The toxic effect of 15 pyrazoline analogs against RP-HzVNC-AW1 (AW1) cells and the contacting activities against 3rd instar larvae of Locusta migratoria were measured by MTT assay and immersion method, then the relevance of cytotoxicity and bioactivity was discussed. It is suggested that 15 compounds had inhibitory effects on AW1 cells and the contacting activities of 15 compounds were observed. The relevance of cytotoxicity and bioactivity of Compound Ⅱ was better than compound Ⅰ. The inhibition rates of compoundsⅡ5、Ⅱ8 and Ⅱ9 were 76.82%, 75.41% and 65.87%, and the adjusted mortality of them were respectively 53.84 %, 52.91 % and 53.55 %, they exhibited well inhibitory effects against AW1 cells and high contacting activities against insects with a better relevance.