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Tetrahydroisoquinoline sulfamates as potent microtubule disruptors: synthesis, anti-proliferative and anti-tubulin activity of dichlorobenzyl-based derivatives and a tubulin co-crystal structure

Abstract:

Tetrahydroisoquinoline (THIQ) 6-O-sulfamate-based anticancer agents, inspired by the endogenous steroid 2-methoxyestradiol and its sulfamate derivatives, are further explored for antiproliferative and microtubule disruptor activity. Based on recently designed C3-methyl C7-methoxy-substituted THIQ derivatives, compounds with mono- and dichloro-substitutions on the pendant N-benzyl ring were synthesized and evaluated. Although improved antiproliferative activity was observed, for example, 4a ve...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1021/acsomega.8b02879

Authors


More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
Pharmacology
Role:
Author
Publisher:
American Chemical Society
Journal:
ACS Omega More from this journal
Volume:
4
Issue:
1
Pages:
755–764
Publication date:
2019-01-09
Acceptance date:
2018-12-24
DOI:
ISSN:
2470-1343
Keywords:
Pubs id:
pubs:956237
UUID:
uuid:d5074d21-284f-4c42-9b34-296c85f348cd
Local pid:
pubs:956237
Source identifiers:
956237
Deposit date:
2019-01-04

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