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四氢异喹啉衍生物的设计、合成与生物抗肿瘤活性评价。

Design, synthesis, and biological antitumor evaluation of tetrahydroisoquinoline derivatives.

机构信息

State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.

State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.

出版信息

Bioorg Med Chem Lett. 2024 Sep 1;109:129824. doi: 10.1016/j.bmcl.2024.129824. Epub 2024 May 31.

Abstract

Cancer, as a public health issue, is the leading cause of death worldwide. Tetrahydroisoquinoline derivatives have effective biological activities and can be used as potential therapeutic agents for antitumor drugs. In this work, we designed and synthesized a series of novel tetrahydroisoquinoline compounds and evaluated their antitumor activity in vitro on several representative human cancer cell lines. The results showed that the vast majority of compounds showed good inhibitory activities against the cancer cell lines of HCT116, MDA-MB-231, HepG2, and A375.

摘要

癌症作为一个公共卫生问题,是全球范围内的主要死亡原因。四氢异喹啉衍生物具有有效的生物活性,可用作抗肿瘤药物的潜在治疗剂。在这项工作中,我们设计并合成了一系列新型四氢异喹啉化合物,并在体外对几种代表性的人癌细胞系评估了它们的抗肿瘤活性。结果表明,绝大多数化合物对 HCT116、MDA-MB-231、HepG2 和 A375 等癌细胞系均显示出良好的抑制活性。

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