肿瘤的化学治疗 ⅩⅧ.若干取代查耳酮的制备

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。

TUMOUR CHEMOTHERAPY ⅩⅧ. PREPARATION OF SEVERAL SUBSTITUTED CHALCONES

Six 2′,6′-dihydroxy-substituted-chalcones (Ⅳa—f), twenty 2′-hydroxy-substituted chalcones (Ⅴa—t) and six substituted chalcones (Ⅵa—f) were prepared as potential antitumour agents. Preliminary biological test indicated that compounds Ⅳd, Ⅴa, Ⅴb, Ⅴc, Ⅴe, Ⅴf and Ⅴi possessed inhibitory action in vitro against Ehrlich ascites tumour at a concentration of 125γ/ml, and compounds Ⅳa, Ⅳb, Ⅳf, Ⅴd, Ⅴk, Ⅴr, Ⅴs, Ⅵa, Ⅵb, Ⅵc and Ⅵf also showed inhibiting action against the same turnout at a concentration of 250γ/ml in vitro. However, none of them showed any significant activity against Ehrlich ascites tumour or sarcoma-180 in mice.