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三嗪支架在抗癌药物研发中的评估:综述。

Evaluation of Triazine Scaffold for Anticancer Drug Development: A Review.

机构信息

Department of Pharmaceutical Chemistry, Delhi Institute of Pharmaceutical Sciences and Research, Mehrauli- Badarpur Road, Sector 3, Pushp Vihar, New Delhi, 110017, India.

Department of Analytical Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, Hradec Králové 500 05, Czech Republic.

出版信息

Curr Drug Discov Technol. 2024;21(2):e170723218813. doi: 10.2174/1570163820666230717161610.

DOI:10.2174/1570163820666230717161610
PMID:37461340
Abstract

INTRODUCTION

The widespread importance of the synthesis and modification of anticancer agents has given rise to many numbers of medicinal chemistry programs. In this regard, triazine derivatives have attracted attention due to their remarkable activity against a wide range of cancer cells. This evaluation covers work reports to define the anticancer activity, the most active synthesized compound for the target, the SAR and, when described, the probable MOA besides similarly considered to deliver complete and target-pointed data for the development of types of anti-tumour medicines of triazine derivatives. Triazine scaffold for the development of anticancer analogues. Triazine can also relate to numerous beneficial targets, and their analogues have auspicious and anti-tumour activity. Fused molecules can improve efficacy, and drug resistance and diminish side effects, and numerous hybrid molecules are beneath diverse stages of clinical trials, so hybrid derivatives of triazine may offer valuable therapeutic involvement for the dealing of tumours.

OBJECTIVE

The objective of the recent review was to summarize the recent reports on triazine as well as its analogues with respect to its anticancer therapeutic potential.

CONCLUSION

The content of the review would be helpful to update the researchers working towards the synthesis and designing of new molecules for the treatment of various types of cancer disease with the recent molecules that have been produced from the triazine scaffold. Triazine scaffolds based on 1,3,5-triazine considerably boost molecular diversity levels and enable covering chemical space in key medicinal chemistry fields.

摘要

简介

合成和修饰抗癌剂的广泛重要性催生了许多药物化学项目。在这方面,三嗪衍生物因其对多种癌细胞的显著活性而引起了关注。本评价涵盖了工作报道,以确定抗癌活性、针对目标的最活跃合成化合物、SAR,以及当描述时,可能的作用机制,以及类似的被认为提供三嗪衍生物类抗癌药物开发的完整和靶向数据。三嗪骨架用于开发抗癌类似物。三嗪还可以与许多有益的靶点相关,它们的类似物具有良好的抗肿瘤活性。融合分子可以提高疗效、降低耐药性和减少副作用,许多混合分子处于不同的临床试验阶段,因此三嗪的混合衍生物可能为治疗肿瘤提供有价值的治疗干预。

目的

本次综述的目的是总结三嗪及其类似物在抗癌治疗潜力方面的最新报道。

结论

综述的内容将有助于更新致力于合成和设计新分子的研究人员,以治疗各种类型的癌症疾病,这些新分子是从三嗪骨架中产生的。基于 1,3,5-三嗪的三嗪骨架大大提高了分子多样性水平,并能够覆盖关键药物化学领域的化学空间。

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Synthesis and cellular effects of novel 1,3,5-triazine derivatives in DLD and Ht-29 human colon cancer cell lines.新型 1,3,5-三嗪衍生物在 DLD 和 Ht-29 人结肠癌细胞系中的合成及细胞效应。
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探索新型吡咯并[2,1-f][1,2,4]三嗪衍生物作为 c-Met/VEGFR-2 的双重抑制剂以提高抗癌疗效。
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Molecules. 2018 Aug 6;23(8):1956. doi: 10.3390/molecules23081956.
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Design, synthesis and molecular modeling studies of new series of antitumor 1,2,4-triazines with potential c-Met kinase inhibitory activity.具有潜在 c-Met 激酶抑制活性的新型抗肿瘤 1,2,4-三嗪类化合物的设计、合成及分子模拟研究。
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