Structure activity relationship studies of imidazo[1,2-a]pyrazine derivatives against cancer cell lines

The effects of some imidazopyrazine derivatives on telomerase inhibition, mtdna damage and mtdna copy number

“…The effect of an Imidazo(1,2-a)pyrazine derivative changes according to side groups (R groups) connected to this molecule. 30 There are many studies which draw attention to anticancer activities of Imidazo(1,2-a)pyrazine derivatives. In their study which was published in 2012, Leng et al analyzed structure-activity relation with QSAR method and suggested that some of imidazopyrazine derivatives can function as Aurora A kinase inhibitors 31 Mitchell and his team stated that imidazo(1,2-a)pyrazine diaryl urea compounds can function as receptor tyrosine kinase inhibitors.…”

Crystal structure of 3-(pyrazin-2-ylamino)-2-benzofuran-1(3H)-one, C12H9N3O2

“…Benzofuranones are an important class of synthetic and naturally occurring products exhibiting diverse biological and pharmacological properties [3].P yrazines form an important class of analogues, which occupy aspecial role in natural and synthetic compounds [4]. Pyrazine derivatives are well knownfor their anticancer, antinociceptive, antimycobacterial,antiinflammatory activities [5][6][7][8].Inthis work we coupled benzofuranone withp yrazine ligands to produce the title compound3 -(pyrazin-2-ylamino)-2-benzofuran-1(3H)-one in good yield. In themolecule of the title compound, C 12 H 9 N 3 O 2 ,the essentiallyplanarphthalide groupisorientedatadihedralangle of 89.47°with respecttothe substituted aromatic ring.…”

Quantitative structure activity relationships of cytotoxicity effect on various cancer cells of some imidazo[1,2-?]pyrazine derivatives

“…The percentage of cytotoxicity, IC50 (Inhibition Concentration), of two human breast cells, MDA-MB-231 (estrogen receptor-negative) and MCF-7 (estrogen receptor-positive), a human neuroblastoma cell line, SK-N-SH, and a human hepatocellular liver carcinoma cells, Hep G2 and synthesis procedure of studied molecules were reported before in literature (Myadaraboina et al 2010). The logIC50 -1 values of investigated derivatives is listed in Table 1.…”

“…Typical QSAR study needs to find a set of molecular descriptors with the higher impact on modeling (Gupta et al 1999;Consonni et al 2002;Horvarth et al 2003;Putta et al 2003). Cytotoxicity effects of the investigated molecules were performed earlier for different cancer lines (Myadaraboina et al 2010). In the present work, our main subject is to assess QSAR models' reliability for cytotoxicity levels (logIC50 -1 ) of some imidazo[1,2-]pyrazine derivatives.…”

“…According to literature, investigations on some imidazo [1,2-α]pyrazine derivatives indicate that these molecules have properties such as anti-bacterial (Rival et al 1992), anti-inflammatory (Abignente et al 1981), uterine relaxing activity (Vitse et al 1997a), antibronchospastic (Sablayrolles et al 1984), anti-ulcer (Bonnet et al 1992), anti-depressant (Lumma et al 1983), hypoglycemic activity (Meurer et al 1992), controlling allergic reactions (Brown et al 2006), useful biological activity on the cardiovascular system (Sablayrolles et al 1984;Vitse et al 1999b;Spitzer et al 1988;Barraclough et al 1993), particularly anti-cancer activity (Barraclough et al 1993;Contour-Galcera et al 2001;Demirayak et al 2005;Myadaraboina et al 2010) and potent smooth muscle relaxant activity (Michel et al 1995).…”