Inhibition of the Ras/Raf interaction and repression of renal cancer xenografts in vivo by an enantiomeric iridium(III) metal-based compound was written by Liu, Li-Juan; Wang, Wanhe; Huang, Shi-Ying; Hong, Yanjun; Li, Guodong; Lin, Sheng; Tian, Jinglin; Cai, Zongwei; Wang, Hui-Min David; Ma, Dik-Lung; Leung, Chung-Hang. And the article was included in Chemical Science in 2017.Recommanded Product: (S)-2-(4-(tert-Butyl)-4,5-dihydrooxazol-2-yl)phenol The following contents are mentioned in the article:
Targeting protein-protein interactions (PPIs) offers tantalizing opportunities for therapeutic intervention for the treatment of human diseases. Modulating PPI interfaces with organic small mols. has been found to be exceptionally challenging, and few candidates have been successfully developed into clin. drugs. Meanwhile, the striking array of distinctive properties exhibited by metal compounds renders them attractive scaffolds for the development of bioactive leads. Here, we report the identification of iridium(III) compounds as inhibitors of the H-Ras/Raf-1 PPI. The lead iridium(III) compound 1 exhibited potent inhibitory activity against the H-Ras/Raf-1 interaction and its signaling pathway in vitro and in vivo, and also directly engaged both H-Ras and Raf-1-RBD in cell lysates. Moreover, 1 repressed tumor growth in a mouse renal xenograft tumor model. Intriguingly, the Δ-enantiomer of 1 showed superior potency in the biol. assays compared to Λ-1 or racemic 1. These compounds could potentially be used as starting scaffolds for the development of more potent Ras/Raf PPI inhibitors for the treatment of kidney cancer or other proliferative diseases. This study involved multiple reactions and reactants, such as (S)-2-(4-(tert-Butyl)-4,5-dihydrooxazol-2-yl)phenol (cas: 135948-04-8Recommanded Product: (S)-2-(4-(tert-Butyl)-4,5-dihydrooxazol-2-yl)phenol).
(S)-2-(4-(tert-Butyl)-4,5-dihydrooxazol-2-yl)phenol (cas: 135948-04-8) belongs to oxazolidine derivatives. Oxazolidines are well known as key portions of bioactive molecules or precursors of chiral molecules, as well as established chiral auxiliaries. Oxazolidines are commonly used as metal ligands in asymmetric catalysis, synthetic intermediates in organic synthesis, and also used as the protecting groups.Recommanded Product: (S)-2-(4-(tert-Butyl)-4,5-dihydrooxazol-2-yl)phenol
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