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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Macromolecular Drug Targets in Cancer Treatment and Thiosemicarbazides as Anticancer Agents
Ş Güniz Küçükgüzel1, Göknil P Coşkun
1Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpaşa 34668 İstanbul, Turkey. gkucukguzel@marmara.edu.tr.
Abstract:
Cancer is known as abnormal cell division and consisting of a group of diseases on various organ tissues. Many therapies are available in cancer treatment such as chemotherapy, radiotherapy etc. Without damaging normal tissue, there is a huge need for specified anticancer drugs which have effect only on abnormal cancer cells. Therefore, advances in anticancer drug discovery in treating cancer in the recent years, directed towards to the macromolecular targets. Heterocyclic molecules, such as fluconazole, acetazolamide, etc., have a significant role in health care and pharmaceutical drug design. Thiosemicarbazides (NH<sub>2</sub>-NH-CSNH<sub>2</sub>) are the simplest hydrazine derivatives of thiocarbamic acid and are not only transition compounds, but they are also very effective organic compounds. Thiosemicarbazides possess an amide and amine protons, carbonyl and thione carbons. These structures have attracted the attention of the researchers in the development of novel compounds with anticonvulsant, antiviral, anti-inflammatory, antibacterial, antimycobacterial, antifungal, antioxidant and anticancer activities. Recently, a number of thiosemicarbazides are available commercially as anticancer drugs for novel anticancer drug discovery. Antineoplastic or anticancer drugs prevent or inhibit the maturation and proliferation of neoplasms. These observations have been guiding the researchers for the development of new thiosemicarbazides that possess anticancer activity.
Insights
Thiosemicarbazides are versatile organic compounds showing significant potential in cancer treatment. Their unique structure allows for targeted anticancer activity, driving the development of novel antineoplastic drugs.
Area of Science:
- Medicinal Chemistry
- Organic Chemistry
- Pharmacology
Background:
- Cancer is characterized by abnormal cell division, necessitating targeted therapies beyond traditional chemotherapy and radiotherapy.
- Current research emphasizes developing anticancer drugs that selectively target cancer cells, minimizing damage to healthy tissues.
- Heterocyclic molecules play a crucial role in pharmaceutical drug design and healthcare.
Purpose of the Study:
- To explore the potential of thiosemicarbazides as a novel class of anticancer agents.
- To highlight the structural features of thiosemicarbazides that contribute to their diverse biological activities.
- To underscore the growing importance of thiosemicarbazides in antineoplastic drug discovery.
Main Methods:
- Review of existing literature on thiosemicarbazide synthesis and biological activities.
- Analysis of the chemical structure of thiosemicarbazides and their functional groups (amide, amine, thione).
- Investigation of reported pharmacological properties including anticonvulsant, antiviral, anti-inflammatory, antibacterial, antifungal, antioxidant, and anticancer activities.
Main Results:
- Thiosemicarbazides exhibit a broad spectrum of biological activities, including potent anticancer effects.
- The presence of specific functional groups in thiosemicarbazide structures is key to their therapeutic potential.
- Several thiosemicarbazide derivatives have shown promise as antineoplastic agents, with some already available commercially.
Conclusions:
- Thiosemicarbazides represent a promising scaffold for the development of new, targeted anticancer drugs.
- Further research into thiosemicarbazide derivatives is warranted to optimize their efficacy and safety in cancer treatment.
- The unique chemical properties of thiosemicarbazides make them valuable candidates for novel drug discovery in oncology.
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