1201646-91-4

Upstream product

• 853908-50-6 6-bromo-3-nitroquinolin-4-ol 
• 723281-72-9 6-bromo-4-chloro-3-nitroquinoline 
• 915019-51-1 2-(4-((6-bromo-3-nitroquinolin-4-yl)amino)phenyl)-2-methylpropanenitrile 
• 171364-85-5 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinoline 
• 5794-88-7 5-Bromo-2-aminobenzoic acid 
• 118-92-3 anthranilic acid 
• 1201643-75-5 (E)-5-bromo-2-((2-nitrovinyl)amino)benzoic acid 
• 1201646-89-0 C₁₈H₁₁N₃O₃ 
• 1201646-90-3 C₁₈H₁₀ClN₃O₂ 
• 115279-57-7 2-(4-aminophenyl)-2-methylpropionitrile 
• 1201646-88-9 C₁₅H₁₇BN₂O₅ 

Downstream Products

• 1201646-92-5 2-(4-((3'-amino[3,6'-biquinolin]-4'-yl)amino)phenyl)-2-methyl propanenitrile 
• 1201646-94-7 C₂₉H₂₁N₅ 
• 1201646-95-8 C₃₀H₂₁N₅O₂ 

Relevant academic research and scientific papers

Novel quinoline-derived mTOR inhibitors with remarkable enzymatic and cellular activities: Design, synthesis and biological evaluation

Herein, we reported the preparation and in vitro development of a novel series of quinoline-based mTOR inhibitors, some of which were obtained via introducing a ring-opening strategy. As for enzymatic activity, more than half of these quinoline derivatives exhibited moderate to potent inhibition against mTOR. Among them, six compounds showed IC50 values below 50 nM. In particular, several quinolines exhibited remarkably enhanced anti-proliferative activities against all the three tested tumor cell lines in contrast to the initial lead 9. As a representative in this series, compound 24 demonstrated IC50 values of 0.11, 0.17 and 0.04 μM against HCT-116, PC-3 and MCF-7 cell lines, respectively. Besides, compounds 17 and 24 were identified to be selective over class I PI3Ks. Further Western blot analysis validated the dual inhibition of mTORC1 and mTORC2 as a result of compound 24 treatment in the MCF-7 cell line, which was beneficial for conquering the S6K/IRS1/PI3K negative feedback loop. Moreover, acceptable stability was displayed by compound 17, another representative of this series, in simulated intestinal fluid (SIF), simulated gastric fluid (SGF), as well as rat liver microsome (RLM). By virtue of the favorable biological profiles, several quinolines merit further in vivo investigation.

PHOSPHATIDYLINOSITOL 3 KINASE INHIBITORS

Provided are compounds according to Formula (I), or stereoisomer, prodrug, polymorph, or pharmaceutically acceptable salt forms thereof, wherein X, Y, R1, R6 , R7, and R8 are as defined, which compounds are effective inhibitors of PI3-kinase and/or other medically and clinically relevant kinases. Also provided are pharmaceutical compositions and methods of using the compounds and compositions as PB -kinase and kinase inhibitors. More particularly, the compounds of the invention provide treatments and therapeutics for human diseases regulated by, or associated with, the activity of, PI3-kinases and/or protein kinases, or mutant or variant forms thereof.