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Synthesis and Antitumor Activity Evaluation of Some N-Heterocycles Derived From Pyrazolyl-Substituted 2(3<i>H</i>)-furanone

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Taylor & Francis Group2016-06-02 更新2026-04-16 收录
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Pyrazolyl-substituted 2(3<i>H</i>)-furanone was allowed to react with different nitrogen nucleophiles such as hydrazine hydrate, ethylenediamine, ethanolamine and anthranilic acid to give pyrrolone and benzoxazinone derivatives. The acid hydrazide <b>3</b> was reacted with some carbonyl compounds such as 4-chlorobenzaldehyde, chloroacetyl chloride and acetic anhydride to give thiazolidinone, oxadiazole, pyridazinone derivatives. Selected examples of the synthesized compounds were evaluated as anticancer agents against three types of carcinoma cell lines (HePG 2, HCT116 and PC3), using <i>Doxorubicin</i> as a reference drug. The result revealed that some of the new compounds showed high activities. Compound <b>6a</b> was more potent than the standard drug. Docking study using MOE 2008.10 program was performed.

提供机构:
Magdy I. El-Zahar
创建时间:
2016-06-02
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