New Hybrids Derived from Podophyllic Aldehyde and Diterpenylhydroquinones with Selectivity toward Osteosarcoma Cells,ACS Medicinal Chemistry Letters

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New Hybrids Derived from Podophyllic Aldehyde and Diterpenylhydroquinones with Selectivity toward Osteosarcoma Cells
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-03-08 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00493
Ángela P. Hernández _{1,

2} , Paula Díez _{3,

4} , Pablo A. García ₁ , José M. Miguel del Corral ₁ , Martín Pérez-Andrés ₃ , David Díez ₂ , Arturo San Feliciano ₁ , Manuel Fuentes _{3,

4} , M Ángeles Castro ₁

Affiliation

A new family of molecular hybrids, between cyclolignans related to podophyllic aldehyde and several diterpenylnaphthohydroquinones (DNHQ), was prepared and its biological activity evaluated in several human solid tumor cell lines, which are representative of the most prevalent solid tumors in the Western world. Both cyclolignan and quinone fragments were linked through aliphatic or aromatic spacers. The new hybrid family was evaluated for its cytotoxicity, and it was found that the hybrids were several times more potent against the osteosarcoma cell line MG-63 than against MCF-7 and HT-29 cell lines. The presence of an aromatic ring in the linker gave the most potent and selective agent, improving the cytotoxicity of the parent compounds. Cell cycle studies demonstrated that this hybrid induces a strong and rapid apoptotic effect and arrests cells at the G2/M phase of the cell cycle, in the same way that the parent compound podophyllic aldehyde does.

中文翻译：

鬼臼醛和二萜对苯二酚衍生的新杂种对骨肉瘤细胞的选择性

制备了一个新的分子杂种家族，介于与鬼臼醛有关的环木脂素和几种二萜烯萘氢醌（DNHQ）之间，并在几种人类实体瘤细胞系中评估了其生物学活性，这些细胞系代表了西方世界上最普遍的实体瘤。环木脂体和醌片段都通过脂族或芳族间隔基连接。评价了新的杂种家族的细胞毒性，发现杂种对骨肉瘤细胞MG-63的效力是对MCF-7和HT-29细胞系的几倍。接头中芳环的存在提供了最有效和最有效的试剂，从而改善了母体化合物的细胞毒性。

更新日期：2018-03-08

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