Synthesis and bioactivity studies of 1-aryl-3-(2-hydroxyethylthio)-1-propanones

Abstract

A series of Mannich bases having piperidine moiety were reacted with 2-mercaptoethanol, leading to 1-aryl-3-piperidine-4-yl-1-propanone hydrochlorides. The cytotoxicity and carbonic anhydrase inhibitory activities of these new compounds were evaluated. Among the compounds, only one derivative, nitro substituent bearing EU9, showed an effective cytotoxicity, although weak tumor specificity against human oral malignant versus nonmalignant cells. The compound induced apoptosis in HSC-2 oral squamous cell carcinoma cells, but not in human gingival fibroblast. Chemical modifications of this lead are thus necessary to further investigate it as a drug candidate and to obtain compounds with a better activity profile.

Microwave-assisted synthesis and bioevaluation of new sulfonamides

“…In this study, the compounds having the chemical structure of [4-[5–(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1 H -pyrazol-1-yl]benzenesulfonamide, the compounds 8–14 ] were designed and successfully synthesized by microwave irradiation with some minor modifications 17 , 39 , 40 by starting from the suitable chalcones synthesized according to the literature 16–18 , 28–31 . Reactions were monitored by TLC.…”

Synthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones

“…After 48 h, the medium was replaced with 0.1 ml of fresh medium containing different concentrations of single test compounds. Cells were incubated further for 48 h and the relative viable cell number was then determined by the MTT method 22,[48][49][50][51][52][53][54] . All benzoxazolone derivatives were dissolved with DMSO at the concentration of 40 mM and stored until use.…”