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首页> 外文期刊>RSC Advances >Synthesis and in vitro anti-proliferative evaluation of naphthalimide–chalcone/pyrazoline conjugates as potential SERMs with computational validation
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Synthesis and in vitro anti-proliferative evaluation of naphthalimide–chalcone/pyrazoline conjugates as potential SERMs with computational validation

机译：萘二烷基酮/吡唑啉缀合物的合成和体外抗增殖评价为具有计算验证的潜在SERMS

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A series of naphthalimide-chalcone/pyrazoline conjugates was prepared and evaluated for their anti-breast cancer potential against estrogen responsive, i.e. MCF-7 (ER+), and triple-negative, i.e. MDA-MB-231 (ER?), cell lines. The structure-activity-relationship (SAR) was deduced based on the influence of linker length, substituents on the phenyl ring and the generated functionalities, on anti-proliferative activities. Docking simulations further delineate the type of interactions of the designed molecules with the selected targets. This report discloses the scope of triazole tethered naphthalimide-chalcone/pyrazoline conjugates as anti breast cancer agents.
机译：制备一系列萘硫胺/吡唑啉缀合物，并评估其对雌激素响应性的抗乳腺癌潜力，即MCF-7（ER +）和三阴性，即MDA-MB-231（ER？），细胞系。基于接头长度，苯环对苯环和产生的函数的影响，推导出结构 - 活性关系（SAR）对抗增殖活性的影响。对接模拟进一步描绘了设计分子与所选靶标的类型的类型。本报告公开了三唑型萘二甲基氨基酮/吡唑啉缀合物作为抗乳腺癌剂的范围。

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