Synthesis And Anti-Thyroid Cancer Effect Of Iodo-Chrysin Derivatives

In recent years, Incidence of thyroid cancer has increased annually. A series of adverse drug reactions and tumor cells drug resistance which limits the application of anti-thyroid drugs. Therefore, it is urgent that research efficiency and low toxicity of anti-thyroid cancer drugs. There have been growing interests in modifying the structure of reactive natural products which were regarded as leading compounds to obtain novel anti-thyroid cancer medicine with high efficacy and low toxicity. Chrysin as a natural flavonoid, has been reported to possess great anticancer activity on human thyroid cancer in vitro. However, due to its low bioavailability, chrysin's clinical application was limited. Iodine is the synthesis of thyroid hormone essential raw materials and incidence of thyroid cancer with thyroid hormone secretion inseparable. Our laboratory will consider the introduction of iodine chrysin synthesized a series of chrysin derivatives research of its anti-cancer activity of the thyroid. This paper could divide into two parts as following:Part one: Eighteen novel iodo-chrysin derivatives with resorcinol as raw materials were synthesized according to Houben-Hoesch reaction, aldol condensation, cyclization acidification and alkylation reactions.Part two: Iodo-chrysin derivatives inhibitory activities in vitro against thyroid cancer cell lines(SW-579 and TT) were evaluated by the standard MTT method. Biological test results showed that these derivatives possessed stronger anti-thyroid cancer activities than 5-FU. Compound 10 showed the strongest activity against TT cell lines with IC50 value of 6.268 ?M and compound 21 showed the strongest activity against SW-579 cell lines with IC50 value of 3.488 ?M, it was better than 5-FU(18.411 ?M, 59.391 ?? respectively).