Telomerase 1 is a reverse transcriptase enzyme found in both healthy and tumor cells, that synthesizes TTAGGG repeats on the ends of chromosomes. These repeats protect chromosomes from degradation and make the cell immortal, a key feature of cancer.  It has been found that nearly every type of cancer exhibits increased telomerase activity, which makes it a novel target for anti-cancer drug development. 2Some acridines have shown promising results in inhibiting the enzyme telomerase.  There is experimental evidence that acridine moieties intercalate with the G- quadruplex structure of telomere and therefore they disrupt the telomerase activity.3  We have developed synthetic procedures for preparation of wide variety of diverse acridine based anticancer libraries.  We will present our results toward library preparation of those libraries along with their biological data for selected acridine derivatives.References1)      Harley B.K. Nat RevCancer 2008 , 8, 167-169.2)      Kim W.N.; Piatyszek A.M.; Prowse R.K.; Harley B.K.; West D.M.; Ho L.C.P.; Coviello M.G.; Wright E.W.; Weinrich L.W.; Shay W.J. Science 1994 . 266. 2011-2015.Campbell H.N.; Parkinson N.G.; Reszka P.A.; Neidle S. J. Am. Chem. Soc 2008 , 130, 6722-6724.

Synthesis and biological evaluation of conjugated acridines

245th National Meeting (2013)

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