Synthesis and anticancer activity of novel quinazolinone and benzamide derivatives
Synthesis and anticancer activity of novel quinazolinone and benzamide derivatives
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DOI：
10.1007/s11164-017-3245-4
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发表时间：
2018-04-01
影响因子：
3.3
通讯作者：
Al-Mabrook, Selima Ali Mohamed
中科院分区：
文献类型：
--
作者：
El-Hashash, Maher Abd El-Aziz Mahmoud;Salem, Marwa Sayed;Al-Mabrook, Selima Ali Mohamed
为了开发新的抗肿瘤药物，以6-碘-2-苯基-4H-苯并恶嗪-4-酮为原料，与甲酰胺、乙酸铵、水合肼、盐酸羟胺、取代芳胺、苄胺、硫代碳酰肼等含氮亲核试剂反应，合成了一系列喹唑啉酮和苯甲酰胺衍生物。所有化合物均通过IR、MS和H-1-NMR谱进行了表征。在体外评价了一些合成的化合物对HePG-2和MCF-7细胞系的抗增殖活性。2-（苯甲酰氨基）-N-（4-羟基苯基）-5-碘苯甲酰胺和四嗪并[1，6-c]喹唑啉-3（4 H）-喹唑啉衍生物对两种癌细胞的作用最强，与阿霉素相当。所合成的化合物大多具有良好的细胞毒活性。
In trying to develop new anticancer agents, a series of quinazolinone and benzamide derivatives were synthesized via reaction of 6-iodo-2-phenyl-4H-benzoxazin-4-one with nitrogen nucleophiles, namely, formamide, ammonium acetate, hydrazine hydrate, hydroxylamine hydrochloride, substituted aromatic amines, benzyl amine, and/or thiocarbonohydrazide. All compounds were fully characterized by means of IR, MS, and H-1-NMR spectra. Some of the synthesized compounds were evaluated in vitro for their anti-proliferative activity against HePG-2 and MCF-7 cell lines. 2-(Benzoylamino)-N-(4-hydroxyphenyl)-5-iodobenzamide and tetrazino[1,6-c]quinazoline-3(4H)-thione derivative were the most potent against the two cancer cells comparable to that of doxorubicin. Most of the synthesized compounds also exhibited good cytotoxic activity.