Design, synthesis and anticancer activity of substituted benzoxazole derivatives
Journal name: World Journal of Pharmaceutical Research
Original article title: Design, synthesis and anticancer activity of substituted benzoxazole derivatives
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Chetan K., Prabhudev S. M., H. J. Kallur and Laxmisagar
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Design, synthesis and anticancer activity of substituted benzoxazole derivatives
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr202314-29340
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
The research article by Chetan et al. discusses the design, synthesis, and anticancer activity of substituted benzoxazole derivatives. These derivatives, particularly those combined with azetidinone, are explored for their potential therapeutic effects against cancer. The study emphasizes the significance of these heterocycles in medical chemistry, particularly their interactions with the Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), a crucial target in cancer therapy. The compounds were characterized using various spectroscopic techniques, and their efficacy was evaluated through in vitro assays.
Anticancer Activity of Benzoxazole Derivatives
Benzoxazole derivatives are known for their diverse biological activities, including their anticancer properties. The study synthesized five derivatives of benzoxazole substituted azetidinone and tested their anticancer effects using the MTT assay. The results indicated that specific compounds, such as CK-5, exhibited significant inhibition of cancer cell viability, demonstrating their potential as effective anticancer agents. The percentages of cell viability and inhibition at different concentrations showcased the promising therapeutic applications of these synthesized compounds in combatting cancer.
Molecular Docking Studies
Molecular docking studies were conducted to assess the binding affinity of the synthesized benzoxazole derivatives to the VEGFR-2 receptor. The docking scores indicated a strong interaction, particularly for compounds CK-5, CK-1, and CK-2, which showed high binding scores, suggesting their potential efficacy in inhibiting VEGFR-2-related pathways involved in cancer progression. This analysis provided insights into the mechanisms through which these compounds could exert their anticancer effects, enhancing their viability as drug candidates.
Spectral Characterization Techniques
The synthesized derivatives were characterized using various spectral techniques, including IR spectroscopy, proton and carbon NMR, and mass spectrometry. These methods confirmed the chemical structures of the derivatives and validated their purity. The IR spectra provided insights into functional groups present, while NMR offered detailed information on the molecular framework. The results from mass spectrometry, particularly for compounds CK-2 and CK-5, further supported the synthesis with clear peaks correlating to expected molecular weights, demonstrating the successful development of new therapeutic candidates.
Conclusion
In summary, the study conducted by Chetan et al. successfully synthesized and evaluated a series of benzoxazole substituted azetidinone derivatives for their anticancer activity. The findings highlighted the significant potential of these compounds as therapeutic agents targeting key pathways in cancer, particularly through their interactions with VEGFR-2. The integration of synthetic methods, biological evaluations, and molecular docking studies underscored the promising future of these derivatives in cancer treatment, warranting further research and development. The collaboration of the authors with the RMES College of Pharmacy indicates a foundation for continued exploration in pharmaceutical chemistry.
FAQ section (important questions/answers):
What are the main compounds studied in this research?
The main compounds studied are benzoxazole and azetidinone derivatives, which exhibit significant anticancer activities.
What methods were used to characterize the synthesized compounds?
The synthesized compounds were characterized using techniques like IR spectroscopy, 1H NMR, 13C NMR, and mass spectral analysis.
How was the anticancer activity of derivatives evaluated?
The anticancer activity was evaluated through the MTT assay performed on SKMEL cell line, measuring cell viability at various concentrations.
Which derivative showed the highest anticancer activity in this study?
The compound CK-5 exhibited the highest anticancer activity compared to other tested derivatives.
What target was selected for the molecular docking studies?
The target selected for molecular docking studies was the VEGFR-2 receptor, which is crucial for cancer cell proliferation.
What was the conclusion of the docking studies?
The docking studies concluded that compounds CK-5, CK-1, and CK-2 showed high binding affinity towards the VEGFR-2 protein.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Design, synthesis and anticancer activity of substituted benzoxazole derivatives”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.
1) Activity:
The term 'activity' in this context refers to the biological effects exhibited by the synthesized benzoxazole derivatives, particularly their ability to inhibit cancer cell proliferation. The activity is a crucial measure in pharmacology, indicating how effective a compound is against diseases, especially cancer. Understanding activity helps in drug development and effectiveness assessments.
2) Table:
In the context of scientific research, 'table' refers to a systematic arrangement of data, typically used to summarize results and findings for easier comparison and analysis. Tables in the study present physical data, spectral information, and results from biological assays, enhancing clarity and allowing straightforward interpretation of experimental outcomes.
3) Study (Studying):
The phrase 'the study' refers explicitly to the presented research work involving the design and synthesis of benzoxazole derivatives and their evaluation for anticancer activity. This study provides insights into the methodologies utilized, results achieved, and the implications of these results for future cancer therapeutics and research.
4) Cancer:
Cancer is a significant focus of the research, representing a group of diseases characterized by uncontrolled cell growth and potential metastasis. Understanding cancer's molecular mechanisms and finding effective compounds to combat it is essential for developing effective therapeutics. This study aims to develop compounds that may offer new avenues for cancer treatment.
