Abstract
Background: Quinazoline and sulfonamide derivatives are considered to be important classes of drugs due to their wide range of biological activities especially anticancer.
Methods: A novel series of sulfonamides incorporating benzo[g] quinazolinemoieties 2-19 and sulfonyl containing benzo[g] quinazolinemoieties 20, 21 were designed and synthesized starting from 4- chlorobenzo[g] quinazoline 1. In-vitro screening as anticancer agents was done for the synthesized compounds. Molecular docking study was also performed to explore the binding interactions of the synthesized compounds within the active site of carbonic anhydrase IX (CA IX), which most commonly expressed in some types of cancer cells.
Conclusion: The results indicated that the most potent compounds were 2 and 7 showing effectiveness on more than one cell line.
Keywords: Synthesis, benzo[g]quinazolines, sulfonamides, anticancer.
Medicinal Chemistry
Title:In-Vitro Anticancer Evaluation and Docking Study of Novel Benzo[g] Quinazoline-sulfonamide Derivatives
Volume: 12 Issue: 5
Author(s): Mostafa M. Ghorab, Mansour S. Alsaid, Mohamed S. Al-Dosary and Marwa G. El-Gazzar
Affiliation:
Keywords: Synthesis, benzo[g]quinazolines, sulfonamides, anticancer.
Abstract: Background: Quinazoline and sulfonamide derivatives are considered to be important classes of drugs due to their wide range of biological activities especially anticancer.
Methods: A novel series of sulfonamides incorporating benzo[g] quinazolinemoieties 2-19 and sulfonyl containing benzo[g] quinazolinemoieties 20, 21 were designed and synthesized starting from 4- chlorobenzo[g] quinazoline 1. In-vitro screening as anticancer agents was done for the synthesized compounds. Molecular docking study was also performed to explore the binding interactions of the synthesized compounds within the active site of carbonic anhydrase IX (CA IX), which most commonly expressed in some types of cancer cells.
Conclusion: The results indicated that the most potent compounds were 2 and 7 showing effectiveness on more than one cell line.
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Cite this article as:
Ghorab M. Mostafa, Alsaid S. Mansour, Al-Dosary S. Mohamed and El-Gazzar G. Marwa, In-Vitro Anticancer Evaluation and Docking Study of Novel Benzo[g] Quinazoline-sulfonamide Derivatives, Medicinal Chemistry 2016; 12 (5) . https://dx.doi.org/10.2174/1573406412666160201120921
DOI https://dx.doi.org/10.2174/1573406412666160201120921 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
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Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
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