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Design, synthesis, AML activity and molecular modeling of novel IDH2 inhibitors.

Author: GuoHui, JinRuyi, NieFayi, TangTian, TangYuping, WangYuwei, ZhouSha

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

This study investigates the anti-AML activity of novel s-triazine derivatives. Compounds Ta and Th showed excellent inhibition in vitro and prolonged survival in vivo compared to AG-221, suggesting potential for developing novel IDH2 inhibitors.
Paper Details　
Original Abstract of the Article :
Enasidenib (AG-221) is the only approved IDH2 inhibitor, clinical study found Enasidenib have some side-effects. In this work, we synthesized series of novel s-triazine derivatives, and the in vitro and in vivo activity of anti-AML has been studied using AM7577 model. The cell activity found Ta and ...See full text at original site
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引用元：
https://doi.org/10.1016/j.bioorg.2022.106225

データ提供：米国国立医学図書館（NLM）

IDH2 Inhibitors: A New Frontier in Acute Myeloid Leukemia Treatment

Acute myeloid leukemia (AML) is a complex and aggressive type of cancer that requires effective treatment options. This research explores the development of novel inhibitors targeting the IDH2 enzyme, a key player in AML cell growth and survival. The study aims to identify new potential treatments for AML, building upon the existing knowledge of the IDH2 inhibitor enasidenib, which has shown some clinical benefits but also displays certain side effects.

New IDH2 Inhibitors: Expanding the Therapeutic Arsenal

The researchers synthesized a series of novel s-triazine derivatives and tested their efficacy against AML cells in both laboratory and animal models. Their findings suggest that these new compounds exhibit promising anti-AML activity, potentially offering a broader range of treatment options for patients. While these new compounds did not significantly reduce the levels of 2-HG, a metabolic byproduct associated with IDH2 mutations, they showed potential in prolonging survival in animal models. This research highlights the ongoing efforts to develop new and effective AML therapies.

A New Oasis in AML Treatment

This research represents a significant step forward in the search for effective AML treatments. It's like finding a hidden oasis in the vast desert of AML research, offering hope for new and improved therapies. While further research is needed to fully understand the potential of these novel IDH2 inhibitors and translate them into safe and effective clinical treatments, this study serves as a testament to the ongoing efforts to conquer AML and improve the lives of patients.

Dr.Camel's Conclusion

This research sheds light on the promising development of novel IDH2 inhibitors, offering a potential breakthrough in the fight against AML. It's like discovering a new spring of hope in the arid desert of AML research, providing a new source of potential therapies. While further research is needed to translate these findings into effective clinical treatments, this study demonstrates the tireless pursuit of innovative solutions for AML, reminding us that the journey towards conquering this disease continues.

Date :
  1. Date Completed 2022-11-29
  2. Date Revised 2022-12-01
Further Info :

Pubmed ID

36335650

DOI: Digital Object Identifier

10.1016/j.bioorg.2022.106225

Related Literature

Article Analysis
・Side Effects of enasidenib
SNS
PICO Info
in preparation
Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

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