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A series of triphenylethylene‐naphthalimide (TPE‐naph) conjugates was synthesized by a molecular hybridization technique, and their anticancer activity was evaluated in vitro on 60 human cancer cell lines through their cytotoxicity. The ratios of E and Z isomers were determined on the basis of HPLC methodology and NMR spectroscopy. The structure‐activity relationship for anticancer activity was deduced on the basis of the nature and bulkiness of the amine attached to the C‐4 position of the naphthalene ring. Experimental and molecular modeling studies of the most active TPE‐naph conjugate bearing a morpholinyl group showed that it was able to inhibit topoisomerase‐II (TOPO‐II) as a possible intracellular target. Moreover, the transportation behavior of TPE‐naph conjugate towards human serum albumin (HSA) indicated efficient binding affinity. The steady‐state and time‐dependent fluorescent results suggested that this conjugate quenched HSA significantly through static as well as dynamic quenching. Thus, this report discloses the scope of triphenylethylene‐naphthalimide (TPE‐naph) conjugates as efficient anticancer agents.

N-Benzothiazolyl-1,8-naphthalimide based fluorescent probes were designed and synthesized for selective detection of human serum albumin (HSA) and bovine serum albumin (BSA) among various bioanalytes and further studied for their in vitro anti-proliferative activity against 60 human cancer cell lines.

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