Design, Synthesis And Biological Evaluation Of Camptothecin Derivatives

Camptothecin is a naturally occurring alkaloid compound. A number of biological activities such as antitumor, antiviral, antifungal, antipsoriasis, antiparasitic trypanosomes, insecticidal, have been reported for camptothecin and many related compounds and derivatives. At present, we mainly focus on its anti-cancer activity, often as a new camptothecin anticancer drugs lead compounds. Currently, there are about reports of the CPT as a pesticide. Pesticide science from the perspective of camptothecin as an alkaloid in plants with a variety of pesticides can be developed for the benefits.In order to seek for effective insecticidal activity of the compounds, the paper design of the two types of compounds (1) the introduction of the 5-position-CPT stable nitroxide spin labeled derivatives of camptothecin. (2) the introduction of different lipophilic groups, aromatic ring, heterocyclic aromatic, aliphatic chain into 7-position-CPT were synthesized.1. Based on having good activity of DRF-1042 as raw materials for the linking group of amino acids, eight pyrroline stable nitroxide radical labeled camptothecin derivatives were synthesized though associated DRF-1042 and pyrroline stable nitroxide radical with natural L-amino acid as linker. Camptothecin derivatives showed more effective antifungal against Botryodiplodia theobromae Pat., Colletotrichum gloeosporioides Penz, Colletotrichum musae (Berk. et Curt.) Arxrot, especially the inhibition of Botryodiplodia theobromae Pat disease is more obvious; camptothecin derivatives have cytotoxic activity against the Brontispa longissima (Gestro) and Prodenia litura(Fabricius), some of compounds have the significant cytotoxic activity against two types of test insects; camptothecin compounds have different levels of herbicidal activity aganist three kinds of weeds.2. Based on camptothecin as raw materials, thirteen camptothecin derivatives were synthesized with the carbonyl group into the 7-position-CPT. The results showed that most of derivatives against third instar larvae of coconut leaf beetle has insecticidal activity than the control group, effect of camptothecin and toosendanin. These compounds have delayed insecticidal activity.