Heterocycles 26: synthesis, characterisation, and anticancer activity of some thiazolic chalcones

Abstract

Chalcones and their derivatives have been shown to have potent anticancer activity. A series of aldehydes A 1-4 and thiazolic chalcones C 1-20 were synthesized and evaluated for their in vitro cytotoxic activity against three human cancer cell lines. In addition, this work led to the synthesis of 12 new thiazolic chalcones using a base-catalyzed Claisen-Schmidt condensation reaction. Compounds C 10 and C 12 were found to be the most promising biologically active samples with IC 50 values below or around 10 lM on both DU-145 and THP-1 cancer cell lines.

An Overview of Recent Advances in the Applications of Click Chemistry in the Synthesis of Bioconjugates with Anticancer Activities

“…Chalcones are a significant constituent of natural products which indicates a broad range of biological properties such as anti‐inflammatory, anti‐oxidant and anti‐tumor activity …”

Phytochemical Screening and Biological Activity Studies of the Extract from the Bark of <i>Ricinodendron heudoletti</i>, Euphorbiaceae

“…Alkaloids and steroids whose anti micro bacterial activities have been demonstrated were also found in this extract. Earlier studies have associated high accumulation of alcaloids [2], flavonoids [14], cardiac glycoside and saponins [3,17], all linked to promising antibacterial and antioxidant activities in studied medicinal plants. The methanol acetate ethyl system (5 and 10%) fraction of the methanolic extract of R. heudoletti released 5 components coloured in green clear, blue fluorescent violet.…”

“…Studies on traditional medicine has become an important priority of the World health organization since almost 80% of the population in developing economies use medicinal plants as alternative source of treatment of diseases [1,2]. The search for new chemical entities from herbal materials has increase the interest of Cameroonian scientist to exploit the rich cocktail of plant biodiversity for phytochemical screening of potential compounds of pharmaceutical importance and test of activities [3,4]. The current problem of bacterial resistance and nosocomial infection has led to more research on the use of medicinal plant research for potential new drugs in the drug development pipeline.…”

Synthesis of Functionalized 1‐Aryl‐3‐phenylthiazolylpropanoids and Their Potential as Anticancer Agents

“…[14,15] Based on the abovementioned information, our research group previously studied and reported a panel of thiazole containing chalcones with antiproliferative property. [16] In the continuation of the search for new anticancer agents, we hereby report on the preparation of nine 1-aryl-3-phenylthiazolpropanoids among them seven contained chalcone structural shape and two possess flavonoid skeleton. Their cytotoxic effects against 20 cancer cell lines and a normal cell line were also evaluated.…”