358721-70-7Relevant academic research and scientific papers
Synthesis of novel 4,5-dihydropyrrolo[1,2-a]quinoxalines, pyrrolo[1,2-a]quinoxalin]-2-ones and their antituberculosis and anticancer activity
Makane, Vitthal B.,Vamshi Krishna, Eruva,Karale, Uattam B.,Babar, Dattatraya A.,Kalari, Saradhi,Rekha, Estharla M.,Shukla, Manjulika,Kaul, Grace,Sriram, Dharmarajan,Chopra, Sidharth,Misra, Sunil,Rode, Haridas B.
, (2020/08/17)
A facile strategy was developed for the synthesis of biologically important 4,5-dihydropyrrolo[1,2-a]quinoxalines and pyrrolo[1,2-a]quinoxalin]-2-ones by treating 2-(1H-pyrrol-1-yl)anilines with imidazo[1,2-a]pyridine-3-carbaldehyde or isatin, using amidosulfonic acid (NH3SO3) as a solid catalyst in water at room temperature. The protocol has been extended to electrophile ninhydrin. The catalyst could be recycled for six times without the loss of activity. The compounds were evaluated for their antituberculosis, antibacterial, and anticancer activities. It is worth noting that compounds 3d and 3e demonstrated a minimum inhibitory concentration value of 6.25 μM against Mycobacterium tuberculosis H37Rv, whereas compounds 3d, 3g, 5d, 5e, and 5i showed a remarkable inhibition of A549, DU145, HeLa, HepG2, MCF-7, and B16-F10 cell lines, respectively. Staphylococcus aureus was inhibited by compounds 5b, 5e, 5d, 5g, and 5l at 32 μg/ml.
Structural Basis of Sirtuin 6 Activation by Synthetic Small Molecules
You, Weijie,Rotili, Dante,Li, Tie-Mei,Kambach, Christian,Meleshin, Marat,Schutkowski, Mike,Chua, Katrin F.,Mai, Antonello,Steegborn, Clemens
supporting information, p. 1007 - 1011 (2017/01/18)
Sirtuins are protein deacylases regulating metabolism and stress responses, and are implicated in aging-related diseases. Small molecule activators for the human sirtuins Sirt1-7 are sought as chemical tools and potential therapeutics, such as for cancer.
Development of Small Molecules that Specifically Inhibit the D-loop Activity of RAD51
Lv, Wei,Budke, Brian,Pawlowski, Michal,Connell, Philip P.,Kozikowski, Alan P.
, p. 4511 - 4525 (2016/06/13)
RAD51 is the central protein in homologous recombination (HR) DNA repair and represents a therapeutic target in oncology. Herein we report a novel class of RAD51 inhibitors that were identified by high throughput screening. In contrast to many previously
A versatile synthesis of 4,5-dihydropyrrolo[1,2-a]quinoxalines
Abonia,Insuasty,Quiroga,Kolshorn,Meier
, p. 671 - 674 (2007/10/03)
The reaction of 1-(2-aminophenyl)pyrrole with aromatic or heteroaromatic aldehydes in ethanol and catalytic amounts of acetic acid leads to 4,5-dihydropyrrolo[1,2-a]quinoxalines in high yields. When aliphatic aldehydes were used under the same conditions, a slow oxidation to the corresponding pyrrolo[1,2-a]quinoxalines can occur; the oxidation can be avoided by preparing in situ the 5-acetyl derivatives of the 4,5-dihydropyrrolo[1,2-a]quinoxalines.
