So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Feng, Yuxin; Xiao, Senhao; Chen, Yantao; Jiang, Hao; Liu, Na; Luo, Cheng; Chen, Shijie; Chen, Hua researched the compound: (S)-3-Methoxypyrrolidine( cas:120099-61-8 ).Reference of (S)-3-Methoxypyrrolidine.They published the article 《Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-one derivatives as BRD4 inhibitors》 about this compound( cas:120099-61-8 ) in European Journal of Medicinal Chemistry. Keywords: benzoindolone preparation BRD4 inhibitor antitumor cancer human; Acetyl-lysine binding pocket; BRD4 inhibitor; Benzo[cd]indol-2(1H)-one; Bromodomain and extra-terminal domain; Sulfonamide. We’ll tell you more about this compound (cas:120099-61-8).
A series of benzo[cd]indol-2(1H)-one derivatives were designed by structural optimization based on compound I and evaluated for their BRD4 (bromodomain-containing protein 4) inhibitory activity. The results showed that four compounds are the most potential ones with the IC50 values of 1.02 μM, 1.43 μM, 1.55 μM and 3.02 μM. According to their co-crystal structures in complex with BRD4_BD1 and the protein thermal shift assays, the binding modes were revealed that the addnl. indirect hydrogen bonds and hydrophobic interactions make such four compounds more active than I against BRD4. Furthermore, compounds I, 1-((1-ethyl-2-oxo-1,2-dihydrobenzo[cd]indol-6-yl)sulfonyl)pyrrolidine-2-carbohydrazide and 1-((1-ethyl-2-oxo-1,2-dihydrobenzo[cd]indol-6-yl)sulfonyl)pyrrolidine-2-carboxylic acid were chosen to evaluate for their antiproliferative activities on the MLL-AF4-expression acute leukemia cell line (MV4-11), other cancer cell lines and the non-cancer cell lines. The results showed that these compounds exhibited good and selective inhibitory activities against MV4-11 cells with the IC50 values of 11.67 μM, 5.55 μM, and 11.54 μM, resp., and could act on the cell proliferation by blocking cell cycle at G1 phase. They could markedly down-regulate the expressions of the c-Myc, Bcl-2 and CDK6 oncogenes in MV4-11 in the qRT-PCR and western blot studies, which further demonstrated that compound I and its derivatives could serve as a promising therapeutic strategy for MLL leukemia by targeting BRD4_BD1 protein.
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Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia