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Synthesis of some novel 3,5-disubstituted 1,3,4-oxadiazole derivatives and anticancer activity on EAC animal model

机译:一些新型3,5-二取代1,3,4-恶二唑衍生物的合成及其对EAC动物模型的抗癌活性

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A series of novel 3,5-disubstituted 1,3,4-oxadiazole-2-thione derivatives (1e, 2e, 3e, 4e, and 5e) have been synthesized from different substituted aromatic acids. The structure determination of these compounds have been made on the basis of IR, 1H NMR, and Elemental analysis. The effect of all the compounds on tumor growth inhibition was evaluated by studying the parameters—tumor volume, percentage of the tumor cell count (viable and nonviable), hematological values, and the mean survival status of the treated animals on eight groups of Swiss albino mice. Compounds were given at the dose of 50 mg/kg body weight intraperitoneally and all exhibited the significant (P < 0.001) anticancer activity compared to control. 5-Fluorouracil was used as a standard drug (20 mg/kg body weight i.p.) in the study. All the compounds demonstrated a prominent anticancer activity. The study supported the derivatives of oxadiazoles for the development as potent anticancer molecules.
机译:从不同的取代芳香酸合成了一系列新颖的3,5-二取代的1,3,4-恶二唑-2-硫酮衍生物(1e,2e,3e,4e和5e)。这些化合物的结构确定是基于IR, 1 1 H NMR和元素分析。通过研究以下参数来评估所有化合物对肿瘤生长的抑制作用:八组瑞士白化病患者的参数-肿瘤体积,肿瘤细胞计数百分比(存活和不存活),血液学值和平均存活状态老鼠。腹膜内给予剂量为50 mg / kg体重的化合物,与对照相比,所有化合物均显示出显着的(P <0.001)抗癌活性。在研究中,将5-氟尿嘧啶用作标准药物(腹腔注射20 mg / kg体重)。所有化合物均显示出突出的抗癌活性。该研究支持了恶二唑衍生物作为有效的抗癌分子的发展。

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    《Medicinal Chemistry Research》 |2011年第8期|p.1206-1213|共8页
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