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1.
Top Curr Chem (Cham) ; 379(2): 13, 2021 Feb 24.
Article in English | MEDLINE | ID: mdl-33624162

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 Relationship
2.
Chem Biol Drug Des ; 93(4): 464-472, 2019 04.
Article in English | MEDLINE | ID: mdl-30393996

ABSTRACT

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.


Subject(s)
Anti-Inflammatory Agents/chemical synthesis , Antioxidants/chemistry , Pyridines/chemistry , Pyrimidines/chemistry , Animals , Anti-Inflammatory Agents/pharmacology , Antioxidants/chemical synthesis , Cattle , Cell Membrane/drug effects , Cell Membrane/metabolism , Erythrocytes/cytology , Humans , Pyridines/chemical synthesis , Pyridines/pharmacology , Pyrimidines/chemical synthesis , Pyrimidines/pharmacology , Serum Albumin, Bovine/chemistry , Serum Albumin, Bovine/metabolism , Spiro Compounds/chemistry
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