Synthesis and Anticancer Properties of Functionalized 1,6-Naphthyridines

Synthesis, In Vitro Cytotoxicity, and DFT Studies of Novel 2‐Amino Substituted Benzonaphthyridines as PDK1 Inhibitors

“…[1,2] These nitrogen containing heterocycles holding amine scaffolds revealed a significant role in the drug discovery, which showed potential anticancer activity against different human cancer cell lines. [3][4][5] The 3-phosphoinositide-dependent protein kinase 1 (PDK1) inhibitors play a significant role in cancer cell growth, survival, and tumor angiogenesis for drug discovery. [6][7][8][9][10] PDK1 inhibitors represent a promising target for anticancer drugs in small molecules.…”

“…Nitrogen containing heterocycles provide with their significant importance in the drug design and drug discovery approved by the FDA database [1,2] . These nitrogen containing heterocycles holding amine scaffolds revealed a significant role in the drug discovery, which showed potential anticancer activity against different human cancer cell lines [3–5] . The 3‐phosphoinositide‐dependent protein kinase 1 (PDK1) inhibitors play a significant role in cancer cell growth, survival, and tumor angiogenesis for drug discovery [6–10] .…”

Efficient synthesis of benzo[h]carbazol[3,2‐b][1,6]naphthyridines

“…The strong DNA binding affinity of 1,6‐naphthyridines is considered to be at least partially important for their therapeutic benefits [7]. The 1,6‐naphthyridine moiety is a major pharmacophore found in a wide range of naturally occurring and synthetically created pharmaceutical substances [8].…”

One‐Pot Synthesis of New Chromeno[1,6]naphthyridine Derivatives Catalyzed by a Basic Ionic Liquid, [HO‐CH2‐CH2‐NH3+][HCOO−]

“…[11] The chromeno[4,3,2-de] [1,6] naphthyridine nucleus and its derivatives represent a remarkable and attractive scaffold in the field of medicinal chemistry and also acquire valuable biological as well as pharmacological properties. [12] Consequently, integration of chromene moieties with naphthyridines in a single molecular-framework may increase their biological and fluorescence properties. [13] While a considerable number of naphthyridines fused with five-membered rings have been described in literature, but derivatives condensed with sixmembered heterocycles have been less investigated.…”

“…Heterocyclic compounds are popular targets for organic chemists because of their wide applications in pharmaceuticals as well as in the drug's industry [11] . The chromeno[ 4,3,2‐de ][ 1,6 ] naphthyridine nucleus and its derivatives represent a remarkable and attractive scaffold in the field of medicinal chemistry and also acquire valuable biological as well as pharmacological properties [12] . Consequently, integration of chromene moieties with naphthyridines in a single molecular‐framework may increase their biological and fluorescence properties [13] .…”