Coumarin–triazole Hybrids and Their Biological Activities

Abstract

Hybridization is emerged as a promising strategy in the discovery of new drugs, especially these with complimentary activities and multiple pharmacological targets that are the potential weapons to prevent the drug resistance. Currently, several hybrids are under different stages of clinical trial, and may be introduced into clinical practice to treat various diseases in the near future. Triazoles including 1,2,3‐triazole and 1,2,4‐triazole as well as coumarins occupy an important position in medicinal chemistry attribute to their various biological activities, and some of them have been used in clinical practice. Obviously, hybridization of these two pharmacophores may lead to novel candidates with broader spectrum, more effective, lower toxicity, and multiple mechanisms of action. This review aims to outline the biological activities of coumarin–triazole hybrids, and discuss their structure–activity relationship to pave the way for the further rational development of this kind of hybrids.

Design, Synthesis, and In Vitro Anticancer Activities of Diethylene Glycol Tethered Isatin‐1,2,3‐triazole‐coumarin Hybrids

“…The general procedure for preparing targets 9a-l. The precursors 5 and 8 were prepared via literature methods [27][28][29][30]. A mixture of isatins 5 (1.0 mmol), 4-methyl-7-(prop-2-ynyloxy)-2H-chromen-2-one 8 (1.0 mmol), and Cu (OAc) 2 (40 mg) in dimethylformamide (20 mL) was stirred for 24 h at room temperature under N 2 atmosphere.…”

Isatin–Coumarin Hybrids Tethered via Diethylene Glycol: Design, Synthesis, and Their In Vitro Antitumor Activities

“…The precursors 4 and 6 were prepared via literature methods . A mixture of isatins 4 (1.0 mmol), coumarin 6 (1.0 mmol), and K 2 CO 3 (3.0 mmol) in DMF (20 mL) was stirred at room temperature overnight.…”

Design, Synthesis, and Evaluation of Tetraethylene Glycol‐Tethered Isatin–1,2,3‐Triazole–Coumarin Hybrids as Novel Anticancer Agents

“…Hybridization of different pharmacophores into a single molecule may provide new candidates with complimentary activities and/or multiple pharmacological targets and/or one part can counterbalance the side effects caused by another part, so hybridization is emerged as an encouraging strategy in the discovery of new drugs with potential therapeutic application . Recently, many isatin–1,2,3‐triazole–coumarin hybrids were found to possess promising anticancer potential and have been widely studied . The structure–activity relationship (SAR) revealed that for these hybrids, the linker between isatin and 1,2,3‐triazole has great influence on the activity .…”

“…Recently, many isatin–1,2,3‐triazole–coumarin hybrids were found to possess promising anticancer potential and have been widely studied . The structure–activity relationship (SAR) revealed that for these hybrids, the linker between isatin and 1,2,3‐triazole has great influence on the activity .…”