Issue 7, 2014
From the journal:

MedChemComm

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

Y. Bendiabdellah,a   K. M. Rahman,b   B. Uranchimeg,‡c   K. S. Nahar,b   D. Antonow,a   R. H. Shoemaker,‡c   G. Melillo,§d   G. Zinzalla*e  and  D. E. Thurston*b  

* Corresponding authors

a School of Pharmacy, University College London, 29-39 Brunswick Square, London, UK

b Institute of Pharmaceutical Science, King's College London, Britannia House, 7 Trinity Street, London, UK
E-mail: david.thurston@kcl.ac.uk
Tel: +44 (0)207 848 7507

c Screening Technologies Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, Maryland, USA

d SAIC-Frederick, Frederick, Maryland, USA

e Centre for Advanced Cancer Therapies, MTC Dept., Karolinska Institutet, Nobelsväg 16, SE-17177 Stockholm, Sweden
E-mail: giovanna.zinzalla@ki.se
Tel: +46 8524 81262

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

DOI
https://doi.org/10.1039/C4MD00111G
Article type
Concise Article
Submitted
10 Mar 2014
Accepted
07 May 2014
First published
30 May 2014

Med. Chem. Commun., 2014,5, 923-926

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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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