Medicinal chemistry (Shariqah (United Arab Emirates)) · 2016
In-Vitro Anticancer Evaluation and Docking Study of Novel Benzo[g] Quinazoline-sulfonamide Derivatives.
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Ghorab Mostafa M, Alsaid Mansour S, Al-Dosary Mohamed S, El-Gazzar Marwa G
Аннотация
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.
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.