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Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
Published on: August 10, 2017
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Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors
Amr K A Bass1, Mona S El-Zoghbi1, El-Shimaa M Nageeb2
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Menoufia University, Menoufia, Egypt.
European Journal of Medicinal Chemistry
|October 20, 2020
Summary
Developing novel anticancer agents is crucial due to rising cancer deaths. Multitargeting hybrids, especially HDAC inhibitors, offer a promising strategy by simultaneously targeting multiple cancer pathways with fewer side effects.
Area of Science:
- Oncology
- Medicinal Chemistry
- Drug Discovery
Background:
- Cancer remains a global health crisis, necessitating innovative therapeutic strategies beyond traditional chemotherapeutics.
- Multitargeting hybrid molecules, which combine multiple pharmacophores, are emerging as a promising approach to overcome treatment challenges and reduce side effects.
- Histone deacetylase (HDAC) inhibitors, a class of multitargeting agents, show potential for synergistic effects with other anticancer drugs and offer facile modification for new drug development.
Purpose of the Study:
- To review recent advancements in multitargeting HDAC inhibitor hybrids for cancer treatment.
- To highlight novel hybrid molecules combining HDAC inhibition with other cancer-targeting pharmacophores.
- To provide insights for future research and development in the discovery of new anticancer therapies.
Main Methods:
- Literature review of recent scientific publications and clinical trial data.
- Analysis of designed multitargeting HDAC inhibitor hybrids and their targeted pathways.
- Identification of key examples of HDAC inhibitor hybrids currently in clinical trials.
Main Results:
- Several HDAC inhibitor hybrids have advanced to clinical trials for various blood and solid tumors, including CUDC-101, CUDC-907, Tinostamustine, and Domatinostat.
- The reviewed multitargeting hybrids incorporate diverse pharmacophores, such as topoisomerase inhibitors, kinase inhibitors, and nitric oxide releasers.
- These hybrids are designed to simultaneously inhibit multiple cancer-related pathways, offering a rationalized approach to treatment.
Conclusions:
- Multitargeting HDAC inhibitor hybrids represent a significant advancement in cancer therapy.
- The development of these rationalized hybrid molecules holds promise for improved efficacy and reduced toxicity.
- This review provides a foundation for further exploration and discovery of novel anticancer agents in this class.
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