In vitro study of antioxidant, antigylycation, sugar hydrolysis enzyme inhibitory effect and molecular in silico docking study of angularly condensed diquinothiazines

Novel Tetracyclic Azaphenothiazines with the Quinoline Ring as New Anticancer and Antibacterial Derivatives of Chlorpromazine

“…Phenothiazines containing one or two quinoline moieties instead of benzene rings are quinobenzothiazines and diquinothiazines. Selected compounds from substituted quinobenzothiazines I and II and diquinothiazines III-VIII (Figure 1) show significant anticancer activity against dozens of cancer cells derived from leukemia, melanoma, non-small cell lung, colon, CNS, ovary, prostate, breast, and skin cancers [37,40,41,43,44]. These compounds also show promising antioxidant effects on rat liver microsomal membranes to protect non-enzymatic lipid peroxidation, inhibitory effects on mitogen-induced proliferation of human peripheral blood mononuclear cells, production of tumor necrosis factor-alpha (TNFα) in human whole blood cultures, against butyrylcholinesterase, and free radical scavenging, antiglycation, and alpha-glucosidase and alpha-amylase inhibition [37,40,44].…”

“…Selected compounds from substituted quinobenzothiazines I and II and diquinothiazines III-VIII (Figure 1) show significant anticancer activity against dozens of cancer cells derived from leukemia, melanoma, non-small cell lung, colon, CNS, ovary, prostate, breast, and skin cancers [37,40,41,43,44]. These compounds also show promising antioxidant effects on rat liver microsomal membranes to protect non-enzymatic lipid peroxidation, inhibitory effects on mitogen-induced proliferation of human peripheral blood mononuclear cells, production of tumor necrosis factor-alpha (TNFα) in human whole blood cultures, against butyrylcholinesterase, and free radical scavenging, antiglycation, and alpha-glucosidase and alpha-amylase inhibition [37,40,44]. They exerted a suppressive effect in in vivo models: delayed-type hypersensitivity to ovalbumin and cutaneous reaction to carrageenan, contact sensitivity to oxazolone, and experimental psoriasis in mice, and showed inhibitory effects on the expression of IFNβ and IFNβ-dependent further genes and proteins involved in the pathogenesis of autoimmune diseases [37,40].…”