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理性设计的 TNF-α 抑制剂:有前途的细胞毒性剂的鉴定。

Rationally designed TNF-α inhibitors: Identification of promising cytotoxic agents.

机构信息

Department of Chemistry, Centre for Advanced Studies, Guru Nanak Dev University, Amritsar 143005, India.

Department of Biotechnology, Guru Nanak Dev University, Amritsar 143005, India.

出版信息

Bioorg Med Chem Lett. 2021 Jun 1;41:127982. doi: 10.1016/j.bmcl.2021.127982. Epub 2021 Mar 23.

DOI:10.1016/j.bmcl.2021.127982
PMID:33766762
Abstract

Design and synthesis of new indole derivatives as tumor growth inhibiting agents via inhibiting the TNF-α is described. The preliminary results showed the inhibition of LPS induced production of NO, TNF-α and IL-6 by these compounds out of which compounds 2d and 2g exhibited appreciable cytotoxicity against the 60 cell lines panel of human cancer. The rationale behind the design of the molecules and the results of their biological studies are presented. 2009 Elsevier Ltd. All rights reserved.

摘要

本文描述了通过抑制 TNF-α 来设计和合成新型吲哚衍生物作为肿瘤生长抑制剂。初步结果表明,这些化合物抑制 LPS 诱导的 NO、TNF-α 和 IL-6 的产生,其中化合物 2d 和 2g 对人癌细胞 60 细胞系面板表现出明显的细胞毒性。介绍了分子设计的原理和生物研究结果。 2009 年爱思唯尔有限公司版权所有。

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