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首页> 外文期刊>Cellular Physiology and Biochemistry >Anticancer potential of 3-(Arylideneamino)-2-phenylquinazoline-4(3H)-one derivatives
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Anticancer potential of 3-(Arylideneamino)-2-phenylquinazoline-4(3H)-one derivatives

机译：3-（亚芳基氨基）-2-苯基喹唑啉-4（3H）-一衍生物的抗癌潜力

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Different quinazoline derivatives have showed wide spectrum of pharmacological activities. Some 3-(arylideneamino)-phenylquinazoline-4(3H)-ones have been reported to possess antimicrobial activity. The present study has been undertaken to evaluate the anticancer effect of these quinazolinone derivatives. The quinazolinone derivatives were synthesized as reported earlier. Compounds containing NO _2, OH, OCH _3, or OH and OCH _3 as substituent(s) on the arylideneamino group were named as P(3a), P(3b), P(3c), and P(3d) respectively. Out of these, P(3a) and P(3d) showed better cytotoxic activity than P(3b) and P(3c) on a panel of six cancer cell lines of different origin, namely, B16F10, MiaPaCa-2, HCT116, HeLa, MCF7, and HepG2, though the effect was higher in B16F10, HCT116, and MCF7 cells. P(3a) and P(3d) induced death of B16F10 and HCT116 cells was associated with characteristic apoptotic changes like cell shrinkage, nuclear condensation, DNA fragmentation, and annexin V binding. Also, cell cycle arrest at G1 phase, alteration of caspase-3, caspase-9, Bcl-2 and PARP levels, loss of mitochondrial membrane potential, and enhanced level of cytosolic cytochrome c were observed in treated B16F10 cells. Treatment with multiple doses of P(3a) significantly increased the survival rate of B16F10 tumor bearing BALB/c mice by suppressing the volume of tumor while decreasing microvascular density and mitotic index of the tumor cells.
机译：不同的喹唑啉衍生物已显示出广泛的药理活性。据报道一些3-（亚芳基氨基）-苯基喹唑啉-4（3H）-具有抗菌活性。已经进行了本研究以评估这些喹唑啉酮衍生物的抗癌作用。如先前报道，合成了喹唑啉酮衍生物。在亚芳基氨基上含有NO _2，OH，OCH _3或OH和OCH _3作为取代基的化合物分别命名为P（3a），P（3b），P（3c）和P（3d）。其中，P（3a）和P（3d）在一组六种不同来源的癌细胞系B16F10，MiaPaCa-2，HCT116，HeLa上显示出比P（3b）和P（3c）更好的细胞毒活性。 ，MCF7和HepG2，尽管在B16F10，HCT116和MCF7细胞中效果更高。 P（3a）和P（3d）诱导的B16F10和HCT116细胞死亡与细胞凋亡，细胞核收缩，DNA片段化和膜联蛋白V结合等特征性凋亡相关。同样，在处理过的B16F10细胞中，观察到细胞周期停滞在G1期，caspase-3，caspase-9，Bcl-2和PARP水平改变，线粒体膜电位丧失以及胞浆细胞色素c水平升高。通过抑制肿瘤体积，同时降低肿瘤细胞的微血管密度和有丝分裂指数，用多剂量的P（3a）治疗可显着提高B16F10荷瘤BALB / c小鼠的存活率。

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