|Authors||Haynes, Richard K.
Chan, Ho Wai
Tsang, Hing Wo
Hsiao, W. L. Wendy
|Source||US Patent, 6,649,647 B1, 2003|
|Summary||New methods for preparing analogues of qinghaosu (QHS, or artemisinin) and synthetic trioxane derivatives are developed. These new derivatives which have attached DNA-ligating groups are capable of aligning the trioxane nucleus proximate to specified base sequences in DNA. Despite the idea of combining DNA-binding and other ligands to pharmacophorea is not new, these derivatives synthesized are of new chemical entities. They were also tested for cytotoxicity and neurotoxity and screened against tumour cell lines. Results are very positive and some of the compounds are found to be active. The invention has the potential of providing a new array of drugs based on the trioxane pharmacophore. They can be developed into antitumour agents which act by selective destruction of DNA in tumour cells. Other potential applications include candidates for development into antineoplastic drugs. Currently, there are no examples of specific compounds of this kind reported in any literature.|
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