评估一些Isoindole-1、3-Dione衍生物对HeLa，C6和A549癌细胞系的细胞毒性潜能。,Medicinal Chemistry

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评估一些Isoindole-1、3-Dione衍生物对HeLa，C6和A549癌细胞系的细胞毒性潜能。
Medicinal Chemistry ( IF 1.9 ) Pub Date : 2020-01-01 , DOI: 10.2174/1573406415666181206115638
Ayse Tan ₁ , Ayse Sahin Yaglioglu ₂ , Nurhan Horasan Kishali ₃ , Ertan Sahin ₃ , Yunus Kara ₃

Affiliation

背景降冰片嘧啶被称为降冰片烷衍生物，并且含有异吲哚骨架结构。异吲哚衍生物对包括癌症在内的炎性病理有积极作用。目的考虑到该信息，首先，由2-烷基/芳基-3a，4,7,7a-四氢-1H-异吲哚-1、3（2H）-二酮合成了含有不同官能团4-13的异吲哚衍生物。方法对于所有化合物的合成，以2-烷基/芳基-3a，4,7,7a-四氢-1H-异吲哚-1,3（2H）-二酮为起始化合物。合成基于两个主要反应：单线态氧的烯反应和环氧化。其次，通过BrdU测定法评估了它们对HeLa，C6和A549癌细胞系的抗癌活性。结果研究了四种浓度（100、50、25和5μM）合成的化合物（4-13）和5-FU（5-氟尿嘧啶）对HeLa，C6和A549细胞的抗癌活性。计算了所有癌细胞系的化合物4-13的IC50值。所研究的化合物根据剂量显示出对癌细胞系的抗癌活性。含有叠氮化物和甲硅烷基醚的化合物7对A549癌细胞系的抑制活性高于其他化合物和5-FU（IC50 = 19.41±0.01μM）。确定化合物9和11表现出对HeLa癌细胞系的细胞选择性活性。在100μM浓度下，化合物11对C6癌细胞系的活性高于阳性对照。结论根据观察到的结果，异吲哚衍生物7、9 由于它们具有抗增殖特性，并且对健康细胞的细胞毒性作用较小，因此11和11可能是治疗宫颈癌和神经胶质瘤癌的潜在抗癌剂。此外，化合物7可用于所有三种癌细胞系（C6，HeLa和A549）的体内研究。

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Evaluation of Cytotoxic Potentials of Some Isoindole-1, 3-Dione Derivatives on HeLa, C6 and A549 Cancer Cell Lines.

BACKGROUND Norcantharimides are known as norcantharidine derivatives and contain an isoindole skeleton structure. Isoindole derivatives have positive effect on inflammatory pathologies including cancers. OBJECTIVE Considering this information, firstly, isoindole derivatives containing different functional groups 4-13 have been synthesized from 2-alkyl/aryl-3a, 4,7,7a-tetrahydro-1H-isoindole-1, 3(2H)-dione. METHODS For the synthesis of all compounds, 2-alkyl/aryl-3a, 4,7,7a-tetrahydro-1H-isoindole- 1,3(2H)-dione was used as the starting compound. The syntheses were based on two main reactions: Ene-reaction of singlet oxygen and epoxidation. Secondly, their anticancer activities were evaluated against HeLa, C6 and A549 cancer cell lines by the BrdU assay. RESULTS Anticancer activities of synthesized compounds (4-13) and 5-FU (5-Florouracil) against HeLa, C6 and A549 cells were investigated at four concentrations (100, 50, 25 and 5 μM). IC50 values of compounds 4-13 were calculated for all cancer cell lines. The investigated compounds showed anticancer activity against the cancer cell lines depending on doses. Compound 7 containing azide and silyl ether exhibited higher inhibitory activity than the other compounds and 5-FU against A549 cancer cell lines (IC50 =19.41± 0.01 μM). Compounds 9 and 11 were determined to exhibit cell-selective activity against HeLa cancer cell lines. Compound 11 had higher activity than the positive control at 100 μM concentrations against C6 cancer cell lines. CONCLUSION According to the results observed, isoindole derivatives 7, 9, and 11 might be good potential anticancer agents for the treatment of cervical and glioma cancer due to their antiproliferative properties, having less cytotoxic effects on healthy cells. In addition, compound 7 could be used in in vivo studies of all three-cancer cell lines (C6, HeLa, and A549).

更新日期：2019-11-01

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