The cross talk between the over expression of
oxygen-
free radicals is known as
reactive oxygen species (ROS) that is associated with the excessive
telomerase activity (TA).
Telomerase activity is an invariable finding where human
telomerase (hTERT) has been implicated in
tumor oxidative stress and redox-mediated
malignancy. The hTERT over expression is a novel
tumor marker and is promising as a novel class of therapeutic weapons to fight against
cancer. A new series of phenylene
diamines were designed, synthesized, and evaluated for their in vitro
antioxidant as an
indicator of inhibiting the oxidative stress
tumor. Compounds 3b and 7b proved to be the most active
antioxidants with high percentage
ABTS inhibition ranged from 89.40% to 88.59% respectively. Molecular modeling studies indicated that the crest configuration of phenylene
diamine nucleus with substitutions of trimethoxy benzamido functional proved to be crucial for enhancing the
free radical scavenging activity. Molecular modeling exploration indicated the proper binding selectivity of the 3b and 7b to the 3KYL pocket with promising hTERT inhibitors as a hallmark of
cancer.