Speaker
Description
The design, synthesis and application of luminescent metal complexes as efficient theragnostic
agents have great significance in the field of medicinal chemistry [1]. Luminescent d‐metal ion
complexes are well-known for their therapeutic activities because of their unique
photochemical and photophysical characteristics [2]. 4-amino‐1,8‐naphthalimide derived
Tröger’s base (TBNap) derivatives are novel organic scaffolds that are famous for their robust
DNA binding affinity, quick cellular uptake, and can also act as apoptosis inducers in cancer
cells [3-5]. We have developed a novel luminescent N-4-pyridyl-4-amino-1,8-naphthalimide
Tröger’s base (TB Nap) with unique chiral cleft shape geometry using N-4-pyridyl-4-amino1,8-naphthalimide as the precursor through facile synthetic strategy. Knowing the significance
of ruthenium metal complexes and the naturally available therapeutic agent "curcumin"
and TBNap in the field of cancer therapy, we designed a novel TBNap-containing Ru(II)
curcumin organometallic conjugate (TB-Ru-Cur) by the self-assembly of TBNap with
previously reported arene-Ru(II)-curcuminato complex, Ru-Cur. TB-Ru-Cur displayed a fast
cellular uptake, highly luminescent characteristics, and cytotoxicity against various cancer cell
lines such as HeLa cells, HCT-116, and HepG2 cancer cells with an efficiency much higher
than clinically used cisplatin. In summary, the work herein demonstrates that the TB‐Ru‐
Cur can act as a potent anticancer theragnostic agent thereby bridging the gap between
therapeutic and diagnosis properties.
