Biological evaluation of novel 6-Arylbenzimidazo [1,2-c] quinazoline derivatives as inhibitors of LPS-induced TNF- alpha secretion

Abstract

This study describes the effect of novel 6-Arylbenzimidazo[1,2-c]quinazoline derivatives as tumor necrosis factor alpha (TNF-α) production inhibitors. The newly synthesized compounds were tested for their in vitro ability to inhibit the lipolysaccharide (LPS) induced TNF-α secretion in the human promyelocytic cell line HL-60. The compound 6-Phenyl-benzimidazo[1,2-c]quinazoline, coded as G1, resulted as the most potent inhibitor and with no significant cytotoxic activity. Thus, 6-Arylbenzimidazo[1,2-c]quinazoline derivatives may have a potential as anti-inflammatory agents.

Synthesis, characterization, and antimicrobial studies of novel 1,3,4-thiadiazolium-5-thiolates

“…Quinazoline derivatives were found to possess various biological activities like, antitumor (Galarce et al, 2008), anti-inflammatory (Baba et al, 1996), antibacterial (Bedi et al, 2004), anticancer (Gudasi et al, 2009), anti HIV [Desai et al, 1998], antileprotic (DeGraw et al, 1974), antimalarial (Bhattacharjee et al, 2004), anticonvulsant, sedative-hypnotic (Kashaw et al, 2010) activity, and many more. Literature survey reveals that mesoionic compounds are most important class of heterocyclic compounds.…”

Synthesis of N-Fused Benzimidazole-4,7-diones via Sequential Copper-Catalyzed C–N Coupling/Cyclization and Oxidation

“…Mp 227–228 °C (lit. 3 230–231). 1 H NMR (500 MHz, CDCl 3 ): δ 6.60 (d, J = 8.3 Hz, 1H), 7.17–7.20 (m, 2H), 7.45–7.48 (m, 1H), 7.59–7.63 (m, 2H), 7.68–7.71 (m, 3H), 7.77–7.81 (m, 2H), 7.95–8.00 (m, 2H), 8.73 (dd, J = 7.8 and 0.8 Hz, 1H).…”

Crystal structure and Hirshfeld surface analysis of [2-(1H-benzimidazol-2-yl-κN 3)aniline-κN]dichloridozinc(II) N,N-dimethylformamide monosolvate

“…Benzimidazoles as organic ligands have attracted interest with regard to the synthesis of metal-organic frameworks, not only because of their coordination abilities to metal ions, but also their significant potential applications in biological systems (Ahmad & Bharadwaj;2013;Sharma et al, 2016;Gu et al, 2017). Benzimidazole compounds and their metal complexes have been found to show diverse biological activity (Podunavac-Kuzmanovic & Cvetkovic, 2010), including inhibition against enteroviruses (Xue et al, 2011) and potent antitumor activity (Galarce et al, 2008). The bidentate ligand 2-(1Hbenzo [d]imidazol-2-yl) aniline (L) has been used to prepare a series of mononuclear transition-metal complexes with halide anions as the active leaving group in our catalytic research.…”