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A facile heterogeneous catalytic approach for one-pot synthesis of fused benzoxazinones using Cuβ zeolite and Evaluation of biological activities
Tetrahedron ( IF 2.1 ) Pub Date : 2024-03-02 , DOI: 10.1016/j.tet.2024.133931
Suchitha Dasu , Krishna Sai Gajula , Vasu Amrutham , Murali Boosa , Ramulamma Madasu , Madhuri Lekkala , Sai Balaji Andugulapati , Narender Nama

A simple heterogeneous catalytic process has been established for the single-step synthesis of fused benzoxazinones, quinazolinones, and thiadazines through Markownikoff's hydroamination followed by intramolecular cyclization using Cuβ zeolite. The probability and limitations of this catalytic approach were explored using various substrates. The efficiency and feasibility of scaling up the current catalytic system were demonstrated through gram-scale experiments. Moreover, the catalyst was reused for up to five cycles with no noticeable decrease in its catalytic effectiveness. Furthermore, the synthesized compounds were subjected to assessment to determine their potential as anticancer agents against human cervical epithelioid carcinoma (HeLa), mouse breast cancer (4T-1), and human lung adenocarcinoma (A-549) cell lines. Cytotoxicity studies revealed that and compounds exhibit anti-cancer activity against breast, cervical and lung cancer cells. Additionally, their antimicrobial activity against bacteria and yeast was also evaluated. The compound exhibited superior antifungal activity against

中文翻译:

Cuβ沸石一锅法合成稠合苯并恶嗪酮的简便多相催化方法及生物活性评价

建立了一种简单的多相催化工艺,通过马氏氢胺化,然后使用 Cuβ 沸石进行分子内环化,一步合成稠合苯并恶嗪酮、喹唑啉酮和噻嗪酮。使用各种底物探索了这种催化方法的可能性和局限性。通过克级实验证明了扩大当前催化系统的效率和可行性。此外,该催化剂可重复使用多达五个循环,其催化效率没有明显下降。此外,对合成的化合物进行了评估,以确定其作为抗人宫颈上皮样癌(HeLa)、小鼠乳腺癌(4T-1)和人肺腺癌(A-549)细胞系的抗癌剂的潜力。细胞毒性研究表明,该化合物对乳腺癌、宫颈癌和肺癌细胞具有抗癌活性。此外,还评估了它们对细菌和酵母的抗菌活性。该化合物表现出优异的抗真菌活性
更新日期:2024-03-02
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