Out-licensing

Method for the High-Yield and Efficient Synthesis of Camptothecin

Introduction/Background

Camptothecin is a pentacyclic alkaloid initially isolated from the wood and back of Camptotheca acuminata. Camptothecin is highly biologically active and displays strong inhibitory activity toward the biosynthesis of nucleic acids. Additionally, camptothecin exhibits potent anti-tumour activity against experimentally transplanted carcinoma such as leukaemia L-1210 in mice or Walker 256 tumour in rats.

Several methods for the synthesis of camptothecin and camptothecin analogues are known. These synthetic methods include (i) methods in which naturally occurring camptothecin is synthetically modified to produce a number of analogues and (ii) totally synthetic methods.

Aims/Hypothesis

There exists a need, therefore, for a high-yield, efficient synthesis of camptothecin and camptothecin analogues which does not require prior isolation of naturally occurring camptothecin.

Research

A method for synthesizing camptothecin and camptothecin analogues using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogues produced by the process. The camptothecin analogues are effective inhibitors of topoisomerase I and show anti-leukemic and anit-tumour activity.

Conclusion

Our research provides a method of synthesizing camptothecin and camptothecin analogues in high yield in a totally synthetic process.

Relevance/Opportunity

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Preclinical

Patent No.: 5122526