5) Discussion:
The term 'discussion' pertains to the section of the paper where results are analyzed and interpreted. It reflects on the synthesized compounds' effectiveness, comparing findings to existing literature. This part is crucial as it contextualizes the research within the broader field, highlighting the study's significance and potential future applications.
6) Karnataka:
Karnataka is a state in India where the research was conducted, specifically at RMES College of Pharmacy in Kalaburagi. The location is relevant as it reflects the geographical and institutional context of the study. Highlighting local research contributions can foster collaborations and showcase the region's commitment to pharmaceutical sciences.
7) Mutation:
Mutation refers to the alterations in the DNA sequence of cells, which can lead to cancer development. Understanding the role of mutations is critical in cancer research, as they often significantly contribute to tumor evolution and resistance to therapies. The study addresses the importance of designing compounds that target hallmark features associated with mutations.
8) Balaji:
Balaji refers to the neighborhood in Kalaburagi, Karnataka, where RMES College of Pharmacy is located. The place is significant as it sets the geographical context for the research environment, influencing local educational initiatives and research output in pharmacology and medicinal chemistry within the region.
9) India:
India is the country where the research was carried out. Its diverse population and increasing burden of diseases like cancer necessitate innovative therapeutic strategies. Conducting the study within India can enhance accessibility to potential treatments and contribute to the global biomedical research landscape, addressing local health challenges.
10) Nakar:
Nagar translates to 'town' or 'city' in many Indian languages and is part of the name Balaji Nagar, where the research is conducted. It indicates the urban environment associated with the study, where educational and healthcare infrastructures support research activities aimed at addressing pressing health issues like cancer.
11) Road:
The word 'road' in this context is part of the address for RMES College of Pharmacy in Kalaburagi, Karnataka. It signifies the physical location where the research is carried out, thereby providing logistical and contextual information about the institutional setting and the infrastructure supporting scientific inquiry.
12) Line:
The term 'line' in a biological context often refers to a line of cells, such as the 'SKMEL cell line' used in the MTT assay within the study. Cell lines are crucial for experimental research, providing consistent and controllable models for testing drug efficacy and understanding cancer mechanisms.
13) Human body:
The 'human body' is the biological context within which cancer develops. Understanding the interactions between drugs and human physiology is essential for developing effective therapeutics. The study emphasizes the importance of targeting specific molecular pathways involved in cancer to improve treatment outcomes for patients in the human body.
14) Antibiotic (Antibacterial):
The term 'anti-bacterial' refers to the ability of certain compounds to inhibit bacterial growth. Although the primary focus of the study is anticancer activity, understanding the broader biological spectrum of benzoxazole derivatives, including their anti-bacterial properties, can pave the way for multifaceted therapeutic applications and potential combination therapies.
15) Inflammation:
Inflammation is a biological response that can play a role in cancer progression. Understanding the relationship between inflammation and cancer is vital in medicinal chemistry to develop compounds that not only target cancer cells directly but also modulate the inflammatory environment, potentially improving therapeutic outcomes.
16) Disease:
The term 'disease' signifies any condition that disrupts normal physiological functions, including cancer. The study's relevance lies in its aim to develop new therapeutic agents to combat diseases like cancer, illustrating the critical importance of innovative research in addressing health challenges and improving patient well-being.
17) Purity:
Purity refers to the degree of absence of impurities in the synthesized compounds, which is crucial for ensuring accurate experimental results. In pharmaceutical research, the purity of compounds influences their biological activity, safety, and efficacy, thus, measuring and optimizing purity is a core aspect of drug development.
18) Glass:
Glass is a material commonly used for laboratory equipment like beakers and petri dishes. Its relevance in the study pertains to the experimental setup, as glassware is fundamental for conducting reactions, crystallization processes, and various assays needed for synthesizing and analyzing the benzoxazole derivatives developed in the study.
19) Water:
Water is a solvent and a critical component in many laboratory procedures. In the study, water plays a role in various synthesis and crystallization steps. The use of water as a solvent highlights the importance of choosing suitable media for reactions, which can impact the efficiency and yields of chemical transformations.
20) Death:
Death in this context refers to the loss of cellular function, especially in cancer cells. The study aims to develop compounds that can induce death in cancer cells, offering therapeutic solutions for effectively treating malignant tumors. Targeting cancer cell survival pathways is a crucial goal in cancer pharmacology.
21) Beta:
Beta often relates to beta-lactams, a class of compounds known for their antibacterial properties. While the focus here is on anticancer activity, understanding various compound classes allows researchers to explore diverse mechanisms of action and potentially develop multi-target drugs that could address several diseases concurrently.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Design, synthesis and anticancer activity of substituted benzoxazole derivatives’. Further sources in the context of Science might help you critically compare this page with similair documents:
Purification method, Anticancer activity, Molecular docking, Binding affinity, Docking Score, MTT assay, Antineoplastic activity, Biological evaluation, Invasion and metastasis.