Background: Apart from the “hit drugs”, there are many others being studied for their
potent activity against several hostilities. To date, anticancer research has been exploited on the
inherent versatility and active core skeleton of the compounds. Literature suggests that nitrogen rich
molecules are most active and found in their potent cancer activity. Purine-based compounds such
as olomoucine and roscovitine, which contain other heterobicyclic ring systems, are useful for the
cell proliferation inhibitors in the treatment of many types of cancer.
Methods: We put forward the novel purine based compounds, aryl amino-quinoline-purine by a
two-step procedure. In the first step, nitrogen rich molecule was synthesized by the coupling of 2,6-
dichloropurine with 3-aminoquinoline in an acidic reaction conditions at the C-6 position of purine.
Aryl amines were introduced at the C-2 position by acid catalyst and using polar solvent at comparatively
higher reaction conditions to furnish the desired products.
Results: Stereochemical aspect was introduced for the identification of attachment of 3-
aminoquinoline at the C-2/ C-6 position of purine and it was concluded by the spectral analysis
(HMBC spectrum). The spectral data revealed that the first chloro-amine coupling was directed at
the C-6 position rather than C-2 and the second chloro-amine coupling by various aryl amines were
directed at the C-2 position. The applications of synthesized compounds were identified by their
cytotoxic study against NCI-60 cell-lines. Out of nine selected molecules by NCI, 5a has shown
promising response in a single dose study and GI50 value, 7.57 µM indicated that it has 7.57% lethality
over HOP-92 cell-line (non-small cell lung cancer panel).
Conclusion: Two straightforward novelties were introduced, first stereochemical identification for
chloro-amine coupling in purine either at the C-2 or C-6 position on the basis of HMBC spectrum.
And a second type of uniqueness was to identify better anti-cancer agents out of synthesized scaffolds.
Overall study shows that compound 5a is a novel therapeutic agent after modification for the
treatment of non-small cell lung and it satisfied determined threshold growth inhibition criteria at a
single dose level.