作为糖皮质激素受体激动剂的肾上腺素类似物

ECSOC 2023 Pub Date : 2023-11-15 DOI:10.3390/ecsoc-27-16152

Eugenia Oleynik, Ekaterina Mikhina, D. Grigoreva, V. Maksimova, Lyubov Grebenkina, A. Matveev, E. Zhidkova, E. Lesovaya, Marianna Yakubovskaya

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引用次数: 0

摘要

:这项研究采用通用方法合成了几种新的异肾上腺素类似物。合成的部分化合物对骨髓性白血病细胞 K562 和淋巴瘤细胞系 Granta-519 具有细胞毒性。研究人员利用糖皮质激素受体（GR）模型（PDB 标识符 1P93）进行了分子对接，以了解化合物作用的可能潜在机制。模拟结果显示，肾上腺素类似物与地塞米松在 GR 配体结合域的结合具有相似性。合成的类似物表现出与地塞米松相似的细胞毒性特征。

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Synephrine Analogues as Glucocorticoid Receptor Agonists

: This work carried out the synthesis of several new synephrine analogues by universal method. Some of the synthesized compounds showed cytotoxicity on myeloid leukaemia cells K562 and lymphoma cell line Granta-519. Molecular docking using the glucocorticoid receptor (GR) model (PDB identifier 1P93) was performed to understand the possible underlying mechanism of compound action. The simulation showed the similarity of synephrine analogues’ binding to the binding of dexamethasone in the GR ligand-binding domain. The synthesized analogues exhibited cytotoxicity profiles similar to those of dexamethasone.

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ECSOC 2023

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