Evaluation of Antioxidant, Antimicrobial and Anticancer activity of Thiazole Tagged Isatin Hydrazones

Abstract

Isatin and its derivatives is versatile lead molecule for potential bioactive agents and shows wide spectrum of activities. In this study, we evaluated antioxidant, antimicrobial and cytotoxic activity of isatin-3-[N2-(2-benzalaminothiazol-4-yl)] hydrazone derivatives using well defined models. Antioxidant activity of the isatin derivatives (Va-Vj) was evaluated by using the 1, 1-diphenyl-2-picryl hydrazine radicals scavenging assay. The antimicrobial activity is evaluated by cup plate method and anticancer activity is evaluated by MTT assay against HBL-100 & HeLa cell lines. Compound Vh (R = 5-Cl, R1 = OH & R2 = OCH3) showed good antioxidant activity with the IC50 of 8.09 M. In addition Ve and Vi have showned most active antibacterial activity against Bacillus subtilis, Staphylococcus aureus and Escherichia coli with a Zone of Inhibition (mm) 20, 16, 18 and 14, 12, 15 on respective organism at 100 g/disc. The compound Vi have produced a good antifungal activity against Aspergillus niger and Clostridium vericulata with the zone of inhibition values of 9 and 8 mm respectively. These isatin derivatives also among the test compounds, compound Vd (R = 5-Cl, R1 = OH & R2 = OCH3) and compound Vh (R = 5-Cl, R1 = OH & R2 = OCH3) have shown nearly equal cytotoxic activity with IC50 values of 246.53 mM and 247.29 mM against HBL-100 cell lines and HeLa cell lines respectively. From the results, isatin derivatives showed powerful antioxidant activity, antimicrobial and anticancer activity may be due to the halogens substituted at 5th position of isatin. The standard drugs used were ampicillin, clotrimazole, cisplatin and ascorbic acid for antibacterial, antifungal, anticancer and antioxidant respectively.

Assessing the Acute Toxicological Effects of Annona muricata Leaf Ethanol Extract on Rats: Biochemical, Histopathological, and Metabolomics Analyses

“…Moreover, all the rats survived throughout the study. This result was corroborated with the previous studies [ 32 , 33 ] in which no severe signs of toxicity and mortality were identified due to the treatment of A. muricata leaf ethanol extract. Furthermore, the weight recorded every two days manifested no significant difference, but the weight of the rats began increasing towards the end of study.…”

Recent advances in isatin hybrids as potential anticancer agents

“…The isatin–hydrazone/hydrazide hybrids possess considerable anticancer activity and compound 11 (IC 50 : 6.3–10.8 μM, MTT assay) was comparable to doxorubicin (IC 50 : 6.1–7.6 μM) against HepG2, A549, and MCF‐7 cancer cell lines, whereas hybrids 12 (IC 50 : 2.90–7.61 μM, MTT assay) were 4.2–17.6‐fold more potent than 5‐fluorouracil (IC 50 : 32.15 and 51.16 μM) against HepG2 and Jurkat cancer cell lines. [ 48–50 ] Moreover, hybrids 12a,b (IC 50 : >100 μM) were nontoxic towards normal HEK‐293 cells and SI > 13.1. Thus, both of them could act as hit compounds for the development of novel anticancer chemotherapeutic agents.…”

Investigation and comparison of biological effects of regioselectively synthesized thiazole derivatives

“…Numerous thiazole derivatives have been synthesized and introduced as antimicrobial [12][13][14], anticonvulsant [15,16], anticancer [17,18], and antidiabetic agents [19,20]. Synthetic thiazoles with antioxidant capacity [21][22][23] or with two or more biological properties, for example, antioxidant, antimicrobial, and anticancer [24], antitumor, antioxidant, and antimicrobial [25], antibacterial, antifungal, and anti-HIV [26], were available.…”