Design, Synthesis And Antitumor Activity Screening Of Novel Chalcone Derivatives

Tumor is a disease characterized by a series of abnormal cells uncontrolled proliferation and spread, is a serious threat to human lives and health, and is one of the important research topics to the medical profession,. According to statistics, the number of cancer mortality in the world each year is more than 790 million, and the number is more than 160 million in China and increasing year by year. There are many drugs for the treatment of cancer, however, the clinical effects of these drugs are not very satisfactory. Therefore, to find effective, safe, lower toxic effects of anticancer drugs and to conquer cancer has long been a sought-after goal that oncology drug development workers seek for. Chalcones were discovered originally in Plants. lt has many kinds of pharmacological activities. lt is an important way currently to explore new drugs applying active components in Chinese drugs as lead compound. Chalcones as lead compound have been modificated to discover and develop new anticancer drugs.A series of N-alkyl-substituted chalcones derivatives were synthesized based on the structure of chlcone in our lab. According to the initial invitro screening results, synthetic compounds showed potent inhibitory effect against tyrosine kinase and tumor cells.13 novel 5-N-alkyl-substituted chalcones derivatives were synthesized from 2,4-dihydroxyacetophenone by protection of hydroxyl group, Blanc reaction, N-alkylation and aldol condensation based on the research work. These structures were confirmed by 1H NMR .The synthesized compounds were evaluated in vitro with A-549(human lung adenocarcinoma cell line), SGC-7901 (human gastric carcinoma cell line), SW- 1990(human pancreatic cancer cell line), MCF-7 (human breast cancer cell line), L-1210 (human leukemia cell line) and SW-1990 (human pancreatic carcinoma cell lines) by MTT method. The synthesized chalcones showed different degree antitumor activities.