In order to obtain new antiproliferative compounds good for acting through the
forementioned mechanisms, including DNA intercalation and topoisomerase inhibition, our
attention was focused on the derivatives of pyridophenoxazinone (PPH, 1 R=H) system, an
iminoquinone containing a planar tetracyclic system suitable for intercalating DNA G-C base pairs
in a site specific mode(2).
Namely, we designed, after molecular modeling calculations, PPH carboxyamide derivatives
holding at C-9 and C-10 positions an amino acidic chain or a sugar.
Unfortunately, the real obstacle to the availability of such molecule was represented by their
synthesis. Therefore, in our opinion it seems to be worthwhile to report a new microwave (μW)
assisted synthetic procedure to prepare PPH carboxyamides. In order to assess the validity of our
method, we applied the procedure to the synthesis of variously substituted PPHs 1 and received
evidence that microwave irradiation enables the preparation of those compounds in high yields and
short reaction times
