Background:
Three series of new 7-fluoro-4-(1-piperazinyl) quinolines (I1~I6, II1~II2 and
IV1~IV4) were synthesized. Their anti-tumor activity was evaluated in vitro against three human
carcinoma cell lines, namely SGC-7901 cells, BEL-7402 cells and A549 cells expressing high levels of
EGFR by Methyl Thiazolyl Terazolium (MTT) assay.
Methods:
Three series of quinoline derivatives were synthesized, characterized and evaluated for their
in vitro anti-tumor activities.
Results and Discussion:
Structures of the newly synthesized compounds were confirmed by spectral
analysis. The preliminary bioassay indicated that compounds I1, I10 and II1 exhibited better anti-tumor
activity than the rest of the target compounds and gefitinib against A549 cell based assay, which
demonstrated that compounds I1, I10 and II1 are potential agents for cancer therapy. Results suggested
that the substitutes on piperazinyl influenced anti-tumor activities remarkably.
Conclusion:
These results are useful for discovering more potent novel anti-tumor compounds and
further studies are ongoing.
The concurrent construction of 1,3-stereocenters remains a challenge. Herein, we report the development of stereoselective union of a point chiral center with allenyl axial chirality in 1,3-position by Pd-catalyzed asymmetric allenylic alkylation between racemic allenyl carbonates and indanone-derived β-ketoesters. Various target products bearing a broad range of functional groups were afforded in high yield (up to 99%) with excellent enantioselectivities (up to 98% ee) and good diastereoselectivities (up to 13:1 dr).
The 4-isothiocyanato pyrazolones were exploited as a class of efficient synthon for the construction of triazoline derivatives via asymmetric [3+2] annulation of 4-isothiocyanato pyrazolones with azodicarboxylates, providing a wide range of structurally diverse multi-nitrogen-containing spirocycles in excellent yields (up to 97%) with excellent enantioselectives (up to 97% ee).
The efficient squaramide-catalyzed asymmetric allylic alkylation of 4-aminopyrazolones with various MBH carbonates via different pathways has been described. This method provides access to a series of pyrazolone derivatives bearing a...
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.