2024年2月22日 · Herein, we describe the design, synthesis, and biological evaluation of a series of ENPP1 inhibitors based on the pyrido [2,3- d]pyrimidin-7-one scaffold. Optimization efforts led to compound 31 with significant potency in both ENPP1 inhibition and STING pathway stimulation in …

Pyrido (2,3-d)pyrimidine | C7H5N3 | CID 582898 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.

This review comprehensively summarizes the fast, facile, and economical synthetic methods for pyrido [2,3- d]pyrimidine derivatives over the past years, which are categorized based on different synthetic precursors, and evaluates their antitumor and antibacterial activities, aiming to make them better serve the cause of human health.

2023年1月12日 · The use of small molecular modulators to target the guanine nucleotide exchange factor SOS1 has been demonstrated to be a promising strategy for the treatment of various KRAS-driven cancers. In the present study, we designed and synthesized a series of new SOS1 inhibitors with the pyrido [2,3- d]pyrimidin-7-one scaffold.

2013年12月15日 · From a data-mining effort, the team has discovered analogues of pyrido [2,3-d]pyrimidines as potent enantio-selective inhibitors of DYRK1B. Cells treated with a tool compound from this series showed the same cellular effects as down regulation of …

Pyrido [2,3- d]pyrimidine is an emerging scaffold in medicinal chemistry having a broad spectrum of activities, including antitumor, antibacterial, CNS depressive, anticonvulsant, and antipyretic activities.

2024年10月1日 · In this study, we aimed to identify potent SHP2 inhibitors by designing and synthesizing 30 target compounds bearing pyrido [1,2- a]pyrimidin-4-one core using a two-round design strategy guided by scaffold hopping protocols.

2019年11月16日 · Pyrido [2,3-<i>d</i>]pyrimidines (<b>1</b>) are a type of privileged heterocyclic scaffolds capable of providing ligands for several receptors in the body. Among such structures, our group and others have been particularly interested in pyrido [2,3-<i>d</i>]pyrimidine-7 (8<i>H</i>)-ones (<b>2</b>) due …

Targeting ataxia telangiectasia mutated and Rad3-related (ATR) kinase is being pursued as a new therapeutic strategy for the treatment of advanced solid tumor with specific DNA damage response deficiency. Herein, we report a series of pyrido [3,2-d]pyrimidine derivatives with potent ATR inhibitory ac …

Pyrimidine derivatives 2a (IC 50 = 42 μΜ), 2f (IC 50 = 47.5 μΜ) and chalcone 1g (IC 50 = 17 μM) were the most potent lipoxygenase inhibitors. All the tested compounds were found to interact with glutathione, apart from 1h. Cell viability and cytotoxicity assays were performed with the HaCaT and A549 cell lines, respectively.