Synthesis of a novel chloroquinoline, rhodanine encompassed 1,2,3-triazole scaffolds and molecular docking evaluation of their cytotoxicity

Abstract

A novel series of quinoline-linked rhodanine bearing 1,2,3-triazole analogs (10a-l) have been designed and prepared. All the novel hybrids were analyzed and characterized by spectroscopic performances like 1H-NMR, 13C-NMR, and HR-MS analysis. The anticancer efficiency of final molecules was screened for their in vitro activity against the diverse cancer cells lines like HeLa (cervical carcinoma), MCF-7 (human breast), HT-29 (colon cancer), and Caco-2 (human epithelial). Amongst, compound (10c) exhibited more potent anticancer activity than Combretastatin-A4 as a standard drug against MCF7, Caco-2, HeLa, HT-29, and Caco-2 cancer cells with IC50 values of 3.67, 3.93, 4.92, and 6.83 μM, respectively. The overview of an electron-releasing substituent on the aryl ring exhibited potent anticancer activity. It is the first report to reveal the quinoline-linked rhodanine-bearing 1,2,3-triazole scaffolds as potential antitumor agents with inclusive docking analysis. Graphical abstract

Design, Synthesis, and Molecular Docking Studies of Integrated Benzylidenethiazolidine‐2,4‐Dione and Thieno[2,3‐d]pyrimidine‐6‐Carboxylate Derivatives as Potent Antidiabetic agents

“…A mixture of compound 2 (10.0 g, 48.43 mmol) and POCl 3 (85.0 mL) was refluxed for 12 h at 110 °C temperature [40] . The reaction mixture was cooled to room temp and then, the excess POCl 3 was distillated.…”

Design, synthesis, biological evolution and in silico studies of a novel 1,2,3,4‐tetrazole fused with 1,3,4‐thiadiazole‐2‐amine derivatives

“…Our research team has recently focused on investigating a range of environmentally friendly techniques, including ultra-sonication, microwave irradiation, and heterogeneous catalysis [40][41][42][43][44], in order to create novel heterocycles with a variety of biological activities, such as antioxidant, antimicrobial, anticancer, and anti-diabetic agents [45][46][47][48]. Based on these literature reports, Using the literature research mentioned above as a basis, we developed, created, and tested new compounds that combine 1,2,3,4-tetrazole with 2-amino-1,3,4-thiadiazole.…”

A simple, safe, eco‐friendly, and unique synthesis of hexahydro‐quinolines employing Fe3O4‐MWCNT@MnO2 as a reusable catalyst

“…Recently, our research group has focused on exploring a range of environmentally friendly protocols to produce novel heterocycles with a range of biological activities, like antimicrobial, antioxidant, anticancer, and anti‐diabetic agents 55–58 . These methods include heterogeneous catalysis, microwave irradiation, and ultra‐sonication 59–63 .…”