Title : Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.

Pub. Date : 2021 Dec 15

PMID : 34610548






3 Functional Relationships(s)
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1 Herein, a series of tetrahydroisoquinoline (THIQ)-hydroxamate conjugates were rationally designed and synthesized as dual SERDs/HDAC inhibitors by incorporating the hydroxamate, a known HDAC pharmacophore, into a privileged THIQ scaffold of selective ERalpha degraders (SERDs). 1,2,3,4-tetrahydroisoquinoline estrogen receptor 1 Homo sapiens
2 Herein, a series of tetrahydroisoquinoline (THIQ)-hydroxamate conjugates were rationally designed and synthesized as dual SERDs/HDAC inhibitors by incorporating the hydroxamate, a known HDAC pharmacophore, into a privileged THIQ scaffold of selective ERalpha degraders (SERDs). 1,2,3,4-tetrahydroisoquinoline estrogen receptor 1 Homo sapiens
3 Herein, a series of tetrahydroisoquinoline (THIQ)-hydroxamate conjugates were rationally designed and synthesized as dual SERDs/HDAC inhibitors by incorporating the hydroxamate, a known HDAC pharmacophore, into a privileged THIQ scaffold of selective ERalpha degraders (SERDs). 1,2,3,4-tetrahydroisoquinoline estrogen receptor 1 Homo sapiens