Comparison of a homologous series of benzonaphthyridine anti-cancer agents in mice: divergence between tumour and plasma pharmacokinetics

Abstract

The plasma pharmacokinetics of this series is related to changes in drug lipophilicity. However, the tumour pharmacokinetics reveals a strong dependence on the nitrogen substituent on the benzonaphthyridine chromophore, with the methyl group providing by far the best tumour tissue retention.

One‐Pot Synthesis of Fused [1,6]Naphthyridine Derivatives via Three‐Component Reaction

“…In view of the biological significance of naphthyridine alkaloid analogs (Figure ), 11c in particular functionalized [1,6] naphthyridines and their benzo/hetero‐fused analogs that show a broad spectrum of physiological activities, such as anticancer (Figure ), antiproliferative, anti‐intestinal nematode, and antimalarial activities, we attempted to synthesize a series of benzo(1,6)naphthyridine derivatives In addition, napthyridine derivatives are used as the clinical stage inhibitors of the protein kinase CK2 for the treatment of cancer (Figure ) and as inhibitors of autotoxins for the treatment of tumors . Though there have been reports in the literature on the synthetic procedures to obtain these analogs, most of the procedures involve multistep syntheses with relatively low product yields.…”