RETRACTED: Cytotoxicity and Anti-Inflammatory Activity of Methylsulfanyl-Triazoloquinazolines

Abstract

A series of twenty five 2-methylsulfanyl-[1,2,4]triazolo[1,5-a]quinazoline derivatives 1–25 was previously synthesized. We have now investigated their cytotoxic effects against hepatocellular Hep-G2 and colon HCT-116 carcinoma cells and effect on the macrophage growth, in addition to their influence of the inflammatory mediators [nitric oxide (NO), tumor necrosis factor-α (TNF-α), prostaglandin E-2 (PGE-2) and in bacterial lipopolysachharide (LPS)-stimulated macrophages]. The findings revealed that compounds 13 and 17 showed the highest cytotoxicity and that 3, 6–8 and 25 are promising multi-potent anti-inflammatory agents.

Inhibition of lipoxygenase by sesamol corroborates its potential anti-inflammatory activity

“…Microbial infection, chemical irradiation and stress also results in ROS generation [12]. ROS, in excess amount than the enzymatic antioxidants (superoxide dismutase and catalase) in the physiological system, cause imbalance resulting in damaged lipids, proteins and DNA due to increased cellular oxidative stress.…”

Synthesis and biological evaluation of 4-(1H-1,2,4-triazol-1-yl)benzoic acid hybrids as anticancer agents

“…For instance, 3-pyridyl-bis- [1,2,4]triazoloquinazoline and 5-ethoxytriazoloquinazoline have shown the highest cytotoxicity against Hep-G2 and colon HCT-116 carcinoma cells. 15 Furthermore, 5-chloro- [1,2,4] triazoloquinazolines have been found to possess promising anticancer activities against medulloblastoma (Daoy) and melanoma (SK-MEL28) cell lines. [16][17][18] Letrozole and anastrozole containing a 1,2,4-triazole ring have been approved by the FDA and used as rst-line therapies for the treatment of breast cancer in postmenopausal women owing to their apparent superiority to estrogen receptor antagonists, such as tamoxifen.…”

“…6 Based on the above information and our interest in determining the anticancer pharmacological activities of triazole compounds, we incorporated benzoic acid and the triazole pharmacophore into one molecule to generate novel 1,2,4-triazole benzoic acid hybrid scaffolds. Herein, we aim to describe the synthesis of seventeen hybrids (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17) and evaluate their in vitro antiproliferative activity against HCT-116 and MCF-7 human cancer cell lines, and normal human RPE-1 cells.…”

Antihistamine Activity of 1,2,4-Triazolo[1,5-a]quinazolines

“…In addition, a number of synthesized 1,2,4-triazolo-4H-[4,3-a]quinazolin-5-ones have been found to display as good antihistamine agents 7,8 . In view of these points, the present work is an extension of our ongoing efforts in the field of triazolo-quinzolines chemistry [9][10][11][12][13][14][15][16] , towards the development and designing of new compounds. Therefore, we aimed to investigate a new set of synthesized 1,2,4-triazolo-[1,5a]quinazolines as antihistamine agents.…”