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.

对1，6-萘啶的合成和生物学应用的迅速增长的兴趣反映了1，6-萘吡啶在合成以及药物化学领域中的重要性。特别地，1,6-萘啶类具有药理活性，具有多种应用，例如抗癌，抗人免疫缺陷病毒（HIV），抗微生物，止痛，抗炎和抗氧化活性。尽管最近合成技术的发展为各种功能化的1，6-萘啶铺平了道路，但合成与生物学活性的完全相关性仍然难以捉摸。本综述着眼于近十年来的合成研究进展，以及对1,6-萘啶类化合物对不同癌细胞系的抗癌活性的透彻研究。抗癌活性与1相关，使用关于结构-活性关系（SAR）的文献以及分子模型研究研究了6-萘啶。例外地，在本评价的最后，显示除抗癌活性外的1,6-萘啶类化合物的实用性也已包含在内。