AI Article Synopsis
- A series of bis-naphthalimide derivatives (NI1-NI8) were created, incorporating nitrogenous heterocycles, and their effects were tested on several cancer cell lines including HeLa, MCF-7, A549, and MGC-803.
- Compounds NI1 and NI4, modified with piperidine and piperazine, demonstrated strong cytotoxic effects, outperforming the control drug Amonafide against HeLa and MGC-803 cells.
- The study also explored DNA binding properties and fluorescence imaging, revealing that NI1 and NI4 had enhanced fluorescence due to strong interactions with Ct-DNA and visibly targeted lysosomes in HeLa cells.
Article Abstract
A series of novel N,N-bis(3-aminopropyl)methylamine bridged bis-naphthalimide derivatives NI1-NI8 containing saturated nitrogenous heterocycles were designed and synthesized, their cytotoxic activities against Hela, MCF-7, A549 and MGC-803 cells were investigated, Compounds NI1-NI4 modified with piperidine and piperazine exhibited good and selective cytotoxic activity, for instance, compounds NI1 and NI4 showed potent cytotoxic activity against Hela cells and MGC-803 cells with the IC values of 2.89, 060, 2.73 and 1.60 μM, respectively, better than the control drug (Amonafide). However, compounds NI5-NI8 conjugated with pyrrole derivatives showed weak cytotoxic activities against the all tested cell lines. Furthermore, their DNA binding properties, fluorescence imaging and cell cycle were investigated. Interestingly, compounds NI1 and NI4 showed fluorescence enhancement because of the strong binding with Ct-DNA, and exhibited fluorescence imaging with Hela cells on the lysosomes.
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| http://dx.doi.org/10.1016/j.bmcl.2018.01.008 | DOI Listing |
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