One-Pot Synthesis of Isoindolin-1-ones with Thiamine Hydrochloride (VB₁) as a Catalyst and Their Inhibitory Activity Against Cancer Cell Lines

ABSTRACT

A simple, highly efficient and green three-component condensation for synthesis of 2-substituted-3-(2-oxoalkyl)isoindolin-1-one derivatives from phthalaldehydic acid, primary amine, and ketone in the presence thiamine hydrochloride (VB₁) as catalyst in water has been developed. Their activities have also shown inhibition activity against HeLa, A549, and Hep2 cancer cell lines. The results showed that some synthesized isoindolin-1-one derivatives have exhibited cytotoxic activity on HeLa, A549, and Hep-2 cancer cell lines at µg/mL concentrations.

KEYWORDS:

• Cytotoxic activity
• isoindolin-1-one
• phthalaldehydic acid
• thiamine hydrochloride (VB₁)

Funding

This work was supported by the Shanghai Biomedical Technology Support Program [grant number 15401901100]; Shanghai Natural Science Foundation [grant number 15ZR1408800]; Shanghai Pujiang Program [grant number 15PJD0122015]. (WY1414050); and Science Research Project-sponsored by MOET of Vietnam (B.2017-TNA-42).