Calycosin derivative and synthesis method thereof

Abstract

The invention discloses a calycosin derivative and a synthesis method thereof. The derivative is prepared by the steps of: dissolving a compound 1 and a compound 2 in an organic solvent, making the compound 1 and the compound 2 react under a basic condition to obtain an intermediate product 3, and dissolving the intermediate product 3 and a compound 4 in an organic solvent to obtain the targeted crude product. Applicants find that the proliferation of human umbilical vein endothelial cells can be promoted by the derivative of low concentration, so that an effect of good vascular protection isachieved, and therefore the derivative can be applied to the preparation of ERalpha and GPR30 agonists; meanwhile, an inhibitory effect on MCF-7 cells can be generated by the derivative of low concentration (10 uM); the structures of the compound 1, the compound 2, the intermediate product 3 and the compound 4 which are involved in the derivative and the synthesis method of the derivative are shown as follows respectively.

Description

Technical field [0001] The invention relates to a mullein derivative and a synthesis method thereof, and belongs to the technical field of medicine. Background technique [0002] Astragalus is the dry root of Astragalus membranaceus (Fisch.) Bge.Var.mongholicus (Bge) Hsiao or Astragalus membranaceus (Fisch.) Bge. According to the pharmacopoeia, Astragalus is sweet in taste and mild in nature. It can nourish qi and raise yang, replenish health, improve heart function, expand coronary arteries, diuresis and swelling, support sore muscles, antibacterial, antiviral, anti-fatigue, anti-aging, and promote Hematopoietic function, liver protection and other functions. [0003] Calycosin is an isoflavone compound extracted and isolated from Astragalus membranaceus (Ma Xiaofeng et al., Study on Flavonoids in Mongolian Astragalus, Chinese Herbal Medicine, Vol. 36 No. 9, September 2005, p1293-1296 ), its structural formula is as follows: [0004] [0005] Existing studies have shown that mull...

AI Technical Summary

Problems solved by technology

[0005] Existing studies have shown that calycosin has the functions of anti-oxidative stress, anti-virus and regulating cell apoptosis, but its disadvantages are that its effective concentration is large and the target is not clear. It can promote the proliferation of ER-positive breast cancer cell MCF-7; although high concentrations of calycosin (>20μM) can inhibit the proliferation of ER-positive breast cancer cells MCF-7 and T47D, but it can inhibit the proliferation of ER-negative breast cancer cell MDA-MB-435s No effect (Zhou Liming, Chen Jian, The effect and mechanism of different concentrations of calycosin on ER-positive breast cancer cells, Proceedings of the 11th National Chemotherapy Pharmacology Symposium of Chinese Pharmacological Society, July 1, 2012, p322 -323)

Images