Coumarin‐Chalcones Generated from 3‐Acetylcoumarin as a Promising Agent: Synthesis and Pharmacological Properties

Abstract

antituberculosis; enzyme-inhibition; antioxidant; anti-inflammatory etc. After introducing the synthesis of 3-acetylcoumarin, the review proceeds with a comprehensive presentation of the synthesis of coumarin-chalcones under various conditions. Last, the reactions of prepared coumarin-chalcones through different mechanisms and the outcomes achieved through such reactions are discussed. It is envisaged that this review will prompt researchers to expand on the knowledge gained in this field the last twenty years.

Synthesis and discovery of potential tyrosinase inhibitor of new coumarin‐based thiophenyl‐pyrazolylthiazole nuclei: In vitro evaluation, cytotoxicity, kinetic, and computational studies

“…For developing high‐quality therapeutic candidates, we combined three heterocyclic units with a coumarin motif. Coumarin has attracted the attention of scientists due to its diverse biological activities in fields such as medicine, pharmacology, cosmetics, and the food industries (Hosseini Nasab, Azimian, et al, 2022; Nasab et al, 2022). Pyrazoline is another well‐known bioactive unit which has been reported to inhibit epidermal growth factor receptor tyrosine kinase (EGFR‐TK) (Lv et al, 2011), aurora kinase (Shin et al, 2013), COX‐2/B‐Raf (Yu et al, 2014), telomerase (Amin et al, 2015), and tubulin assembling (Qin et al, 2015).…”

4-Methyl-7-((2-((5-methyl-1,3,4-thiadiazol-2-yl)thio)ethyl)thio)-coumarin

“…Its derivatives have found broad applications such as fluorescent probes [1][2][3][4], food additives [5][6][7], in polymer chemistry [8][9][10][11], and so on. Numerous representatives have displayed variable bioactivity profiles [12][13][14][15][16][17][18], including anticancer [19][20][21][22][23][24], anti inflammatory [25][26][27], anti-tuberculosis [28,29], antimicrobial [30], and many others. Several drugs with coumarin skeleton are available on the market, such as immunosuppressant scoparone, anti-inflammatory drug 8-methoxypsoralen, vasodilator carbochromen, anticoagulants warfarin and phenprocoumon, antifungal agent osthole, anti-HIV preparatus calanolide, anticancer drug flavopiridol, antibiotics novobiocin and clorobiocin, and so on; some are shown in Figure 1.…”

Exploring chalcone-sulfonyl piperazine hybrids as anti-diabetes candidates: design, synthesis, biological evaluation, and molecular docking study

“…The melting points were determined in open capillary tubes using an uncorrected MPA 160 apparatus from Fisher Scientific (USA). 1 H NMR signals were recorded at 400 MHz and 13 C NMR at 100 MHz in DMSO-d6 employing Bruker Avance III (Germany). FT-IR spectra were obtained using a Frontier IR spectrophotometer from Perkin Elmer, USA.…”

“…Chalcones are open chain flavonoids and predominantly biosynthesized by plants, but they can also be obtained through numerous synthetic methodologies. Chalcone consists of two aromatic rings that are connected by a threecarbon system, known as an alpha, beta unsaturated carbonyl system [13]. Their simple chemistry, ease of synthesis, and diversity of substituents make them a subject of great fascination among researchers in the 21 st Century.…”