Oxindole

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

羟吲哚是一种芳香族杂环结构单元。 2-二氢吲哚酮衍生物已成为激酶抑制剂研究中的先导化合物。 羟吲哚结构已用于受体酪氨酸激酶（RTK）抑制剂，如SU4984和intedanib，RTK家族代表了抗癌药物开发的重要治疗靶点。

Oxindole is an aromatic heterocyclic building block.?2-indolinone derivatives have become lead compounds in the research of kinase inhibitors.Oxindole structure has been used in receptor tyrosine kinases (RTKs) inhibitors such as SU4984 and intedanib, the RTK family represents an important therapeutic target for anti-cancer drug development.We synthesized a series of novel 5-24 derivatives of Oxindole. METHODS AND RESULTS: 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 μM) and 11 (IC50 = 19.20 ± 0.50 μM) showed potent activity as compared to the standard drug thiourea (IC50 = 21.00 ± 0.01 μM). Other compounds showed moderate to weak activity.

Oxindole (Indolin-2-one) is a bicyclic structure consisting of a benzene ring fused to 2-pyrrolidone. Substituted indolinones can be referred as ‘privileged structures’ owing to their excellent binding affinity for many receptors and to the number of approved drugs containing this scaffold. Oxindole has been found in tissues and fluids of mammals as well as natural products produced by a range of plants, bacteria and invertebrates. 2-indolinone derivatives possess diverse range of pharmacological activities including anti-cancer, anti-HIV, anti-diabetic, antibacterial, antioxidant, kinase inhibitory, AChE inhibitory, anti-leishmanial, b3 adrenergic receptor agonistic, phosphatase inhibitory, analgesic, spermicidal, vasopressin antagonists, progesterone antagonists, neuroprotection, NMDA blocker and sleep inducing activities.

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Indolin-2-one

Others

Other Targets

Others

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59-48-3

133.2

C8H7NO

>98% (HPLC)

DMSO:97 mg/mL (728.23 mM; Need ultrasonic)

O=C1Cc2ccccc2N1

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(-20℃)

With Ice Pack

≥ 2 years