Abstract
Continuing our search for natural product-based compounds for the control of Brontispa longissima Larvae, 31 camptothecin analogs were first tested for their insecticidal activity against the fifth-instar larvae of B. longissima in vivo. Among them, compounds 6–8, 11, 26, 28, and 29 showed more promising and pronounced insecticidal activity than toosendanin, a commercial insecticide derived from Melia azedarach. The different insecticidal activity ranges of compounds 1–31 indicated that variation of chemical structures in the camptothecin skeleton markedly affected the activity profiles of this compound class, and some important SAR information has been revealed from it. The quantitative structure–activity relationship (QSAR) model was applied to provide insight into the camptothecin analogs’ structural properties that are responsible for their activities. The results obtained from SAR analysis showed good correlation with the QSAR studies, which allowed for the rational design of more potent camptothecin analogs in the development of potential new insecticides.
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Acknowledgments
This work was financially supported by the National Natural Science Foundation of China (30800720); the Post-Doctor Research Foundation (20090450142); the Fundamental Research Funds for the Central Universities (lzujbky-2013-69); Key Scientific Research Programme of EPPI (2010hzsZDZX003) of Chinese Academy of Tropical Agricultural Science from the Ministry of agriculture; the Fundamental Research Funds for the Central Universities (zujbky-2010-134) and Natural Science Foundation of Gansu Province (0916RJZA033).
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Liu Yang and Zhi-Jun Zhang have contributed equally to this work.
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Yang, L., Zhang, ZJ., Liu, YQ. et al. Evaluation of insecticidal activity of camptothecin analogs against Brontispa longissima . Med Chem Res 23, 980–986 (2014). https://doi.org/10.1007/s00044-013-0703-4
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DOI: https://doi.org/10.1007/s00044-013-0703-4