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Synthesis of Pyridoclax Analogues: Insight into Their Druggability by Investigating Their Physicochemical Properties and Interactions with Membranes.
ChemMedChem ( IF 3.6 ) Pub Date : 2019-11-26 , DOI: 10.1002/cmdc.201900542 Martina De Pascale 1 , Domenico Iacopetta 2 , Marc Since 1 , Sophie Corvaisier 1 , Véronique Vie 3 , Gilles Paboeuf 3 , Didier Hennequin 4 , Serge Perato 1 , Marcella De Giorgi 1 , Maria Stefania Sinicropi 2 , Jana Sopkova-De Oliveira Santos 1 , Anne-Sophie Voisin-Chiret 1 , Aurélie Malzert-Freon 1
ChemMedChem ( IF 3.6 ) Pub Date : 2019-11-26 , DOI: 10.1002/cmdc.201900542 Martina De Pascale 1 , Domenico Iacopetta 2 , Marc Since 1 , Sophie Corvaisier 1 , Véronique Vie 3 , Gilles Paboeuf 3 , Didier Hennequin 4 , Serge Perato 1 , Marcella De Giorgi 1 , Maria Stefania Sinicropi 2 , Jana Sopkova-De Oliveira Santos 1 , Anne-Sophie Voisin-Chiret 1 , Aurélie Malzert-Freon 1
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Pyridoclax is considered a promising anticancer drug, acting as a protein-protein interaction disruptor, with potential applications in the treatment of ovarian, lung, and mesothelioma cancers. Eighteen sensibly selected structural analogues of Pyridoclax were synthesized, and their physicochemical properties were systematically assessed and analyzed. Moreover, considering that drug-membrane interactions play an essential role in understanding the mode of action of a given drug and its eventual toxic effects, membrane models were used to investigate such interactions in bulk (liposomes) and at the air-water interface. The measured experimental data on all original oligopyridines allowed the assessment of relative differences in terms of physicochemical properties, which could be determinant for their druggability, and hence for drug development.
中文翻译：
Pyridoclax类似物的合成：通过研究其理化性质和与膜的相互作用来了解其可药用性。
Pyridoclax被认为是一种有前途的抗癌药物，可作为蛋白质-蛋白质相互作用破坏剂，在卵巢癌，肺癌和间皮瘤癌症的治疗中具有潜在的应用。合成了十八个Pyridoclax的明智选择的结构类似物，并对其物理化学性质进行了系统的评估和分析。此外，考虑到药物-膜相互作用在理解给定药物的作用方式及其最终毒性作用中起着至关重要的作用，因此使用膜模型研究了散装（脂质体）和空气-水界面的相互作用。在所有原始低聚吡啶上测得的实验数据可以评估理化性质方面的相对差异，这可以决定其可药物性，从而决定药物的开发。
更新日期：2019-11-27
中文翻译：
Pyridoclax类似物的合成：通过研究其理化性质和与膜的相互作用来了解其可药用性。
Pyridoclax被认为是一种有前途的抗癌药物，可作为蛋白质-蛋白质相互作用破坏剂，在卵巢癌，肺癌和间皮瘤癌症的治疗中具有潜在的应用。合成了十八个Pyridoclax的明智选择的结构类似物，并对其物理化学性质进行了系统的评估和分析。此外，考虑到药物-膜相互作用在理解给定药物的作用方式及其最终毒性作用中起着至关重要的作用，因此使用膜模型研究了散装（脂质体）和空气-水界面的相互作用。在所有原始低聚吡啶上测得的实验数据可以评估理化性质方面的相对差异，这可以决定其可药物性，从而决定药物的开发。
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