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1.
Org Biomol Chem ; 21(35): 7173-7179, 2023 Sep 13.
Article in English | MEDLINE | ID: mdl-37609939

ABSTRACT

An 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 nitrogen-containing quaternary stereocenter in high yields with excellent enantioselectivities and regioselectivities under mild conditions. In addition, we utilized the target products to construct a range of bi-heterocyclic skeletons through [3 + 2] cycloadditions. These novel hybrid heterocycles would be promising candidates for drug-discovery programs and chemical biology.

2.
Molecules ; 28(7)2023 Mar 24.
Article in English | MEDLINE | ID: mdl-37049689

ABSTRACT

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 ß-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).

3.
Pak J Pharm Sci ; 35(2): 605-612, 2022 Mar.
Article in English | MEDLINE | ID: mdl-35642418

ABSTRACT

Fifteen novel 4-amino-quinolines (I1-III3) as antitumor agent were synthesized by p-nitroaniline and ethoxymethylene malonic ester (EMME) via condensation, cyclization, hydrolysis, decarboxylation, chlorination, nucleophilic substitution, reduction and amidation. The antitumor activity of compounds I1-III3 was evaluated on SGC-7901, BEL-7402 and A549 cancer cell lines. In vitro bioassay indicated that some compounds showed different degree activity against all tested cancer cell lines. Compound I1, I4 and II2 exhibited high effects against A549 cell lines (IC50 = 1.34µM, 1.36µM and 3.00µM, respectively). In addition, the result of molecular docking showed that compound I1, I4 and II2 could dock into the pocket of EGFR.


Subject(s)
Antineoplastic Agents , Quinolines , A549 Cells , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Humans , Molecular Docking Simulation , Quinolines/pharmacology , Uricosuric Agents
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