Peipei Han, Wenhua Zhou, Mingxia Chen and Qiuan Wang* Pages 117 - 121 ( 5 )
A series of eight polymethoxychalcone Mannich base derivatives 2a-2h was synthesized via the microwave-assisted Mannich reaction of natural product 2'-hydroxy-3,4,4',5,6'-pentamethoxychalcone (1) with various secondary amines and formaldehyde. Compared to conventional heating method (80°C), the microwave-assisted method (700W, 65°C) is efficient with short reaction time (0.5-1 h) and good yields (74-88%). The antiproliferative activities of eight Mannich base derivatives were evaluated in vitro on a panel of three human cancer cell lines (Hela, HCC1954 and SK-OV-3) by CCK-8 assay. The results showed that all of the Mannich base derivatives exhibited potential antiproliferative activities on tested cancer cell lines with the IC50 values of 9.13-48.51 µM. Some active compounds exhibited more activity as compared to positive control cis-Platin. Among them, compound 2b revealed to have the strongest antiproliferative activity against all the three cancer cell lines with IC50 values ranging from 9.13 to 11.24 µM.
Polymethoxychalcone, mannich base derivatives, microwave-assisted synthesis, antiproliferative activity, cancer cells, formaldehyde.
College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, Hunan Key Laboratory of Processed Food for Special Medical Purpose, Central South University of Forestry and Technology, Changsha 410004, College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082