新型4,5 -二氢- 1h -吡唑-1-乙酸酯衍生物抗癌药物的药理评价

Shahlaa Zuhair Abdul-Majeed, Monther Faisal Mahdi, Suhad Faisal Hatem Al-Mugdadi
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引用次数: 0

摘要

Shahlaa等人在体外研究了一系列新的4,5 -二氢- 1h -吡唑-1-乙酸酯衍生物(IVa-i)对乳腺癌细胞系(MCF-7)和肺癌细胞系(A549)的抗增殖活性,根据这些化合物的细胞毒性作用,与其他化合物相比,IVa、IVc和IVi化合物对MCF-7细胞系作用72h时的抗增殖作用百分比分别为81.30%、87.4%和54.66%。这些结果表明,作为标准抗肿瘤药物,新化合物IVc对雌激素受体阳性乳腺癌细胞系72h后的抗增殖率高于他莫昔芬,IVa 72h后的抗增殖率为83.31%。化合物IVb对肺癌细胞系(A549)的细胞毒性作用在48和72h时最高,其抗增殖率分别为58.49%和75.04%,但低于标准抗肿瘤药物埃洛替尼对肺癌细胞系的细胞毒性作用(77.10%和82.46%)。三种化合物(IVa, IVc和IVi)对乳腺癌细胞系(MCF-7)具有抗增殖作用,化合物(IVc)的抑制率与授权药物他莫昔芬相当。其中一种化合物(IVb)对肺癌细胞系(A549)具有抗增殖活性,但低于厄洛替尼,我们的对接结果与实验结果吻合较好。
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Pharmacological Evaluation of New 4, 5-dihydro-1H- Pyrazole-1-yl acetate Derivatives as anti-cancer agents
A series of nine novel 4, 5-dihydro-1H- pyrazole-1-yl acetate derivatives (IVa-i) by Shahlaa et al. was investigated in vitro for their antiproliferative activity against two cancer cell lines, breast cancer cell line (MCF-7) and lung cancer cell lines (A549), According to   the cytotoxicity effect of these compounds, IVa, IVc and IVi compounds have antiproliferative effect with percentage (81.30%, 87.4% & 54.66%) respectively at 72h treatment on MCF-7 cell line compared to other compounds, these results indicate that the new compound IVc have the higher antiproliferative percent comparable to tamoxifen as a standard anti-tumour for oestrogen receptor positive breast cancer cell line after 72h followed by IVa after 72h (83.31%). cytotoxicity effect of compound IVb was highest among tested compounds on lung cancer cell line (A549) with antiproliferative percentage (58.49% & 75.04%) at 48 & 72h respectively, but it is less than erlotinib as a standard anti-tumour for lung cancer cell line cytotoxicity effect (77.10% & 82.46%) at these times. three compounds (IVa, IVc & IVi) have antiproliferative effect on breast cancerous cell line (MCF-7) and compound (IVc) have inhibition percentage comparable to that of the authorized medication Tamoxifen. One compound (IVb) had antiproliferative activity, but less than that of erlotinib on lung cancerous cell line (A549) and there is good agreement between our docking results and the experimental results.
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