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Molecules 2017, 22(11), 1811; doi:10.3390/molecules22111811

Design, Synthesis and Bioactivity Evaluation of Novel β-carboline 1,3,4-oxadiazole Derivatives

1
Key Laboratory of Natural Pesticide and Chemical Biology, Ministry of Education, Guangzhou 510642, China
2
Lab of Insect Toxicology, South China Agricultural University, Guangzhou 510642, China
*
Author to whom correspondence should be addressed.
Received: 4 October 2017 / Revised: 15 October 2017 / Accepted: 19 October 2017 / Published: 29 October 2017
(This article belongs to the Section Medicinal Chemistry)
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Abstract

A series of novel β-carboline 1,3,4-oxadiazole derivatives were designed and synthesized, and the in vitro cytotoxic activity against Sf9 cells and growth inhibitory activity against Spodoptera litura were evaluated. Bioassay results showed that most of these compounds exhibited excellent in vitro cytotoxic activity. Especially, compound 37 displayed the best efficacy in vitro (IC50 = 3.93 μM), and was five-fold more potent than camptothecin (CPT) (IC50 = 18.95 μM). Moreover, compounds 5 and 37 could induce cell apoptosis and cell cycle arrest and stimulate Sf-caspase-1 activation in Sf9 cells. In vivo bioassay also demonstrated that compounds 5 and 37 could significantly inhibit larvae growth of S. litura with decreasing the weight of larvae and pupae. Based on these bioassay results, compounds 5 and 37 emerged as lead compounds for the development of potential insect growth inhibitions. View Full-Text
Keywords: β-carboline; cytotoxic activity; Sf9 cells; Spodoptera litura; growth inhibitory activity β-carboline; cytotoxic activity; Sf9 cells; Spodoptera litura; growth inhibitory activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Zhang, Z.-J.; Zhang, J.-J.; Jiang, Z.-Y.; Zhong, G.-H. Design, Synthesis and Bioactivity Evaluation of Novel β-carboline 1,3,4-oxadiazole Derivatives. Molecules 2017, 22, 1811.

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