2022
DOI: 10.3390/molecules27123819
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Cell Fate following Irradiation of MDA-MB-231 and MCF-7 Breast Cancer Cells Pre-Exposed to the Tetrahydroisoquinoline Sulfamate Microtubule Disruptor STX3451

Abstract: A tetrahydroisoquinoline (THIQ) core is able to mimic the A and B rings of 2-methoxyestradiol (2ME2), an endogenous estrogen metabolite that demonstrates promising anticancer properties primarily by disrupting microtubule dynamic instability parameters, but has very poor pharmaceutical properties that can be improved by sulfamoylation. The non-steroidal THIQ-based microtubule disruptor 2-(3-bromo-4,5-dimethoxybenzyl)-7-methoxy-6-sulfamoyloxy-1,2,3,4-tetrahydroisoquinoline (STX3451), with enhanced pharmacokinet… Show more

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Cited by 3 publications
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“…These data suggested that the activation of the repair mechanism may be slightly delayed or that the response may be abrogated. A similar delay in the DNA damage response was reported with an STX3541 (non-steroidal 2-ME analogue) and radiation combination treatment in breast cancer cells, in which the ATM response was depressed in response to increased micronuclei formation [ 53 ]. Further investigations are needed to link these findings with the decreased cellular survival quantified in the clonogenic studies.…”
Section: Discussionsupporting
confidence: 52%
“…These data suggested that the activation of the repair mechanism may be slightly delayed or that the response may be abrogated. A similar delay in the DNA damage response was reported with an STX3541 (non-steroidal 2-ME analogue) and radiation combination treatment in breast cancer cells, in which the ATM response was depressed in response to increased micronuclei formation [ 53 ]. Further investigations are needed to link these findings with the decreased cellular survival quantified in the clonogenic studies.…”
Section: Discussionsupporting
confidence: 52%