1404508-27-5
Chemical Structure
OBHSA
- CAS No.: 1404508-27-5
- Formula:C27H24F3NO6S
- Molecular Weight:547.54
SMILES: FC(F)(F)CN(C1=CC=C(C=C1)OC)S(=O)([C@@H]2[C@@]3([H])C(C4=CC=C(C=C4)O)=C(C5=CC=C(C=C5)O)[C@](C2)([H])O3)=O
Biological Activity: OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders[1][2].
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OBHSA | OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders. | |||||||||||||||||||||
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- [1]. OBHSA, a novel selective estrogen receptor degrader, overcomes tamoxifen resistance through cell cycle arrest and unfolded protein response-mediated apoptosis in breast cancer [Content Brief]
- [2]. Zhou J, et al. A novel selective estrogen receptor degrader induces cell cycle arrest in breast cancer via ERα degradation and the autophagy-lysosome pathway[J]. Bioorganic & Medicinal Chemistry, 2023, 82: 117235. [Content Brief]
Keywords
