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用2,6-二羟基苯乙酮和相应的苯甲醛在60％氢氧化钾溶液存在下制备了六个2′,6′-二羟基取代查耳酮(Ⅳ_(a-f)),又从2-羟基取代苯乙酮和相应的苯甲醛制备了2′-羟基取代查耳酮(Ⅴ_(a-t))二十个。利用相似的方法制备了另一系列的取代查耳酮(Ⅵ_(a-f))六个。化合物Ⅳ_d,Ⅴ_a,Ⅴ_b,Ⅴ_c,Ⅴ_e,Ⅴ_f和Ⅴ_i在浓度为125微克/每毫升,化合物Ⅳ_a,Ⅳ_b,Ⅳ_f,Ⅴ_d,Ⅴ_k,Ⅴ_r,Ⅴ_s,Ⅳ_a,Ⅳ_b,Ⅳ_c和Ⅳ_f在浓度为250微克/每毫升体外试验对Ehrlich腹水瘤有明显抑制作用。但体内试验上述三系列32个查耳酮在口服时对小白鼠肉瘤-180或Ehrlich腹水瘤无明显抑制作用。
Six 2 ’, 6’-dihydroxy-substituted chalcone (Ⅳ_ (af)) were prepared from 2,6-dihydroxyacetophenone and the corresponding benzaldehyde in the presence of 60% potassium hydroxide solution. - hydroxy substituted acetophenones and the corresponding benzaldehydes were prepared twenty (2) - hydroxy substituted chalcone (Ⅴ_ (at)). Another series of substituted chalcone (Ⅵ_ (a-f)) were prepared by a similar method. Compounds IV_a, IV_b, IV_f, V_d, V_k, V_r, V_s, IV_a, IV_b, IV_c and IV_f at a concentration of 250 micrograms per milliliter of compounds IV_d, V_a, V_b, V_c, V_e, / Ml in vitro test on Ehrlich ascites tumor significantly inhibited. However, in vivo tests of the above three series of 32 chalcone oral administration of mouse sarcoma -180 or Ehrlich ascites had no significant inhibitory effect.