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Anticancer Effects of New Dibenzenesulfonamides by Inducing Apoptosis and Autophagy Pathways and Their Carbonic Anhydrase Inhibitory Effects on hCA I, hCA II, hCA IX, hCA XII Isoenzymes

Anticancer Effects of New Dibenzenesulfonamides by Inducing Apoptosis and Autophagy Pathways and Their Carbonic Anhydrase Inhibitory Effects on hCA I, hCA II, hCA IX, hCA XII Isoenzymes

Halise Inci Gul, Cem Yamali, Merve Bulbuller, Petek Ballar Kirmizibayrak, Mustafa Gul, Andrea Angeli, Silvia Bua, Claudiu T Supuran

Bioorg Chem. 2018 Aug;78:290-297.

PMID: 29621641

Abstract:

In this study, new dibenzensulfonamides, 7-9, having the chemical structure 4,4'-(5'-chloro-3'-methyl-5-aryl-3,4-dihydro-1'H,H-[3,4'-bipyrazole]-1',2-diyl)dibenzenesulfonamide were synthesized in five steps to develop new anticancer drug candidates. Their chemical structures were confirmed by 1H NMR, 13C NMR and HRMS spectra. Cytotoxicities of the dibenzensulfonamides were investigated towards HCC1937, MCF7, HeLa, A549 as tumor cell lines and towards MRC5 and Vero as non-tumor cells. Carbonic anhydrase (CAs, EC 4.2.1.1) inhibitory effects of the dibenzensulfonamides 7-9 were also evaluated on the cytosolic human (h) hCA I and II and the tumor-associated hCA IX and XII isoenzymes. Results indicate that both 7 and 8 induced cleavage of poly (ADP ribose) polymerase (PARP), activation of caspases -3, -7 and -9 which are the hallmarks of apoptosis. Meanwhile both compounds induced autophagy in HCC1937 cells which is shown by enhanced expression of LC3 and decreased level of p62 protein. The compounds tested were also effectively inhibited tumor-associated hCA IX and hCA XII isoenzymes in the range of 20.7-28.1 nM and 4.5-9.3 nM, respectively.

Chemicals Related in the Paper:

Catalog Number	Product Name	CAS Number	Price
AP220509740	Caspase-3/7 Inhibitor I - CAS 220509-74-0	220509-74-0	Price
AP489457672	PARP Inhibitor XII - CAS 489457-67-2	489457-67-2	Price
AP775289208	Caspase-3/7 Inhibitor II - CAS 775289-20-8	775289-20-8	Price

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