Beilstein J. Org. Chem.2021,17, 558–568, doi:10.3762/bjoc.17.50
-929 cell line, proved that some amino derivatives of phthalazinone show interesting anticancer activities. The detailed synthesis, spectroscopic data, and biological assays are reported.
Keywords: amination; complexes; cytotoxicity; Pd cross-coupling; phthalazinone; Introduction
Phthalazine and its
anticancer drug vatalanib [26][27][28] (Figure 1). On the other hand, aminophthalazinones can be prospective candidates as N- and O-donor ligands to form complexes with biological significant metal ions, such as copper or zinc [29].
Recently, we have demonstrated a strategy for the synthesis of phthalazinone
phthalazinone derivatives 5 and 6 (Scheme 1, route B).
In the literature, the number of reported synthetic methods for 4-aminophthalazin-1(2H)-ones is limited to a few examples and they usually involve two main approaches: 1) the application of multicomponent reactions starting from, e.g., the available o
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Graphical Abstract
Figure 1:
Structure of biologically active phthalazine derivatives.