Journal article
Tetrahydroisoquinoline sulfamates as potent microtubule disruptors: synthesis, anti-proliferative and anti-tubulin activity of dichlorobenzyl-based derivatives and a tubulin co-crystal structure
- Abstract:
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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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(Preview, Version of record, pdf, 3.9MB, Terms of use)
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- Publisher copy:
- 10.1021/acsomega.8b02879
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Bibliographic Details
- 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:
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2470-1343
Item Description
- Keywords:
- Pubs id:
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pubs:956237
- UUID:
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uuid:d5074d21-284f-4c42-9b34-296c85f348cd
- Local pid:
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pubs:956237
- Source identifiers:
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956237
- Deposit date:
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2019-01-04
Terms of use
- Copyright holder:
- American Chemical Society
- Copyright date:
- 2019
- Notes:
- © 2019 American Chemical Society. ACS AuthorChoice - This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
- Licence:
- CC Attribution (CC BY)
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