Oxindole

The herbs of Isatis indigotica

Synthesis and biological evaluation of novel oxindole-based RTK inhibitors as anti-cancer agents.[Pubmed:25456085]

Bioorg Med Chem. 2014 Dec 15;22(24):6953-60.

Given that receptor tyrosine kinases (RTKs) have emerged as key regulators of all aspects of cancer development, including proliferation, invasion, angiogenesis and metastasis, the RTK family represents an important therapeutic target for anti-cancer drug development. Oxindole structure has been used in RTK inhibitors such as SU4984 and intedanib. In this study, two series of new heterocyclic compounds containing Oxindole scaffold have been designed and synthesized, and their inhibitory activity against the proliferation of nine cancer cell lines has been evaluated. Among them, compounds 9a and 9b displayed the strongest anti-proliferative activity with the IC50s below 10muM. Flow cytometric analysis showed that the compounds 9a and 9b dose-dependently arrested the cell cycle at G0/G1 phase. Although the leading compounds SU4984 and intedanib targets FGFR1, the kinase activity test revealed that these compounds only showed slight inhibitory activity on FGFR1 kinase. Further enzymatic test aided by molecular docking simulation in the ATP-binding site demonstrated that 9a and 9b are potent inhibitors of c-Kit kinase. These compounds are worthy of further evaluation as anticancer agents.

Synthesis of novel derivatives of oxindole, their urease inhibition and molecular docking studies.[Pubmed:26077497]

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3285-9.

We synthesized a series of novel 5-24 derivatives of Oxindole. The synthesis started from 5-chloroOxindole, which was condensed with methyl 4-carboxybezoate and result in the formation of benzolyester derivatives of Oxindole which was then treated with hydrazine hydrate. The Oxindole benzoylhydrazide was treated with aryl acetophenones and aldehydes to get target compounds 5-24. The synthesized compounds were evaluated for urease inhibition; the compound 5 (IC50 = 13.00 +/- 0.35 muM) and 11 (IC50 = 19.20 +/- 0.50 muM) showed potent activity as compared to the standard drug thiourea (IC50 = 21.00 +/- 0.01 muM). Other compounds showed moderate to weak activity. All synthetic compounds were characterized by different spectroscopic techniques including (1)H NMR, (13)C NMR, IR and EI MS. The molecular interactions of the active compounds within the binding site of urease enzyme were studied through molecular docking simulations.

Oxindole (Indolin-2-one) is an aromatic heterocyclic building block. 2-indolinone derivatives have become lead compounds in the research of kinase inhibitors.

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