Phen-DC3 probes that reveal G4 ligand localization

A Phen-DC3 handle lets chemists add BODIPY or a cell-penetrating peptide without losing G4 selectivity, showing the parent ligand misses the nucleus.

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Why is Phen-DC3 surprisingly weak on HeLa viability?

It causes only about 20% cell death at 100 μM after 48 h because it fails to enter the nucleus.

Where does fluorescent Phen-DC3 go in live cells?

It cannot enter the nucleus and partially localizes in mitochondria.

What mitochondrial DNA phenotype follows Phen-DC3 treatment?

A concentration-dependent decrease in mtDNA copy number in HeLa cells.

Which phenanthroline positions are safe attachment points?

Positions 5 and 6 on the central phenanthroline scaffold.

What yield was reported for dicarboxylic acid 4?

56% overall yield from the nitration/oxidation sequence.

What yield was reported for HATU coupling to 6?

87% yield.

How was the Phen-DC3 primary amine 7 obtained?

Pd/C hydrogenation of the nitro group, 72% yield.

Does BODIPY attachment wreck G4 vs dsDNA selectivity?

No: FRET melting still shows efficient G4 stabilization and selectivity over dsDNA.

What assay checked polymerase stalling at G4 DNA?

A Taq polymerase stop assay.

What does the cell-penetrating peptide conjugate do?

It retains G4 selectivity/stabilization in vitro but strongly increases cellular effects via better cellular and nuclear localization.

Do large charged conjugates destroy G4 stabilization?

No: even large and charged groups leave Phen-DC3’s potent, selective G4 stabilization intact.