The synthesis of N‐benzoylindoles as inhibitors of rat erythrocyte glucose‐6‐phosphate dehydrogenase and 6‐phosphogluconate dehydrogenase

Abstract

Glucose-6-phosphate dehydrogenase (G6PD) and 6-phosphogluconate dehydrogenase (6PGD) play an important function in various biochemical processes as they generate reducing power of the cell. Thus, metabolic reprogramming of reduced nicotinamide adenine dinucleotide phosphate (NADPH) homeostasis is reported to be a vital step in cancer progression as well as in combinational therapeutic approaches. In this study, N-benzoylindoles 9a--9d, which form the main framework of many natural indole derivatives such as indomethacin and N-benzoylindoylbarbituric acid, were synthesized through three easy and effective steps as an in vitro inhibitor effect of G6PD and 6PGD. The N-benzoylindoles inhibited the enzymatic activity with IC in the range of 3.391505 μM for G6PD and 2.19-990 μM for 6PGD.

Purification and characterization glutathione S-transferase enzyme from quail (Coturnix, coturnix japonica) heart and investigation the effect of some metal ions on enzyme activity

“…Recent research has been found that various metal ions and organic compounds cause toxicity on enzyme activities purified from different sources [37][38][39][40][41]. The effect of metal ions on the GST enzyme were determined.…”

Methyl benzoate derivatives as inhibitors of pentose phosphate pathway, which promotes cancer progression and drug resistance: An in silico study supported by in vitro results

“…46,47 Many medicines, such as antibiotics, chemotherapeutics, and antidepressants, have been studied to date for their impact on G6PD and 6PGD activity. [48][49][50][51][52][53][54] Bayindir et al 55 synthesized N-benzoylindole derivatives and examined their in vitro effects on rat G6PD and 6PGD activities. They discovered that while some of them did not show any effect, some activated both enzymes.…”

6‐Phosphogluconate dehydrogenase fuels multiple aspects of cancer cells: From cancer initiation to metastasis and chemoresistance

“…N-Benzoylindole, N-(4-Chlorobenzoyl) indole, and 1H-Indol-1il)(tiyofen-2-il)methanon were found to be potent inhibitors of 6PGD (IC50 = 2.75 μM, 2.19 μM, 3.36 μM respectively) (Figure 6). N-Benzoylindole inhibited 6PGD non-competitively while other two were characterized as competitive inhibitors of 6PGD (81). No one has still attempted to explore the cytotoxic activity of these inhibitors against different cell lines which should be investigated.…”