Synthesis and photobiological applications of naphthalimide-benzothiazole conjugates: cytotoxicity and topoisomerase IIα inhibition

Conjugates of naphthalimide, benzothiazole, and indole moieties are synthesized that show excellent cytotoxicity against A549 (lung), MCF7 (breast), and HeLa (cervix) cancer cell lines with IC50 values in the range of 0.14-8.59 mu M. Compounds 12 and 13 substituted with ethanolamine and propargyl groups reveal potent cytotoxicity towards A549 cancer cells with IC50 values of 140 and 310 nM, respectively. These compounds are further evaluated as potent inhibitors of human type II alpha topoisomerase. These conjugates also reveal strong interaction towards human serum albumin (HSA) with binding constant values of 1.75 x 10(5) M-1 and 1.88 x 10(5) M-1, respectively, and formation of the stable complex at ground state with static quenching. Docking studies also confirm the effective interactions between conjugates and topoisomerase.

Automated summary

Synthesized conjugates of naphthalimide, benzothiazole, and indole moieties exhibit excellent cytotoxicity against various cancer cell lines, with compounds substituted with ethanolamine and propargyl groups showing potent toxicity towards A549 cancer cells. These conjugates demonstrate strong interaction with HSA and effective inhibition of topoisomerase.