dc.contributor.author |
Field, Jessica J |
|
dc.contributor.author |
Singh, A Jonathan |
|
dc.contributor.author |
Sinha, Saptarshi |
|
dc.contributor.author |
Rowe, Matthew R |
|
dc.contributor.author |
Denny, William A |
|
dc.contributor.author |
Brooke, Darby G |
|
dc.contributor.author |
Miller, John H |
|
dc.coverage.spatial |
Germany |
|
dc.date.accessioned |
2022-03-07T23:27:49Z |
|
dc.date.available |
2022-03-07T23:27:49Z |
|
dc.date.issued |
2019-4 |
|
dc.identifier.issn |
1861-4728 |
|
dc.identifier.uri |
https://hdl.handle.net/2292/58513 |
|
dc.description.abstract |
While clinically useful, microtubule-targeting agents are limited by factors that include their susceptibility to multidrug resistance. A series of aryl sulfonamides, terminally substituted with an amide or carboxylic acid, was synthesized and assayed for biological activity in two human cancer cell lines. The resulting antiproliferative activity data demonstrated that an amide was superior to a carboxylic acid in the para position. The most potent compound (3) had an IC<sub>50</sub> for growth inhibition in the low micromolar range, caused cells to accumulate in G<sub>2</sub> M of the cell cycle, and led to depolymerization of microtubules. It was also not susceptible to the P-glycoprotein drug efflux pump that underpins the resistance of cells to long-term drug treatment schedules. |
|
dc.format.medium |
Print-Electronic |
|
dc.language |
eng |
|
dc.publisher |
Wiley |
|
dc.relation.ispartofseries |
Chemistry, an Asian journal |
|
dc.rights |
Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. |
|
dc.rights.uri |
https://researchspace.auckland.ac.nz/docs/uoa-docs/rights.htm |
|
dc.subject |
antiproliferative activity |
|
dc.subject |
aryl sulfonyl amide |
|
dc.subject |
cancer |
|
dc.subject |
microtubule-destabilizing agents |
|
dc.subject |
microtubules |
|
dc.subject |
Science & Technology |
|
dc.subject |
Physical Sciences |
|
dc.subject |
Chemistry, Multidisciplinary |
|
dc.subject |
Chemistry |
|
dc.subject |
antiproliferative activity |
|
dc.subject |
aryl sulfonyl amide |
|
dc.subject |
cancer |
|
dc.subject |
microtubules |
|
dc.subject |
microtubule-destabilizing agents |
|
dc.subject |
PELORUSIDE-A |
|
dc.subject |
TUBULIN |
|
dc.subject |
CANCER |
|
dc.subject |
DYNAMICS |
|
dc.subject |
AGENTS |
|
dc.subject |
POLYMERIZATION |
|
dc.subject |
INHIBITORS |
|
dc.subject |
GROWTH |
|
dc.subject |
DRUGS |
|
dc.subject |
1115 Pharmacology and Pharmaceutical Sciences |
|
dc.subject |
Cancer |
|
dc.subject |
03 Chemical Sciences |
|
dc.title |
Synthesis and Microtubule-Destabilizing Activity of N-Cyclopropyl-4-((3,4-dihydroquinolin-1(2H)-yl)sulfonyl)benzamide and its Analogs. |
|
dc.type |
Journal Article |
|
dc.identifier.doi |
10.1002/asia.201801313 |
|
pubs.issue |
8 |
|
pubs.begin-page |
1151 |
|
pubs.volume |
14 |
|
dc.date.updated |
2022-02-23T18:12:03Z |
|
dc.rights.holder |
Copyright: The author |
en |
pubs.author-url |
https://www.ncbi.nlm.nih.gov/pubmed/30311418 |
|
pubs.end-page |
1157 |
|
pubs.publication-status |
Published |
|
dc.rights.accessrights |
http://purl.org/eprint/accessRights/RestrictedAccess |
en |
pubs.subtype |
Journal Article |
|
pubs.elements-id |
756823 |
|
dc.identifier.eissn |
1861-471X |
|
pubs.online-publication-date |
2018-11-14 |
|