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J Med Chem. 2022 Mar 10;65(5):3894-3912. doi: 10.1021/acs.jmedchem.1c01730. Epub 2022 Jan 26.
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PROTAC targeted protein degraders: the past is prologue.PROTAC 靶向蛋白降解剂：过去是序幕。
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Discovering new biology with drug-resistance alleles.发现具有耐药性等位基因的新生物学。
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ERα is an RNA-binding protein sustaining tumor cell survival and drug resistance.雌激素受体α是一种 RNA 结合蛋白，能维持肿瘤细胞的存活和耐药性。
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Mitochondrial estrogen receptors alter mitochondrial priming and response to endocrine therapy in breast cancer cells.线粒体雌激素受体改变乳腺癌细胞中的线粒体启动及对内分泌治疗的反应。
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A small-molecule activator of the unfolded protein response eradicates human breast tumors in mice.小分子未折叠蛋白反应激活剂可消除小鼠体内的人乳腺癌肿瘤。
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3-(4-羟基苯基)吲哚啉-2-酮作为具有强效和选择性抗癌活性支架的演变。

Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity.

作者信息

Boudreau Matthew W, Hergenrother Paul J

机构信息

Dept. of Chemistry, Carl R. Woese Institute for Genomic Biology, Cancer Center at Illinois, University of Illinois at Urbana-Champaign Urbana IL 61801 USA

出版信息

RSC Med Chem. 2022 May 9;13(6):711-725. doi: 10.1039/d2md00110a. eCollection 2022 Jun 22.

DOI:10.1039/d2md00110a
PMID:35814932
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9215341/
Abstract

Development of targeted anticancer modalities has prompted a new era in cancer treatment that is notably different from the age of radical surgery and highly toxic chemotherapy. Behind each effective compound is a rich and complex history from first identification of chemical matter, detailed optimization, and mechanistic investigations, ultimately leading to exciting molecules for drug development. Herein we review the history and on-going journey of one such anticancer scaffold, the 3-(4-hydroxyphenyl)indoline-2-ones. With humble beginnings in 19th century Bavaria, we review this scaffold's synthetic history and anticancer optimization, including its recent demonstration of tumor eradication of drug-resistant, estrogen receptor-positive breast cancer. Compounds containing the 3-(4-hydroxyphenyl)indoline-2-one pharmacophore are emerging as intriguing candidates for the treatment of cancer.

摘要

靶向抗癌药物的发展开启了癌症治疗的新时代，这与根治性手术和高毒性化疗时代显著不同。每一种有效化合物的背后都有着丰富而复杂的历史，从化学物质的首次发现、详细的优化到机理研究，最终产生了令人兴奋的药物开发分子。在此，我们回顾一种抗癌骨架——3-(4-羟基苯基)吲哚啉-2-酮的历史及发展历程。它起源于19世纪的巴伐利亚，我们将回顾这种骨架的合成历史和抗癌优化过程，包括其最近在根除耐药性、雌激素受体阳性乳腺癌方面的表现。含有3-(4-羟基苯基)吲哚啉-2-酮药效团的化合物正成为治疗癌症的有趣候选药物。