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Published on: November 10, 2013
A Review on the Synthesis and Anticancer Potentials of Imidazothiazole Derivatives
Payal Kamboj1, Anjali Mahore1, Asif Husain1
1Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.
Abstract:
Cancer is one of the severe diseases in which abnormal cells divide and proliferate in an uncontrolled manner without any regulation. Globally cancer is among the leading causes of death; according to a recent report of by the WHO, around 10 million people died in 2018 due to cancer. It has also been reported that by 2040, approximately 30 million new cases will be reported every year. The increase in the incidences of cancer is taking a toll on the health care system worldwide. Considerable scientific literature is available on anticancer agents but newer therapeutic strategies are still required in this field to address novel approaches to drug design and discovery to counter this problem. Imidazothiazole represents a privileged scaffold in medicinal chemistry and provides the medicinal chemist the possibility to modulate the physiochemical properties of the lead compound. In recent times, imidazothiazole scaffold is broadly explored for its anticancer activity, which acts through various mechanisms such as EGFR, B-RAF, DHFR kinase inhibition and tubulin polymerization inhibition and other molecular mechanisms of action. Due to their feasible synthetic accessibility and promising pharmacological profile, it has attracted various medicinal chemists to explore and develop imidazothiazole derivatives as potent and safe anticancer agents. In the present article, we have reviewed various potent imidazothiazole scaffold-based derivatives reported as anticancer agents, their synthetic strategies, Structure Activity Relationship (SAR), mechanism of action, and molecular docking along with their future perspective. This review will be very useful for medicinal chemists for drug design and development of imidazothiazole-based potent antiproliferative agents.
Insights
Imidazothiazole derivatives show promise as anticancer agents, acting through various molecular mechanisms. This review explores their synthesis, SAR, and potential for developing novel antiproliferative drugs.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Oncology
Background:
- Cancer is a leading global cause of death, with increasing incidence necessitating novel therapeutic strategies.
- Existing anticancer agents face challenges, driving the need for new drug design and discovery approaches.
- The imidazothiazole scaffold is recognized for its potential in developing effective anticancer drugs.
Approach:
- This review synthesizes recent findings on imidazothiazole derivatives as anticancer agents.
- It covers synthetic strategies, Structure-Activity Relationships (SAR), and mechanisms of action.
- Molecular docking studies and future perspectives are also discussed.
Key Points:
- Imidazothiazole derivatives exhibit anticancer activity via diverse mechanisms, including kinase inhibition (e.g., EGFR, B-RAF, DHFR) and tubulin polymerization inhibition.
- Their synthetic accessibility and favorable pharmacological profiles make them attractive for drug development.
- SAR studies guide the optimization of these compounds for enhanced potency and safety.
Conclusions:
- Imidazothiazole-based compounds represent a promising class of antiproliferative agents.
- Further research into their synthesis and mechanism of action can lead to novel cancer therapies.
- This review provides valuable insights for medicinal chemists in designing next-generation anticancer drugs.
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