|
|
Home > Fused xanthone derivatives as antiproliferative ag
| | |
|
Blog - Fused Xanthone Derivatives as Antiproliferative Agents
|
Last Updated January, 2009
|
|
Xanthones have been isolated from several natural sources, mainly belonging in Guttiferae and Gentianaceae families as secondary plant metabolites and many of them are endowed with diverse pharmacological properties. We have focused in the study of cytotoxic fused xanthone derivatives, having in mind that some furano- and pyranoxanthone natural products are particularly interesting, in terms of cytotoxic potency and novelty in their mechanism of action and could serve as lead compounds for the development of clinically effective anticancer agents. In this review, a general classification has been attempted based on the type of ring fusion, in such a way that natural compounds as well as synthetic derivatives are discussed. The furanoxanthone psorospermin is a highly promising isolated xanthone derivative exhibiting significant cytotoxicity through a novel mechanism of action, being an irreversible topoisomerase II poison and it was selected for further development as an antineoplastic agent. An important number of pyranoxanthones have been synthesized using as lead compound the acridone alkaloid acronycine. Adducts on the double bond of these compounds provided cytotoxic derivatives possessing cell-cycle selectivity. The synthesis of pyranoxanthones bearing aminosubstituted side-chains resulted in compounds that exhibit markedly improved cytotoxicity towards leukemic and solid tumor cell lines. Azabioisosters of the aminoderivatives exhibit solid tumor selectivity whereas additional pyrazole or/and benzene ring fusion has been incorporated into the xanthone skeleton and resulted in compounds with promising activity, which retain full antiproliferative activity against P-glycoprotein-overexpressing cells. Gambogic acid, a highly effective anticancer drug candidate with low toxicity to normal tissue, together with structurally related representative analogues are also mentioned.
|
|
Posted by Pouli N, Marakos P. on January, 2009
|
| Comments 0 of 0
|
|
|
|
If you would like to comment on this post, please fill out the form below.
|
* denotes required field
Post Your Comments On*
Comment*
99999 characters remaining
|
| *All comments will undergo a review process before they are posted online. This is to prevent spam and ads from being posted. Thank you for your time and patience.
|
|
Opinions expressed on the ACC Corporation Blog and all corresponding comments are the individual opinions of the original authors and don’t in any way reflect the opinions of ACC Corporation.
|
| |
| | |
|
You must be logged in to view your shopping cart information
We accept all major credit cards
We have clients in over
75 countries spanning 5
continents
Advertise with American Custom Chemical Corporations. We make it beneficial and profitable for you to work with us.
To track your order please click on the shipping options below
For the latest updates on industry information and news
|
|