Abstract :
Background: The development of new anticancer agents is one of the most pressing research areas in medicinal chemistry and medicine. The importance of triazole and pyridine rings as scaffolds present in a wide range of therapeutic agents has been well reported and has driven the synthesis of a large number of novel anticancer agents. The presence of these heterocyclic furnishes extensive synthetic possibilities due to the presence of several reaction sites. Prompted by these data we designed, synthesized and evaluated a series of novel 1, 2, 4-triazole-pyridine hybrid derivatives as potential anticancer agents.
Aims and Objectives: To design and synthesize series of novel 1, 2, 4-triazole-pyridine hybrid derivatives as potential anticancer agents
Materials and Methods: Derivatives were synthesized by the reaction of nicotinohydrazide with carbon disulfide to yield potassium-3-pyridyl-dithiocarbazate (I). This was further cyclized with ammonia solution to yield 5-mercapto-substituted 1, 2, 4-triazole-pyridine hybrid (II). This was finally reacted with different substituted benzyl derivatives to produce 1, 2, 4-triazole-pyridine hybrid derivatives (III). The purity of the derivatives was confirmed by thin-layer chromatography and melting point. Structure of these derivatives was set up by determining its infrared spectroscopy, nuclear magnetic resonance spectroscopy and mass spectroscopy. Further, the synthesized 1, 2, 4 triazole pyridine derivatives were tested for their in vitro anticancer activities against murine melanoma (B16F10) using the MTT reduction assay method.
Results: The cell viability study of synthesized compounds concludes that all compounds have moderate to potent anticancer activities against cancer cell lines. Compounds TP1-TP7 have IC in the range of 41.12?M to 61.11?M and the highest activity was observed for compound TP6 against murine melanoma (B16F10) cell line.
Thepresent research may pave a way for the development of 1, 2, 4-triazole-pyridine as novel anticancer agents with good efficacy and lesser adverse effects.
Keyword :
Anticancer agents, MTT assay, Murine melanoma, Heterocyclic