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Trioxane Derivatives

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.
Technology Benefits
1. Compounds are relatively accessible by conducting straight forward chemical transformation on starting materials that are commercially available in large quantities
2. Families of compounds can be prepared
3. Structural variation of the compounds can be achieved in control
4. More stable
Technology Application
- Antitumour agents for anti-cancer drugs
- Candidates for anti neoplastic drugs
Supplementary Information
Patent Number: US6649647B1
Application Number: US2001743860A
Inventor: Haynes, Richard | Chan, Ho Wai | Lam, Wai Lun | Tsang, Hing Wo | Hsiao, Wen Luan | Lerchen, Hans Georg | Baumgarten, Jörg
Priority Date: 14 Jul 1998
Priority Number: US6649647B1
Application Date: 15 Apr 2002
Publication Date: 18 Nov 2003
IPC Current: C07D049120 | C07D049320
US Class: 514450 | 4240092 | 514451 | 514452 | 549348
Title: Trioxane derivatives
Usefulness: Trioxane derivatives
Summary: As cytotoxic agents and antitumor agents for treating cancer.
Novelty: Use of new and known trioxane derivatives as cytotoxic agents for treating cancer
Disease Diagnostic/Treatment
Sub Category
Application Date
15 Apr 2002
Application No.
US 09/743860
Patent Information
US 6649647
ID No.
Hong Kong

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