Crude acetone and ethanol extracts of the aerial parts of 21 Cephalaria species collected from Turkey were investigated for larvicidal and adult topical activity against Aedes aegypti. The ethanol extracts from C. elazigensis var. purpurea, C. anatolica, and C. elmaliensis possessed the highest mortality against first instar Ae. aegypti larvae. Luteolin-7-O-β-D-glycoside (1), isolated from C. elmaliensis ethanol extract, demonstrated 33% and 53% mortality at 0.1 μg/mL concentration against first instar ORL (susceptible) and PR (pyrethroid resistant) strains, respectively. C. scoparia acetone extract showed 100% mortality against adult Ae. aegypti. From this extract compounds 2-8 were isolated. Compound 2 (isoorientin) possessed the highest toxicity with 31.7% and 65% mortality at a 10 μg/mL concentration against adult ORL and PR strains, respectively. This is the first screening report of potential insecticides from Cephalaria species against the yellow fever mosquito, Ae. aegypti, and the active compounds (1 and 2) could lead to the development of a new class of insecticide.