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2,3-取代吲哚类化合物对凋亡抵抗性癌细胞的抗增殖活性。

Antiproliferative activity of 2,3-disubstituted indoles toward apoptosis-resistant cancers cells.

机构信息

Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA.

出版信息

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3277-82. doi: 10.1016/j.bmcl.2013.03.110. Epub 2013 Apr 8.

Abstract

Many types of cancer, including glioma, melanoma, NSCLC, among others, are resistant to apoptosis induction and poorly responsive to current therapies with propaptotic agents. We describe a series of 2,3-disubstituted indoles, which display cytostatic rather than cytotoxic effects in cancer cells, and serve as a new chemical scaffold to develop anticancer agents capable of combating apoptosis-resistant cancers associated with dismal prognoses.

摘要

许多类型的癌症,包括神经胶质瘤、黑色素瘤、非小细胞肺癌等,对凋亡诱导具有抗性,并且对当前使用促凋亡剂的治疗反应不佳。我们描述了一系列 2,3-取代的吲哚,它们在癌细胞中表现出细胞生长抑制而非细胞毒性作用,并作为开发能够对抗与预后不良相关的抗凋亡癌症的抗癌药物的新化学支架。

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本文引用的文献

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Why does cytotoxic chemotherapy cure only some cancers?为什么细胞毒性化疗只能治愈某些癌症?
Nat Clin Pract Oncol. 2009 Jan;6(1):43-52. doi: 10.1038/ncponc1260. Epub 2008 Nov 4.

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