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Synthesis and antitumor activities of novel bis‐quinazolin‐4(3H)‐ones
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-01-06 , DOI: 10.1002/jhet.3749 Nasrin Rahmannejadi 1 , Issa Yavari 2 , Soghra Khabnadideh 3
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-01-06 , DOI: 10.1002/jhet.3749 Nasrin Rahmannejadi 1 , Issa Yavari 2 , Soghra Khabnadideh 3
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With the aim of obtaining new antitumor agents, a series of bis‐quinazolin‐4(3H)‐ones (3a‐3 f) were designed and synthesized. These products contain 4‐oxo‐1,2,3,4‐tetrahydro‐quinazoline and 3H‐quinazolin‐4‐one moieties linked together via a propyl chain. Cytotoxic activities of 3a‐3 f were evaluated against lung adenocarcinoma (A549), breast carcinoma (MCF‐7) and ovarian cancer (SKOV3) cell lines using MTT method. Cisplatin was used as a positive control. Among the tested compounds 3a, 3b, and 3e showed the best cytotoxic activities against all cancerous cell lines with IC50 values even less than cisplatin. Compounds 3d and 3f also showed desirable cytotoxic activities especially against A549 and MCF‐7.
中文翻译：
新型双喹唑啉-4（3H）-酮的合成及抗肿瘤活性
为了获得新的抗肿瘤药，设计并合成了一系列的双喹唑啉-4（3 H）-酮（3a- 3f ）。这些产品包含通过丙基链连接在一起的4-氧-1,2,3,4-四氢喹唑啉和3 H-喹唑啉-4-酮部分。使用MTT方法评估了3a- 3f对肺腺癌（A549），乳腺癌（MCF-7）和卵巢癌（SKOV3）细胞系的细胞毒活性。顺铂用作阳性对照。在测试的化合物3a，3b和3e中，对所有癌细胞的IC 50表现出最佳的细胞毒性活性值甚至小于顺铂。化合物3d和3f也显示出理想的细胞毒性活性，尤其是对A549和MCF-7的毒性。
更新日期：2020-01-07
中文翻译：
新型双喹唑啉-4（3H）-酮的合成及抗肿瘤活性
为了获得新的抗肿瘤药，设计并合成了一系列的双喹唑啉-4（3 H）-酮（3a- 3f ）。这些产品包含通过丙基链连接在一起的4-氧-1,2,3,4-四氢喹唑啉和3 H-喹唑啉-4-酮部分。使用MTT方法评估了3a- 3f对肺腺癌（A549），乳腺癌（MCF-7）和卵巢癌（SKOV3）细胞系的细胞毒活性。顺铂用作阳性对照。在测试的化合物3a，3b和3e中，对所有癌细胞的IC 50表现出最佳的细胞毒性活性值甚至小于顺铂。化合物3d和3f也显示出理想的细胞毒性活性，尤其是对A549和MCF-7的毒性。
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