Abstract:
:Carbonic anhydrases (CA I, II, IX and XII) are known to be highly expressed in various human malignancies. CA IX is overexpressed in colorectal cancer specifically in hereditary nonpolyposis colorectal cancer. Inhibition of CA activity by small molecular CA inhibitor like sulphonamides, sulphonamide derivative (SU.D2) or HIF1a inhibitor Chetomin leads to inhibition of tumorigenesis. Eighteen new quinazolin-4-sulfonamide derivatives were prepared and characterized by means of IR, NMR and mass spectra. Certain selected derivatives were tested for their ability to inhibit four isoforms of the metalloemzyme CA, namely, CA I, CA II, CA IX and CA XII. Compound 3c was found to be highly effective in inhibiting the cancer cell proliferation. 3c decreased cell viability of human HT-29 cells in dose and time dependent manner and with IC50 of 5.45 μM. Moreover, it was tested on metastatic colon cancer cell SW-620 where it was found to be equally effective on human SW-620 cells. This novel compound inhibited the CA IX and CA XII protein expression in HT-29 cells without affecting CA I and CA II expression. These findings indicate that 3c inhibits cellular proliferation in two human colon cancer cells by specifically targeting the CA IX and CA XII expression.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Alafeefy AM,Ahmad R,Abdulla M,Eldehna WM,Al-Tamimi AM,Abdel-Aziz HA,Al-Obaid O,Carta F,Al-Kahtani AA,Supuran CTdoi
10.1016/j.ejmech.2016.01.001subject
Has Abstractpub_date
2016-02-15 00:00:00pages
247-53eissn
0223-5234issn
1768-3254pii
S0223-5234(16)30001-0journal_volume
109pub_type
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