Design, synthesis and anticancer evaluation of novel tetrahydroquinoline derivatives containing sulfonamide moiety

Sulfonamides posses many types of biological activities and have recently been reported to show substantial antitumor activity in vitro and/or in vivo. There are a variety of mechanisms for the anticancer activity and the most prominent of these is through the inhibition of carbonic anhydrase isozym...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2009-10, Vol.44 (10), p.4211-4217
Main Authors: Ghorab, Mostafa M., Ragab, Fatma A., Hamed, Mostafa M.
Format: Article
Language:English
Subjects:
Anticancer
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Breast Neoplasms - drug therapy
Carbonic anhydrase
Carbonic Anhydrase II - chemistry
Carbonic Anhydrase II - metabolism
Carbonic Anhydrase Inhibitors - chemical synthesis
Carbonic Anhydrase Inhibitors - chemistry
Carbonic Anhydrase Inhibitors - pharmacology
Catalytic Domain
Cell Line, Tumor
Cell Survival - drug effects
Drug Screening Assays, Antitumor
Female
General aspects
Humans
Medical sciences
Models, Molecular
Pharmacology. Drug treatments
Protein Binding
Quinoline
Quinolines - chemical synthesis
Quinolines - chemistry
Quinolines - pharmacology
Structure-Activity Relationship
Sulfonamide
Sulfonamides - chemical synthesis
Sulfonamides - chemistry
Sulfonamides - pharmacology
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Summary:Sulfonamides posses many types of biological activities and have recently been reported to show substantial antitumor activity in vitro and/or in vivo. There are a variety of mechanisms for the anticancer activity and the most prominent of these is through the inhibition of carbonic anhydrase isozymes. The present work reports the synthesis of some novel quinoline and pyrimido[4,5- b]quinoline derivatives bearing a substituted or unsubstituted sulfonamide moiety. The design of the structures of these compounds complies with the general pharmacophore of the sulfonamide compounds that act as carbonic anhydrase (CA) inhibitors as this may play a role in their anticancer activity. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against breast cancer cell line (MCF7). Most of the screened compounds showed interesting cytotoxic activities compared to a reference drug. [Display omitted]
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2009.05.017