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Some 1,3,5-trisubstituted pyrazoline derivatives targeting breast cancer: Design, synthesis, cytotoxic activity, EGFR inhibition and molecular docking.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-03-21 , DOI: 10.1016/j.bioorg.2020.103780 Riham F George 1 , Manal Kandeel 2 , Dina Y El-Ansary 2 , Ahmed M El Kerdawy 3
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-03-21 , DOI: 10.1016/j.bioorg.2020.103780 Riham F George 1 , Manal Kandeel 2 , Dina Y El-Ansary 2 , Ahmed M El Kerdawy 3
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Different 1,3,5-trisubstituted pyrazoline derivatives 2a-c, 3-c, 4a-f, 6a-c, 7a-f and 8a-d were prepared via condensation reaction of the appropriate chalcone 1a-c or 5a-c with various hydrazine derivatives. All compounds were screened for their cytotoxicity against breast MCF-7 cancer cell line and the normal fibroblasts WI-38. Thirteen compounds 2a, 3a, 3c, 4a-d, 6c, 7d, 7e, 8b, 8d and 8f revealed promising cytotoxicity against MCF-7 compared to the reference standard staurosporine and they were safe to the normal fibroblasts WI-38. In addition, compounds 3c, 6c, 7d, 8b and 8d elicited higher cytotoxicity than erlotinib and exhibited promising EGFR inhibitory activity at submicromolar level comparable to that of erlotinib except for compound 8b that may exert its cytotoxicity via another mechanism besides EGFR inhibition. Molecular docking of 3c, 6c, 7d, 8b and 8d in the active site of EGFR confirmed the obtained results.
中文翻译：
一些针对乳腺癌的1,3,5-三取代吡唑啉衍生物：设计，合成，细胞毒活性，EGFR抑制和分子对接。
通过适当查耳酮1a-c或5a-c与适当查尔酮1a-c或5a-c的缩合反应制备不同的1,3,5-三取代吡唑啉衍生物2a-c，3-c，4a-f，6a-c，7a-f和8a-d。各种肼衍生物。筛选所有化合物对乳腺癌MCF-7癌细胞系和正常成纤维细胞WI-38的细胞毒性。与参考标准星形孢菌素相比，十三种化合物2a，3a，3c，4a-d，6c，7d，7e，8b，8d和8f显示出有希望的针对MCF-7的细胞毒性，并且它们对正常成纤维细胞WI-38是安全的。另外，化合物3c，6c，7d，8b和8d比埃洛替尼引起更高的细胞毒性，并且在亚微摩尔水平上显示出与厄洛替尼相当的有希望的EGFR抑制活性，除了化合物8b可能通过除EGFR抑制外的另一种机制发挥细胞毒性作用。3c的分子对接
更新日期：2020-04-20
中文翻译：
一些针对乳腺癌的1,3,5-三取代吡唑啉衍生物：设计，合成，细胞毒活性，EGFR抑制和分子对接。
通过适当查耳酮1a-c或5a-c与适当查尔酮1a-c或5a-c的缩合反应制备不同的1,3,5-三取代吡唑啉衍生物2a-c，3-c，4a-f，6a-c，7a-f和8a-d。各种肼衍生物。筛选所有化合物对乳腺癌MCF-7癌细胞系和正常成纤维细胞WI-38的细胞毒性。与参考标准星形孢菌素相比，十三种化合物2a，3a，3c，4a-d，6c，7d，7e，8b，8d和8f显示出有希望的针对MCF-7的细胞毒性，并且它们对正常成纤维细胞WI-38是安全的。另外，化合物3c，6c，7d，8b和8d比埃洛替尼引起更高的细胞毒性，并且在亚微摩尔水平上显示出与厄洛替尼相当的有希望的EGFR抑制活性，除了化合物8b可能通过除EGFR抑制外的另一种机制发挥细胞毒性作用。3c的分子对接
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