2H-1-苯并吡喃衍生物的合成及其体外抗癌活性的初步评价

摘要

Aim To design and synthesize novel 2H-1-benzopyran derivatives and to evaluate their anticancer activity.Methods 2'-Hydroxychalcones were transferred to flavones derivatives under microwave irradiation.The flavones derivatives were reacted with POCl3 to get 4-chloro-2H-chromene-3-carbaldehydes.Novel 2H-1-benzopyran derivatives were prepared by the reaction of various 4-chloro-2H-chromene-3-carbaldehydes with R3CONHNH2 under microwave irradiation combining solution phase parallel synthesis.HL-60 cell line was employed to evaluate anticancer activity of these compounds in vitro.Results and conclusion A combinatorial library containing 32 novel 2H-1-benzopyran derivatives was synthesized.Some of these compounds exhibited inhibitory activity against HL-60 cell proliferation.The inhibitory rate of compound 9e was 70.8% at the concentration of 30 μmol·L-1.%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POC13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%.