Indolo-quinazoline in Medicinal Chemistry as an Anticancer Agents: Current Trends and Future Opportunities

IF 4.7 2区化学 Q2 CHEMISTRY, PHYSICAL Journal of Molecular Structure Pub Date : 2025-09-05 Epub Date: 2025-04-12 DOI:10.1016/j.molstruc.2025.142351

Bhagyashri Rathod , Sachin Puri , Vikrant Abbot , Kapil Kumar

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Abstract

Cancer is a prevalent disease globally, influenced by various factors such as lifestyle changes and genetic predisposition. Additionally, multidrug resistance (MDR) is a significant cause of chemotherapy failure in cancer treatment. To address these issues and restore normal biological functions, numerous medicinal compounds have been developed. This review focuses on tryptanthrin and its derivatives, particularly those demonstrating anti-proliferative effects. Tryptanthrin features a quinazoline scaffold fused with indole fragments, with carbonyl groups located at the sixth and twelfth positions. It acts through various pathways and enzymes, including JNK signalling, the kynurenine pathway, IDO1, TDO, and IDO2. The review also includes relevant data from studies conducted by researchers, encompassing in vivo and in vitro experiments (such as cell line studies and IC₅₀ values), as well as the structure-activity relationship of these compounds. These insights will aid in the future design and development of potent new molecules against cancer, with tryptanthrin as a core component.

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吲哚-喹唑啉在药物化学中的抗癌作用：现状和前景

癌症是一种全球流行的疾病，受生活方式改变和遗传易感性等多种因素的影响。此外，多药耐药（MDR）是癌症化疗失败的重要原因。为了解决这些问题和恢复正常的生物功能，已经开发了许多药物化合物。本文综述了色氨酸及其衍生物，特别是那些具有抗增殖作用的衍生物。色胺菊酯具有与吲哚片段融合的喹唑啉支架，羰基位于第6和第12位。它通过多种途径和酶起作用，包括JNK信号，犬尿氨酸途径，IDO1， TDO和IDO2。本综述还包括研究人员进行的相关研究数据，包括体内和体外实验（如细胞系研究和IC50值），以及这些化合物的构效关系。这些见解将有助于未来设计和开发以色氨酸为核心成分的有效抗癌新分子。

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来源期刊

Journal of Molecular Structure 化学-物理化学

CiteScore

7.10

自引率

15.80%

发文量

2384

审稿时长

45 days

期刊介绍： The Journal of Molecular Structure is dedicated to the publication of full-length articles and review papers, providing important new structural information on all types of chemical species including: • Stable and unstable molecules in all types of environments (vapour, molecular beam, liquid, solution, liquid crystal, solid state, matrix-isolated, surface-absorbed etc.) • Chemical intermediates • Molecules in excited states • Biological molecules • Polymers. The methods used may include any combination of spectroscopic and non-spectroscopic techniques, for example: • Infrared spectroscopy (mid, far, near) • Raman spectroscopy and non-linear Raman methods (CARS, etc.) • Electronic absorption spectroscopy • Optical rotatory dispersion and circular dichroism • Fluorescence and phosphorescence techniques • Electron spectroscopies (PES, XPS), EXAFS, etc. • Microwave spectroscopy • Electron diffraction • NMR and ESR spectroscopies • Mössbauer spectroscopy • X-ray crystallography • Charge Density Analyses • Computational Studies (supplementing experimental methods) We encourage publications combining theoretical and experimental approaches. The structural insights gained by the studies should be correlated with the properties, activity and/ or reactivity of the molecule under investigation and the relevance of this molecule and its implications should be discussed.