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Issue 7, 2014
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Tetracycline analogues with a selective inhibitory effect on HIF-1α

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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.

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

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Article information


Submitted
10 Mar 2014
Accepted
07 May 2014
First published
30 May 2014

Med. Chem. Commun., 2014,5, 923-926
Article type
Concise Article

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

Y. Bendiabdellah, K. M. Rahman, B. Uranchimeg, K. S. Nahar, D. Antonow, R. H. Shoemaker, G. Melillo, G. Zinzalla and D. E. Thurston, Med. Chem. Commun., 2014, 5, 923
DOI: 10.1039/C4MD00111G

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