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新型邻苯二甲酰亚胺-1,3-噻唑衍生物的合成、抗癌活性及作用机制。

Synthesis, anticancer activity and mechanism of action of new phthalimido-1,3-thiazole derivatives.

机构信息

Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Pernambuco, 50740-520, Recife, PE, Brazil; Université de Nantes, Cibles et Médicaments des Infections et Du Cancer, IICiMed, EA 1155, F-44000, Nantes, France.

Laboratório de Imunomodulação e Novas Abordagens Terapêuticas, Universidade Federal de Pernambuco (LINAT-UFPE), 50670-901, Recife, PE, Brazil.

出版信息

Chem Biol Interact. 2021 Sep 25;347:109597. doi: 10.1016/j.cbi.2021.109597. Epub 2021 Jul 23.

Abstract

In this work, 22 new compounds were obtained and evaluated for their cytotoxic activity on peripheral blood mononuclear cells (PBMC) and eight different tumor cell lines. All compounds displayed IC values above 100 μM when assayed against PBMCs. The cytotoxic assays in tumor cell lines revealed that sub-series of phthalimido-bis-1,3-thiazoles (5a-f) exhibited the best anti-tumor activity profile, presenting viability values below 59 %. As a result, the IC value was calculated for compounds 5a-f and 4c, and compounds 5b and 5e were selected for further assays due to their best ICs. Considering the results presented by the sub-series 5a-f, the importance of the 1,3-thiazole ring in improving the anti-tumor activity was pointed out. Together, the results highlighted the anti-tumor activity of phthalimido-bis-1,3-thiazole derivatives.

摘要

在这项工作中,获得了 22 种新化合物,并评估了它们对外周血单个核细胞(PBMC)和八种不同肿瘤细胞系的细胞毒性活性。当对 PBMC 进行检测时,所有化合物的 IC 值均高于 100 μM。在肿瘤细胞系中的细胞毒性测定表明,邻苯二甲酰亚胺双-1,3-噻唑(5a-f)亚系列表现出最佳的抗肿瘤活性谱,呈现出低于 59%的存活率。因此,计算了化合物 5a-f 和 4c 的 IC 值,并且由于其最佳 IC 值,选择了化合物 5b 和 5e 进行进一步的测定。考虑到 5a-f 亚系列呈现的结果,指出了 1,3-噻唑环在提高抗肿瘤活性方面的重要性。总之,这些结果突出了邻苯二甲酰亚胺双-1,3-噻唑衍生物的抗肿瘤活性。

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