Introduction of a new synthetic route about 87240-07-1

I hope my short article helps more people learn about this compound(7-Bromo-5-nitro-1H-indole)HPLC of Formula: 87240-07-1. Apart from the compound(87240-07-1), you can read my other articles to know other related compounds.

HPLC of Formula: 87240-07-1. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 7-Bromo-5-nitro-1H-indole, is researched, Molecular C8H5BrN2O2, CAS is 87240-07-1, about 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.

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.

I hope my short article helps more people learn about this compound(7-Bromo-5-nitro-1H-indole)HPLC of Formula: 87240-07-1. Apart from the compound(87240-07-1), you can read my other articles to know other related compounds.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem