Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib, Author is Li, Yangfeng; Zhao, Jiong; Gutgesell, Lauren M.; Shen, Zhengnan; Ratia, Kiira; Dye, Katherine; Dubrovskyi, Oleksii; Zhao, Huiping; Huang, Fei; Tonetti, Debra A.; Thatcher, Gregory R. J.; Xiong, Rui, which mentions a compound: 87240-07-1, SMILESS is O=[N+](C1=CC2=C(NC=C2)C(Br)=C1)[O-], Molecular C8H5BrN2O2, HPLC of Formula: 87240-07-1.
Acquired resistance to fulvestrant and palbociclib is a new challenge to treatment of estrogen receptor pos. (ER+) breast cancer. ER is expressed in most resistance settings; thus, bromodomain and extra-terminal protein inhibitors (BETi) that target BET-amplified ER-mediated transcription have therapeutic potential. Novel pyrrolopyridone BETi leveraged novel interactions with L92/L94 confirmed by a cocrystal structure of 27 with BRD4. Optimization of BETi using growth inhibition in fulvestrant-resistant (MCF-7:CFR) cells was confirmed in endocrine-resistant, palbociclib-resistant, and ESR1 mutant cell lines. 27 was more potent in MCF-7:CFR cells than six BET inhibitors in clin. trials. Transcriptomic anal. differentiated 27 from the benchmark BETi, JQ-1, showing downregulation of oncogenes and upregulation of tumor suppressors and apoptosis. The therapeutic approach was validated by oral administration of 27 in orthotopic xenografts of endocrine-resistant breast cancer in monotherapy and in combination with fulvestrant. Importantly, at an equivalent dose in rats, thrombocytopenia was mitigated.
There is still a lot of research devoted to this compound(SMILES：O=[N+](C1=CC2=C(NC=C2)C(Br)=C1)[O-])HPLC of Formula: 87240-07-1, and with the development of science, more effects of this compound(87240-07-1) can be discovered.
Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem