1404449-01-9

Upstream product

• 2033-24-1 cycl-isopropylidene malonate 
• 1583-58-0 2,4-difluoro-benzoic acid 
• 72482-64-5 2,4-difluorobenzoyl chloride 

Downstream Products

• 58101-23-8 ethyl 3-(2,4-difluorophenyl)-3-oxopropanoate 
• 1436418-48-2 C₁₇H₁₃ClF₂N₂O₃ 
• 1436418-49-3 C₁₇H₁₃F₃N₂O₃ 

Relevant academic research and scientific papers

Synthesis and antitumor activity of novel 4-(2-fluorophenoxy)quinoline derivatives bearing the 4-Oxo-1,4-dihydroquinoline-3-carboxamide moiety

A series of 4-(2-fluorophenoxy)quinoline derivatives bearing the 4-oxo-1,4-dihydroquinoline-3-carboxamide moiety were designed, synthesized, and evaluated for their in vitro antitumor activity against the H460, HT-29, MKN-45, U87MG, and SMMC-7721 cancer cell lines. Most of the tested compounds showed potent activity and high selectivity toward the HT-29 and MKN-45 cell lines. Furthermore, compounds 21b, 21c, and 21i were further examined for their c-Met kinase activity and exhibited strong efficacy with IC50 values in the single-digit nanomolar range, which was comparable with the positive control foretinib. The most promising compound 21c showed excellent cytostatic activity with IC50 values from 0.01 to 0.53 μM against all tested cell lines, thus being 1.7-2.2 times more active than foretinib. Novel 4-(2-fluorophenoxy)quinoline derivatives bearing the 4-oxo-1,4-dihydroquinoline- 3-carboxamide moiety were evaluated for their in vitro antitumor activity against several cancer cell lines. Compounds 21b, 21c, and 21i were also examined for their c-Met kinase activity in comparison to foretinib. Compound 21c showed excellent cytostatic activity with IC50 values from 0.01 to 0.53 μM against all tested cell lines and higher activity than foretinib.

Discovery of novel 4-(2-fluorophenoxy)quinoline derivatives bearing 4-oxo-1,4-dihydrocinnoline-3-carboxamide moiety as c-Met kinase inhibitors

A series of novel 4-(2-fluorophenoxy)quinoline derivatives containing 4-oxo-1,4-dihydrocinnoline-3-carboxamide moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and six typical cancer cell lines (A549, H460, HT-29, MKN-45, U87MG and SMMC-7721). All the prepared compounds showed moderate to excellent antiproliferative activity, and the analysis of their structure-activity relationships indicated that 2-chloro or 2-trifluoromethyl substituted phenyl group on the 1-position of cinnoline ring was more favorable for antitumor activity. In this study, a promising compound 33, with a c-Met IC50 value of 0.59 nM, was identified as a multitargeted receptor tyrosine kinase inhibitor.

HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK

Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.