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Quinazolinone-based anticancer agents: synthesis, anti-proliferative SAR, anti-tubulin activity and tubulin co-crystal structure

Abstract:

Quinazolinone-based anti-cancer agents were designed, decorated with functional groups from a 2-methoxyestradiol-based microtubule disruptor series, incorporating the aryl sulfamate motif of steroid sulfatase (STS) inhibitors. The steroidal AB-ring system was mimicked, favoring conformations with an N-2 substituent occupying D-ring space. Evaluation against breast and prostate tumor cell lines identified 7b with DU-145 anti-proliferative activity (GI50 300 nM). A preliminary structure-activit...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Accepted Manuscript

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Publisher copy:
10.1021/acs.jmedchem.7b01474

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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
Pharmacology
Role:
Author
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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
61
Issue:
3
Pages:
1031–1044
Publication date:
2017-12-11
Acceptance date:
2017-12-11
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Pubs id:
pubs:810425
URN:
uri:155aa7cf-de4c-4218-89b7-d8d0a596c10a
UUID:
uuid:155aa7cf-de4c-4218-89b7-d8d0a596c10a
Local pid:
pubs:810425
Paper number:
3

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