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目的设计并合成2H-1-苯并吡喃衍生物化合库并对其体外抗癌活性进行评价。方法以2′-羟基查耳酮为原料通过微波促进合成得到黄酮衍生物中间体,此中间体与POCl3反应得到4-氯-2H-色原烯-3-醛,通过微波辅助液相平行合成的方法,此醛与R3CONHNH2反应得到2H-1-苯并吡喃衍生物化合库。利用HL-60细胞系评价该化合物库的体外抗癌活性。结果与结论合成了含有32个化合物的2H-1-苯并吡喃衍生物库,体外活性评价表明,部分化合物对HL-60细胞的增殖有一定的抑制作用,其中,化合物9e在浓度为30μmol·L-1的抑制率为70.8 %。
OBJECTIVE To design and synthesize 2H-1-benzopyran derivatives library and evaluate its antitumor activity in vitro. Methods 2’-hydroxy-chalcone was used as raw material to synthesize flavonoid derivatives by microwave irradiation. The intermediate was reacted with POCl3 to obtain 4-chloro-2H-chromen-3-aldehyde by microwave assisted liquid-phase parallel synthesis The reaction of this aldehyde with R3CONHNH2 gives the 2H-1-benzopyran derivative library. In vitro anticancer activity of this compound library was evaluated using the HL-60 cell line. RESULTS AND CONCLUSION: The library of 2H-1-benzopyran derivatives containing 32 compounds was synthesized. The in vitro activity of some compounds showed that some compounds could inhibit the proliferation of HL-60 cells. Among them, The inhibition rate of L-1 was 70.8%.