ABSTRACT
The burgeoning interest in synthesis and biological applications of 1,6-naphthyridines reflects the importance of 1,6-naphthyridines in the synthetic as well as medicinal chemistry fields. Specially, 1,6-naphthyridines are pharmacologically active, with variety of applications such as anticancer, anti-human immunodeficiency virus (HIV), anti-microbial, analgesic, anti-inflammatory and anti-oxidant activities. Although collective recent synthetic developments have paved a path to a wide range of functionalized 1,6-naphthyridines, a complete correlation of synthesis with biological activity remains elusive. The current review focuses on recent synthetic developments from the last decade and a thorough study of the anticancer activity of 1,6-naphthyridines on different cancer cell lines. Anticancer activity has been correlated to 1,6-naphthyridines using the literature on the structure-activity relationship (SAR) along with molecular modeling studies. Exceptionally, at the end of this review, the utility of 1,6-naphthyridines displaying activities other than anticancer has also been included as a glimmering extension.
Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Naphthyridines/chemical synthesis , Naphthyridines/pharmacology , Antineoplastic Agents/chemistry , Cell Proliferation/drug effects , Drug Screening Assays, Antitumor , Humans , Models, Molecular , Molecular Structure , Naphthyridines/chemistry , Structure-Activity RelationshipABSTRACT
A new series of functionalized fused pyridines 4(a-i) and fused pyrido[2,3-d]pyrimidines 8(a-c) were designed and synthesized through a multi-component reaction where in pyridine ring formation step plays a key role. All the newly formed compounds were well characterized by spectral techniques such as FTIR, 1 HNMR, 13 CNMR, HRMS and XRD. The potential therapeutic activities such as anti-inflammatory activity by protein denaturation and RBC membrane stabilization methods, and anti-oxidant activity by DPPH scavenging method of the newly synthesized compounds were studied. Interestingly, in-vitro testing of these compounds reveals that the compounds 4d, 4g, 4i, 8a and 8b showed comparable anti-inflammatory activity with respect to the standard drug, diclofenac. Similarly, fused pyridine 4f showed excellent anti-oxidant activity when compared with the standard, ascorbic acid.