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Synthesis of novel N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl | 4000
Drug Designing: Open Access

Drug Designing: Open Access
Open Access

ISSN: 2169-0138

+44 1223 790975

Synthesis of novel N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl) piperidine-4- carboxamide derivatives as potential antiangiogenic and DNA cleavage agents


International Conference and Expo on Drug Discovery & Designing

August 11-13, 2015 Frankfurt, Germany

Vinaya K

Posters-Accepted Abstracts: Drug Des

Abstract :

A series of novel N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)piperidine-4-carboxamide derivatives 10(a-f),
12(a-c) and 14(a-c) were synthesized and were characterized by FTIR, 1H-NMR, mass spectral and elemental analysis. In the
present study, the efficacy of the derivatives to inhibit the angiogenesis in vivo was evaluated in chorioallantoic membrane (CAM)
model and also evaluated DNA cleavage studies by gel electrophoresis. The compounds suppressed the blood vessel formation in vivo
in chorioallantoic membrane model. The difference observed in the band width and intensity is the criterion for the evaluation of
binding/cleavage ability of synthetic molecule with calf thymus DNA. Among the tested compounds 10a, 10b, 10c, 12b, 14b and 14c
showed a significant anti-angiogenic and DNA cleavage activity. We reasoned that the presence of electron donating and withdrawing
groups at the 2nd, 3rd and 4th position of the phenyl ring of the side chain may determine the potency of the molecule. Further
studies are required to reveal the exact mechanism of action of these N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)
piperidine-4-carboxamide structures.

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