CA amide analogs and its preparation method and application
The invention relates to the technical field of medicines. Piplartine is alkaloid extracted from perennial herbaceous vine piper longum of piperaceae. The invention provides a Piplartine analogue, which comprises a cis-trans-isomer, and any arbitrary mixture in those forms or medicinal salt thereof, and the structural formula of the Piplartine analogue is shown in a general formula (I). The invention also provides a preparation method of substituted Piplartine compounds, and an application thereof in preparation of an antitumor medicament.
-
Paragraph 0104-0106; 0108-0110
(2016/10/09)
Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents
In an effort to expand the structure-activity relationship of the natural anticancer compound piperlongumine, we have prepared sixteen novel piperlongumine derivatives with halogen or morpholine substituents at C2 and alkyl substituents at C7. Most of 2-halogenated piperlongumines showed potent in vitro activity against four cancer cells and modest selectivity for lung normal cells. The highly active anticancer compound 11h exhibited obvious ROS elevation and excellent in vivo antitumor potency with suppressed tumor growth by 48.58% at the dose of 2 mg/kg. The results indicated that halogen substituents as electrophilic group at C2 played an important role in increasing cytotoxicity.