Synthesis of novel 2-alkyl triazole-3-alkyl substituted quinoline derivatives and their cytotoxic activity

Tandem synthesis of 1-formyl-1,2,3-triazoles

“…Analogs of the 4-formyl-1,2,3-triazole motif have recently been reported to display enzyme inhibitory, 22 anti-cancer 23,24 antileishmanial 25 and anti-tuberculosis activity. 26,27 With the aldehyde group an attractive handle for synthetic diversification, such compounds have also served as synthons for preparing bioimaging, 28 anti-cancer, 23,24 and antituberculosis 26,27 agents.…”

“…26,27 With the aldehyde group an attractive handle for synthetic diversification, such compounds have also served as synthons for preparing bioimaging, 28 anti-cancer, 23,24 and antituberculosis 26,27 agents. Likewise, 4-imino-1,2,3-triazoles formed from amine condensation reactions have been shown to be useful for constructing novel coordination compounds.…”

“…A two-step method of CuAAC reaction with propargyl alcohol followed by oxidation of the hydroxymethylated triazole intermediate with reagents such as CrO 3 24 or MnO 2 30 is effective but limited to substituents that can withstand such oxidants, and is environmentally unfriendly. Advances in this approach using organic oxidants 23,33 and polymer-immobilized two-component catalysis 34 methods have recently been reported. Lastly, two-step methods using CuAAC reactions with commercially available acetal-protected propargyl aldehydes followed by deprotection of the formyl group via acid-catalyzed hydrolysis are known, 35,36 but are limited to substituents tolerant of strong acids such as HCl or TFA.…”

Synthesis of Novel Pyrido[1,2-<i>a</i>]pyrimidine-3-carboxamide Derivatives and Their Anticancer Activity

“…Fused pyrimidine derivatives are extensively used in neurology, particularly in the treatment of neurodegenerative disorders such as Parkinson's disease, 23) antianxiety disorders, 24) and depression. 25) Recent literature also shows that the trifluoromethyl 26,27) group at a strategic position of an organic molecule dramatically alters the properties of the molecule in terms of lipid solubility, oxidative thermal stability thereby enhancing the transport mechanism and bio-efficacy. Similarly, amide derivatives were associated with broad spectrum of biological activities and when amides conjugates with other aliphatic, aromatic and heterocyclic ring produces various type of biological activity.…”

“…Based on the importance of pyrimidine derivatives, encouraged us to synthesize some new highly functionalized substituted pyrido[1,2-a] pyrimidine-3-carboxamide derivatives. In continuation to our efforts, [28][29][30] we designed and synthesized a series of novel trifluoromethyl substituted pyrido[1,2-a] pyrimidine-3-carboxamide derivatives, screened for anti cancer activity against four human cancer cell lines and promising compounds have been identified.…”