
SYNTHESIS OF POLYMETHOXYQUERCETIN MANNICH BASE DERIVATIVES AND THEIR ANTIPROLIFERATIVE ACTIVITY ON HUMAN CANCER CELL LINE
Author(s) -
VanSon Nguyen,
Ting An,
Nguyễn Văn Cường,
Vo Thanh Cong
Publication year - 2020
Publication title -
khoa học và công nghệ
Language(s) - English
Resource type - Journals
ISSN - 2525-2267
DOI - 10.46242/jst-iuh.v39i03.278
Subject(s) - hela , mannich base , chemistry , cervical carcinoma , cell culture , formaldehyde , mannich reaction , ic50 , proton nmr , carbon 13 nmr , in vitro , combinatorial chemistry , stereochemistry , biochemistry , cancer , organic chemistry , cervical cancer , biology , catalysis , genetics
Several novel of polymethoxyquercetin Mannich base derivatives (2-7) were synthesized through O-methylation and based on Mannich reaction with various secondary amines and formaldehyde, starting from abundant and inexpensive natural sources quercetin. All the synthesized compounds were confirmed by 1H NMR, 13C NMR and MS techniques and the synthetic compounds were test for antiproliferative activities on human cervical carcinoma Hela cell line by the standard CCK-8 assay, the result showed that most of the target compounds exhibited moderate to potent antiproliferative activities on Hela (cervical carcinoma) cell which is comparable to the positive control cis-Platin. Among them, polymethoxyquercetin Mannich base derivatives (2) showed the strongest activity (IC50 3.80 μM), they are potential and selective anticancer agent and worthy of further development