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首页> 外文期刊>Journal of Medicinal Chemistry >Sequential cytotoxicity: A theory evaluated using novel 2-[4-(3-aryl-2-propenoyloxy)phenylmethylene]cyclohexanones and related compounds
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Sequential cytotoxicity: A theory evaluated using novel 2-[4-(3-aryl-2-propenoyloxy)phenylmethylene]cyclohexanones and related compounds

机译：顺序细胞毒性：使用新型2- [4-（3-芳基-2-丙烯酰氧基）苯基亚甲基]环己酮和相关化合物评估的理论

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摘要

Five series of novel compounds were synthesized in order to evaluate the theory of sequential cytotoxicity which seeks to exploit the view that various cancer cells are particularly susceptible to successive attacks by cytotoxic agents. The compounds prepared were various 2-[4-(3-aryl-2-propenoyloxy)phenylmethylene]cyclohexanones 1 and the related Mannich bases 2. In addition the analogues 3-5 lacking an olefinic bond in the ester group were also synthesized, which were predicted to be less cytotoxic than the compounds of series 1 and 2. The atomic charges at the potential sites for interaction with cellular constituents were determined by molecular modeling calculations. The biodata obtained from murine and human neoplastic cells revealed that the predictions made regarding the viability of the theory were fulfilled in approximately two-thirds of the cases indicating that further investigation of this hypothesis is warranted. In addition, the significant potencies of some of the Mannich bases toward human tumor cell lines, in particular coupled to their selective toxicity toward human leukemic and colon cancer cells, confirms their usefulness in serving as lead molecules for further development. A preliminary investigation into the mode of action of representative compounds revealed their ability to induce apoptosis and inhibit the biosyntheses of ribonucleic acid and proteins. [References: 42]
机译：为了评估顺序细胞毒性的理论，合成了五组新化合物，该理论试图利用以下观点：各种癌细胞特别容易受到细胞毒剂的连续攻击。制备的化合物是各种2- [4-（3-（2-芳基-2-丙烯酰氧基）苯基亚甲基]环己酮1和相关的曼尼希碱2。此外，还合成了在酯基团中缺少烯键的类似物3-5，预计它们的毒性要小于系列1和2的化合物。通过分子模型计算确定与细胞成分相互作用的潜在位点的原子电荷。从鼠和人类肿瘤细胞获得的生物数据表明，有关理论可行性的预测在大约三分之二的案例中得到了实现，这表明有必要对该假设进行进一步的研究。另外，一些曼尼希碱对人肿瘤细胞系的显着效力，特别是它们对人白血病和结肠癌细胞的选择性毒性，证实了它们在用作进一步发展的先导分子方面的有用性。对代表性化合物的作用方式的初步研究表明，它们具有诱导细胞凋亡和抑制核糖核酸及蛋白质生物合成的能力。 [参考：42]

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