Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives

Abstract

A series of new thiazoline derivatives were synthesized. Structure analyses were accomplished employing 1H-NMR, 13C-NMR, X-ray and MS techniques. The in vitro antitumor activities were assessed against human hepatocellular carcinoma (HepG-2) and colorectal carcinoma (HCT-116) cell lines. The results revealed that the thiazolines 5b and 2c exhibited significant activity against the two cell lines. The in vitro antimicrobial screening showed that the thiazolines 2c, 5b and 5d showed promising inhibition activity against Salmonella sp. Additionally, the inhibition activity of thiazolines 2e and 5b against Escherichia coli was comparable to that of the reference compound gentamycin.

New N-Adducts of Thiadiazole and Thiazoline with Levoglucosenone and Evaluation of Their Significant Cytotoxic (Anti-Cancer) Activity

“…A review of the few available literature data on the anticancer properties of thiazolines suggests that they are potent inhibitors of PIM kinases, a type of serine/threonine kinase abnormally expressed in many cancers [19,20]. Other biological activities of thiadizole and functionalized thiazoline are reported in the literature as well [21][22][23][24][25][26][27][28][29][30][31][32][33][34].…”

Recent advances in the synthesis and utility of thiazoline and its derivatives

“…Mabkhot et al 128 successfully synthesized a series of novel thiazoline compounds. The reaction sequence for the synthesis of thiazolines 221a–e involved treatment of dione 219a/b with 1° amines 220a–c at room temperature in ethanolic media.…”

One-Pot Tandem/Spirocyclization Reaction: Synthesis of Spiro[pyridine-thiazolidine] Ring Derivatives

“…However, very few studies have focused on the synthesis of thiazole spirocyclic derivatives containing thiazole spirocycles. For example, Mahapatra et al and Mabkhot et al reported excellent methods for synthesizing thiazole spirocyclic backbone compounds, which are primarily formed through efficient spirocyclization reactions (Scheme a). Therefore, although constructing structurally novel spirothiazole spirocyclic backbone molecules using environmentally friendly methods is challenging, it holds considerable research value.…”