AU - Bendiabdellah, Yassine

AU - Rahman, Khondaker

AU - Uranchimeg , B

AU - Nahar, Kazi

AU - Antonow, Dyeison

AU - Shoemaker, R.H.

AU - Melillo, G.

AU - Zinzalla, Giovanna

AU - Thurston, David E

PY - 2014/7

Y1 - 2014/7

N2 - As part of a programme to discover novel transcription factor inhibitors, a 40-membered library of tetracycline analogues was screened to identify potential HIF-1 inhibitors. Two novel analogues (5b and 5c) with significant HIF-1 modulation properties were identified. These molecules possess good cellular penetration properties, and provide significant down-regulation of VEGF in U251 cells.

AB - As part of a programme to discover novel transcription factor inhibitors, a 40-membered library of tetracycline analogues was screened to identify potential HIF-1 inhibitors. Two novel analogues (5b and 5c) with significant HIF-1 modulation properties were identified. These molecules possess good cellular penetration properties, and provide significant down-regulation of VEGF in U251 cells.

U2 - 10.1039/C4MD00111G

DO - 10.1039/C4MD00111G

M3 - Article

SN - 2040-2503

VL - 5

SP - 923

EP - 926

JO - MedChemComm

JF - MedChemComm

IS - 7

ER -

Tetracycline analogues with a selective inhibitory effect on HIF-1α

Abstract

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