Synthesis of 2,6-diaryl-substituted pyridines and their antitumor activities

Synthesis of some new bipyridines, thieno[2,3‐b]pyridines, and pyrazolo[3,4‐b]pyridines

“…Thus, it has been found that 2-acetylpyridine reacted with ethyl formate in dry ether containing sodium methoxide to give sodium salt of 3-hydroxy-1-(pyridin-3-yl)prop-2-en-1-one 1. Vol 49 takes place at the formyl group of the salt 1 and subsequent Michael cyclization followed by elimination of two moles of water leads to the [2,3 0 ]-substituted products 5, whereas in the second, initial nucleophilic attack by the methylene carbon takes place at the ketonic group, followed by cyclization and elimination of water leads to [3,4 0 ]bipyridine-substituted isomers 6. In fact, only isomer 5 was obtained because of the fact that initial attack of the active methylene carbon at the unhindered formyl group being much more probable than attack at the hindered and electronically disfavored ketonic group.…”

“…Treatment of bipyridine derivative 5b with iodomethane in ethoxide solution gave 6-methylsulfonyl [2,3 0 ]bipyridine derivative 7. Treatment of 5b with active methylene derivatives 8a-c in methanolic potassium hydroxide solution afforded the corresponding thieno [2,3-b]pyridine derivatives 10a-c, respectively (Scheme 2).…”

“…Pyridines and pyrazolopyridines have attained considerable interests due to their wide range of applications in medicine and agriculture, such as anti-inflammatory, antitumor, antimycobacterial, antifungal, and antiviral activities [1][2][3]. In the last decades, they are used as anticancer drugs, antihypertension, antifungal reagents, pesticides, herbicides, and plant growth reagents [4][5][6][7].…”

An Efficient Synthesis of Novel Pyrazole-Based Heterocycles as Potential Antitumor Agents

“…Some pyridine derivatives were studied for their topoisomerase inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. As a result, it has been reported that various pyridine derivatives, as bioisosteres of α-terthiophene (potent protein kinase C inhibitor) [23], have significant topoisomerase I and/or II inhibitory activity, and cytotoxicity against several human cancer cell lines [24][25][26][27][28]. Early reports on the ability of α-terpyridine to form metal complexes [29] and to and to bind with DNA/RNA [30] have been the base for the study on pyridine derivatives as antitumor agents.…”

Efficient synthesis of differently substituted triarylpyridines with the Suzuki-Miyaura cross-coupling reaction

“…13 Some polyarylated pyridines were found to be topoisomerase I and II inhibitors exhibiting toxicity toward human tumor cells depending on the nature of the aryl substituents. 14,15 Our previous studies in forensic chemistry were focused on the identification and synthesis of novel "route-specific" impurities, including dibenzylpyridines P1 and P2, and aryl/methylpyridines P3, and P4 ( Figure 1). [16][17][18][19][20] We also studied their interesting atropoisomeric properties and we investigated in detail the process of their formation, creating libraries of their 2-and 4-alkoxy and 2-and 4-amino derivatives.…”