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以姜黄素为先导化合物合成了两个对称的单羰基姜黄素类似物和五个查尔酮类单羰基姜黄素类似物,结构经IR,1HNMR及ESI-MS确认,用11种临床常用耐药株对其进行了体外抗菌活性筛选,同时采用MTT法测定了它们对3种人体肿瘤细胞株的细胞毒活性.其中化合物A5的体外抗肿瘤活性与姜黄素相当,并且A5对部分临床耐药菌也有一定的抑菌活性.通过单晶培养得到了A5的晶体结构,经测定表明其结构属于正交晶系,空间群Fdd2.晶胞参数a=26.085(3),b=28.248(3),c=7.9615(9),α=90.00°,β=90.00°,γ=90.00°,V=5866.4(12)3,Z=16,DX=1.288Mg/m3,μ=0.09mm-1,F(000)=324,最终偏离因子R=0.047,wR=0.112.
Two symmetrical monocarbonylcurcumin analogues and five chalcone monocarbonylcurcumin analogues were synthesized with curcumin as the lead compound. The structures were confirmed by IR, 1HNMR and ESI-MS, Strains were screened for their antimicrobial activity in vitro, and their cytotoxic activities against three human tumor cell lines were determined by MTT assay, in which the anticancer activity of compound A5 was comparable to that of curcumin, and A5 was resistant to some clinically resistant bacteria The results showed that the crystal structure of A5 belongs to the orthorhombic system with space group Fdd2. The unit cell parameters a = 26.085 (3) and b = 28.248 (3) c = 7.9615 α α = 90.00 ° β = 90.00 ° γ = 90.00 ° V = 5866.4 123 Z = 16 DX = 1.288 Mg / m3 μ = 0.09 mm- 1, F (000) = 324, final deviation factor R = 0.047, wR = 0.112.