Studies on synthesis of novel pyrido[2,3-d]pyrimidine derivatives, evaluation of their antimicrobial activity and molecular docking

Kinase Inhibitors of Novel Pyridopyrimidinone Candidates: Synthesis and In Vitro Anticancer Properties

“…In the same time, 1 HNMR spectrum displayed two singlets at δ 12.26 and 13.01 ppm assignable for 2NH protons. Also, 13 CNMR spectrum showed signal at 178.01 ppm for C�S carbon. Treatment of hydrazine hydrate with thioxo derivative 3 afforded the corresponding 2-hydrazinyl derivative 4.…”

“…1 H NMR spectrum displayed two singlets at 5.60 and 12.55 attributed to NH 2 and NH protons of the new fused ring. 13 C NMR spectrum displayed the carbons at their expected regions, and MS gave a [M + ]-ion peak at m/z 355 equivalents to the molecular formula of 9. Figure 2 was screened against three human cancer cell lines (HepG2, PC3, or HCT-116) [23].…”

“…Heterocycles have emerged as strong scaffolds for numerous biological considerations [5] and represent a significant part in the designing and detection of novel pharmacologically active entities [6]. e pyridopyrimidine compounds are a group of fused heterocycles that possess various pharmacological applications as antitumor, topoisomerase I inhibitor, adenosine kinase inhibitor, growth regulator, antihepatitis C virus, antiinflammatory, antileishmanial, antiviral, antimicrobial, anticonvulsant, antimycobacterial, CNS depressant, antihypertensive, antiallergic, diuretic, tyrosine kinase inhibitor, and calcium channel antagonist [7][8][9][10][11][12][13][14][15][16]. Among them, pyrido [2,3-d] pyrimidin-4-ones (A-C) were found to lower cell proliferation in various cancer cell lines through inhibition of various kinases, e.g., TKs, PI3K, and CDK4/6 ( Figure 1) [17][18][19].…”

Synthesis and Pharmacological Evaluation of Some Amide Functionalized 1H‐Benzo[d]imidazole‐2‐thiol Derivatives as Antimicrobial Agents

“…Biofilm is a community of microorganisms enclosed in a self‐produced matrix of extracellular polymeric substance (EPS) which adhere to each other on living or non‐living surfaces . The ability of Staphylococcus aureus to form biofilms on biomaterial surfaces causes difficulty in eradicating these bacterial biofilms and also imparts resistance towards antimicrobial agents .…”

Magnetically recoverable copper ferrite catalyzed cascade synthesis of 1,3‐dimethyl‐6‐nitro‐5‐arylpyrido[2,3‐d]pyrimidine‐2,4(1H,3H)‐diones under microwave irradiation and solvent‐less condition

“…Research works toward construction of heterocyclic frameworks have always been constituting a pivotal area of research, as advancement of medicinal chemistry is considerably dependent on the development of newer and efficient synthetic methodologies for these heterocycles. Among various heterocycles, pyrido [2,3-d]pyrimidine is one of the most significant entities as numerous molecules bearing this core structure are established to have excellent biological activities like antitumor, [1][2][3][4][5] antitmicrobial, [6][7][8][9][10][11] anti-inflammatory, [12,13] herbicidal, [14] tyrosine kinase inhibitory activity, [15][16][17][18] and activity against dengue virus [19] . The moiety started gaining special attention from researchers dealing with antibacterial studies of synthesized compounds after the landmark publication by Stover et al in Proceedings of the National Academy of Sciences of the United States of America.…”