Synthesis, Anticancer and Antioxidant Activity of Novel 2,4-Disubstituted Thiazoles

Abstract

A new series of carbazole based 2,4-disubstituted thiazole derivatives were synthesized. All the synthesized compounds were tested for their cytotoxicity against three different cancer cell lines A549, MCF-7, and HT29. Some of these compounds showed good cytotoxicity. These compounds were also evaluated for antioxidant activity. Compounds 3a, 3b, 3d-f and 3i showed higher antioxidant activity than standard BHT.

Thiazole: A Versatile Standalone Moiety Contributing to the Development of Various Drugs and Biologically Active Agents

“…The radical scavenging properties of compounds 146a, 146b, and 146c have been demonstrated, possibly due to the presence of an electron-donating substituent on substituted aldehydes [180]. Tran et al (2014) have produced a unique set of disubstituted thiazole derivatives based on carbazoles when 2-((6bromo-9-ethyl-9H carbazol-3-yl)methylene)-hydrazinecarbothioamide was synthesized by the condensation of 6-bromo-9-ethyl-9H-carbazole-3-carbaldehyde with thiosemicarbazide in ethanol in the presence of a catalytic amount of acetic acid in the initial step of synthesis, and the product obtained was subsequently converted into the final products. The anti-oxidant (AO) attributes of these molecules were tested.…”

“…Compound 147 had higher antioxidant properties than the standard BHT. The activity of compound 147 might be due to the presence of the p-tolylthiazole substitute [181]. A broad range of thiazole compounds containing pyrazole and tetrazole were initially produced with the synthesis of compound 4-(4-fluorophenyl)-2-(1H-pyrazol-1-yl) thiazole, and after a series of subsequent reactions, the final products were obtained.…”

Urease inhibitory kinetics, molecular docking, SAR and ADME studies of imine analogues

“…Oxazoles displayed numerous biological activities; for instance, anticancer, 29 antimicrobial, 30,31 anti-mycobacterial, 32,33 antifungal, 31 antioxidant, 34 anti-inflammatory, 35,36 anti-obesity 34 and antidiabetic 37 activities. Thiazoles also display numerous biological activities, for example, anti-inflammatory, 38,39 antimicrobial, 40 anti-hypertensive, [41][42][43] anti-pseudomonal, 44 antiviral, 45 antimalarial, 46 antifungal, 47 anticancer 48 and anti-HIV activities. 49 Thiazoles also exhibit inhibition activities against different enzymes such as p38a mitogen-activated protein kinase, 50 FabH, 51,52 tissuenonspecific and intestinal alkaline phosphatases, 53 VEGFR-2 (KDR) kinase, 54 monoamine oxidase, [55][56][57][58][59][60] acetylcholinesterase 61 and urease.…”

Anticancer activity of some new series of 2-(substituted)amino-1,3-thiazole derivatives

“…The rapid spread of cancer has sparked and intense worldwide search for new structure lead which may be of use in designing novel antitumor drugs. In this context, thiazoles and thiazoles linked to various heterocyclic rings through different linkages have recently attract great attention [3][4][5][6][7][8] . The antitumor activities of the natural antineoplastic antibiotics bleomycin, netropsin and thiazole netropsin have been reported 9 .…”