Abstract
A series of sulfanilamide-1,2,3-triazole hybrids were designed by a molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, MCF-7 and PC-3). The detailed structure-activity relationships for these sulfanilamide-1,2,3-triazole hybrids were investigated. All these sulfanilamide-1,2,3-triazole hybrids exhibited moderate to potent activity against all cell lines. In particular 4-methyl-N-((1-(3-phenoxybenzyl)-1H-1,2,3-triazol-4-yl)methyl)benzenesulfonamide (11f) showed the most potent inhibitory effect against PC-3 cells, with an IC50 value of 4.08 μM. Furthermore, the tubulin polymerization inhibitory activity in vitro of compound 11f was 2.41 μM. These sulfanilamide hybrids might serve as bioactive fragments for developing more potent antiproliferative agents.
Highlights
Microtubules, as a key component of the cytoskeleton, play important roles in many cellular events, including the maintenance of cell shape, cell migration, cell division and intracellular transport [1,2,3,4]
Alkyne intermediates 9a~i were synthesized as shown in Scheme 1
9a~i were synthesized as coumarinsulfonyl shown in Scheme chloride, 1
Summary
Dong-Jun Fu 1,† , Ji-Feng Liu 1,† , Ruo-Han Zhao 1,† , Jia-Huan Li 1 , Sai-Yang Zhang 2, * and.
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