ChemInform Abstract: Synthesis and Structure—Activity Relationship of 1‐ and 2‐Substituted 1,2,3‐Triazole Letrozole‐Based Analogues as Aromatase Inhibitors.

Abstract

Synthesis and Structure-Activity Relationship of 1-and 2-Substituted 1,2,3-Triazole Letrozole-Based Analogues as Aromatase Inhibitors. -1,2,3-Triazole analogues, e.g. (III) and (V), of letrozole are synthesized by employing the "click" chemistry as the key step. The presence of a para-cyano group and two aryl groups seems to be important for good activity. Compounds (IIIe) and (Ve) could serve as potential lead compounds. -(DOIRON, J.; SOULTAN, A. H.; RICHARD, R.; TOURE, M. M.; PICOT, N.; RICHARD, R.; CUPERLOVIC-CULF, M.; ROBICHAUD, G. A.; TOUAIBIA*, M.; Eur. J. Med. Chem. 46 (2011) 9, 4010-4024, http://dx.

Design, synthesis, anticancer activity, and in silico studies of novel imidazo[1,2‐a]pyridine based 1H‐1,2,3‐triazole derivatives

“…In conclusion, novel imidazo[1,2-a]pyridine based 1,2,3-triazole amide derivatives were designed, synthesized, and confirmed by 1 H NMR, 13 C NMR, 19 F NMR, MS Spectra, and elemental analysis, and evaluated for in vitro anticancer activity against two human cancer cell lines, HeLa and MCF-7. The obtained results clearly revealed that most of the tested compounds such as 9d, 9b, 9c, 9f, and 9j were found to be more effective inhibitors of growth of two cell lines with IC 50 values that are close to that of standard drug.…”

“…[10,11] ] It has been discovered that triazole moieties showed vast range of biological activities through diverse mechanisms like enzymatic action, receptor-mediated mechanism, etc. The 1,2,3-triazole derivatives are well known for various biological activities such as anti-HIV, [12][13][14][15] anticancer, [16][17][18][19] antibacterial activities. [20,21] On the other hand, imidazopyridine showed a wide range of biological activities.…”

“…Inspired by the aforementioned facts, it is planned to design novel imidazopyridine based 1,2,3-triazole derivatives as directed by molecular docking studies against PI3Kα active site. The designed molecules were synthesized, characterized by 1 H NMR, 13 C NMR, 19 F NMR, MS, and elemental analysis, and evaluated for their in vitro anticancer activity.…”

Acetylene and Ethylene: Universal C2 Molecular Units in Cycloaddition Reactions

“…The reaction was performed using dimethyl sulfoxide as a solvent at atmospheric pressure of acetylene. 9a b The best results were observed for the aryl-substituted azides, benzyl azide, and n -nonyl azide. Sterically hindered azides, such as o -substituted phenyl azides and 1-functionalized benzyl azides, gave triazoles 104 in low to moderate yields (Scheme 52 ).…”

“…Sterically hindered azides, such as o -substituted phenyl azides and 1-functionalized benzyl azides, gave triazoles 104 in low to moderate yields (Scheme 52 ). 9a b…”