新型PARP1抑制剂的制备及其在癌症治疗中的应用

IF 4 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2025-07-23 DOI:10.1021/acsmedchemlett.5c00411

Xin Zhou, and , Steven H. Liang*,

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引用次数: 0

摘要

聚（adp -核糖）聚合酶1 （PARP1）是研究最广泛的PARP酶，在DNA损伤修复中起重要作用。PARP1抑制已成为一种经过临床验证的策略，可选择性靶向两种癌症亚型：同源重组缺陷（HRD）肿瘤和eb病毒相关恶性肿瘤。本专利重点介绍了PARP1抑制剂的合成和药物组成及其在癌症治疗中的应用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Preparation of Novel PARP1 Inhibitors and Their Use in Cancer Treatment

Poly(ADP-ribose) polymerase 1 (PARP1) is the most widely studied PARP enzyme, which plays a significant role in DNA damage repair. PARP1 inhibition has emerged as a clinically validated strategy to selectively target two cancer subtypes: tumors with homologous recombination deficiency (HRD) and Epstein–Barr virus (EBV)-associated malignancies. This patent highlights the synthesis and pharmaceutical compositions of PARP1 inhibitors and their uses in the treatment of cancer.

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来源期刊

ACS Medicinal Chemistry Letters CHEMISTRY, MEDICINAL-

CiteScore

7.30

自引率

2.40%

发文量

328

审稿时长

1 months

期刊介绍： ACS Medicinal Chemistry Letters is interested in receiving manuscripts that discuss various aspects of medicinal chemistry. The journal will publish studies that pertain to a broad range of subject matter, including compound design and optimization, biological evaluation, drug delivery, imaging agents, and pharmacology of both small and large bioactive molecules. Specific areas include but are not limited to: Identification, synthesis, and optimization of lead biologically active molecules and drugs (small molecules and biologics) Biological characterization of new molecular entities in the context of drug discovery Computational, cheminformatics, and structural studies for the identification or SAR analysis of bioactive molecules, ligands and their targets, etc. Novel and improved methodologies, including radiation biochemistry, with broad application to medicinal chemistry Discovery technologies for biologically active molecules from both synthetic and natural (plant and other) sources Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response Pharmacogenetic and pharmacogenomic studies used to enhance drug design and the translation of medicinal chemistry into the clinic Mechanistic drug metabolism and regulation of metabolic enzyme gene expression Chemistry patents relevant to the medicinal chemistry field.