Design, synthesis and antitumor activity evaluation of 1,4-naphthoquinone-benzene sulfonamide hybrids

A series of novel 1, 4-naphthoquinone-benzene sulfonamide hybrids were designed and synthesized in order to explore the anticancer activity of 1, 4-naphthoquinone and benzene sulfonamide derivatives.

1,4-naphthoquinone-benzene sulfonamide hybrids were synthesized and characterized using ¹HNMR and ¹³CNMR followed by traditional chemical synthesis methods techniques. Then, synthetic compounds were evaluated in vitro for their potentials to anticancer activity.

Derivative 4m displayed the most potent antiproliferative activities against bladder cancers (T24 cells) with the IC₅₀ value of 8.12 μM. Further pharmacological experiments have shown that 4m can inhibit the formation of T24 cells colonies and induce cell apoptosis by downregulating the expression of Bcl-2, caspase-3, caspase-8, caspase-9, and Fas protein, and upregulating the expression of P21 and Cytochrome c protein. It also has an inhibitory effect on the migration of cancer cells. Moreover, 4m showed potent anti-tumor activity in vivo.

Present study highlighted compound 4m could be a potential anti-bladder cancer agent in future.