發(fā)布時(shí)間：2018-04-03 04:08

  本文選題：齊墩果酸　切入點(diǎn)：熊果酸　出處：《有機(jī)化學(xué)》2016年04期

【摘要】：根據(jù)拼合原理,以天然產(chǎn)物齊墩果酸和熊果酸作為先導(dǎo)化合物,通過(guò)丁二酸連接片段,在C-28位分別導(dǎo)入哌嗪、N-甲基哌嗪及嗎啉片段,共設(shè)計(jì)、合成了12種未見文獻(xiàn)報(bào)道的齊墩果酸和熊果酸衍生物.利用IR、1H NMR、13C NMR和HRMS等波譜技術(shù)對(duì)所合成的目標(biāo)化合物進(jìn)行了結(jié)構(gòu)表征,并采用3-(4,5-二甲基-2-噻唑)-2,5-二苯基溴化四氮唑噻唑藍(lán)(MTT)法觀察其對(duì)癌細(xì)胞的抑制作用,結(jié)果表明化合物OA-4、OA-7、OA-8a、OA-8b、UA-4、UA-7、UA-8a和UA-8b對(duì)人乳腺癌細(xì)胞(MCF-7)、人宮頸癌細(xì)胞(Hela)和人肺腺癌細(xì)胞(A549)的抑制作用遠(yuǎn)優(yōu)于先導(dǎo)化合物齊墩果酸和熊果酸,且OA-4,OA-7,UA-4和UA-7與陽(yáng)性對(duì)照物Gefitinib的IC50值相當(dāng).
[Abstract]:According to the splicing principle, the natural products oleanolic acid and ursolic acid were used as the leading compounds, and the fragments of piperazine N-methylpiperazine and morpholine were introduced at C-28, respectively.Twelve derivatives of oleanolic acid and ursolic acid which have not been reported in literature have been synthesized.The structures of the target compounds were characterized by IR 1H NMR13 C NMR and HRMS spectra. The inhibitory effects of these compounds on cancer cells were observed by using the method of 3 ~ (4) O ~ (4) -dimethyl -2-thiazolium -2-diphenyl tetrazolium tetrazolyl thiazolyl blue (MTT).緇撴灉琛ㄦ槑鍖栧悎鐗㎡A-4,OA-7,OA-8a,OA-8b,UA-4,UA-7,UA-8a鍜孶A-8b瀵逛漢涔寵吅鐧岀粏鑳，

本文編號(hào)：1703539