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采用活性基团拼接法将含氟苯甲醛与酮反应,合成了5个含氟单羰基姜黄素类似物,结构经IR,1HNMR及ESI-MS确认.对所合成的化合物进行了抗肿瘤活性测试(MTT法),结果表明,部分化合物对肿瘤细胞有较强的选择性抑制活性,其中2,6-二(4-氟亚苯基)环己酮(3a)和2,6-二(2-氟亚苯基)环己酮(3b)的抗肿瘤谱广,活性较好,就此对化合物3b作了单晶培养,并就晶体结构进行了X衍射分析.结构表明化合物3b属三斜晶系,空间群P-1.晶胞参数a=0.9222(2)nm,b=0.9732(2)nm,c=1.0127(2)nm,α=88.920(4)°,β=75.672(3)°,γ=62.404(3)°,V=0.7755(3)nm3,Z=2,Dc=1.329Mg?m-3,μ=0.097mm-1,F(000)=324,最终偏离因子R=0.0590,wR=0.1841.
Five reactive fluorocarbonylcurcumin analogs were synthesized by reactive group splicing method and their structures were confirmed by IR, 1HNMR and ESI-MS. The antitumor activity of the synthesized compounds was tested (MTT method), the results showed that some compounds have strong selective inhibitory activity on tumor cells, of which 2,6-bis (4-fluorophenylene) cyclohexanone (3a) and 2,6- -fluorophenylene) -cyclohexanone (3b) showed broad spectrum of anti-tumor activity and good activity. Compound 3b was single crystal culture and X-ray diffraction analysis was performed on the crystal structure of compound 3b. The structure showed that compound 3b belongs to triclinic (2) nm, c = 1.0127 (2) nm, α = 88.920 (4) °, β = 75.672 (3) ° , γ = 62.404 (3) °, V = 0.7755 (3) nm3, Z = 2, Dc = 1.329Mg? m-3, μ = 0.097mm- 1, F (000) = 324, final deviation factor R = 0.0590 , wR = 0.1841.