Trioxane Derivatives
Patent Information:
Filing Country: USA
Application No: 09/743860
Filing Date: 15 April 2002
Patent No: 6649647
Issue Date: 18 November 2003
Inventor 1: Prof. Richard Kingston, HAYNES
Inventor 2: Dr. Wendy Wenluan, HSIAO
Inventor 3: Dr. William Wai Lun, LAM
Inventor 4: . Jorg, BAUMGARTEN
Inventor 5: . Hans Georg, LERCHEN
Inventor 6: Dr. Ho Wai, CHAN
Inventor 7: Mr. Hing Wo, TSANG

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.
Potential Application   Advantage
- Antitumour agents for anti-cancer drugs
- Candidates for anti neoplastic drugs
  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
Patent documents are available at [], and can be viewed by inserting patent no., application no. or TTC code <TTC Code> into the corresponding field.
Contact information :
Ms Shirley Woo
(852) 2358 7918
HKUST R and D Corporation Ltd
(852) 2358 7917
Technology Transfer Center
香港九龍清水灣 香港科技大學