Anup K Chakraborty

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. Keywords: Anticancer agents, MTT assay, Murine melanoma, Heterocyclic

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Abstract

Background: Catharanthus roseus is a significant therapeutic plant has a place with family apocynaceae contains in excess of 70 distinct sorts of chemotherapeutic agents and alkaloids which help in treating different illnesses. For the most part, it is known as Vincarosea, Ammocallisrosea and Lochnerarosea. There are numerous or more than 400 alkaloids present in plant, which are used as flavor, agrochemicals, pharmaceuticals, fragrance, ingredients, food addictives, and pesticides. Aims and Objectives: To develop a validated high performance thin layer chromatographic method for the analysis of leaves and flower extracts of Sample solutions were applied onto the plates with automatic TLC sampler Linomat V (Camag, Muttenz, Switzerland) and were controlled by WinCATS software. Plates were developed in 10 x 10cm twin trough glass chamber (Camag, Muttenz, Switzerland). A CAMAG TLC scanner was used for scanning the TLC plates. Pre-coated silica gel aluminium plates 60F254. Results: For vincristine, simultaneous estimation of vincristine was performed by HPTLC on a silica gel plate using toluene-methanol-diethylamine (8.75: 0.75: 0.5, v/v/v) as the mobile phase. The method was validated as per the ICH guidelines. The Rf value was found to be 0.76 for flower and 0.80 for leaves at 250 nm which shows the presence of vincristin in . Conclusion: In this research paper, a validated HPTLC Method has been developed for the analysis of leaves and flower extracts Keywords: Catharanthus roseus, Extraction, metabolites, HPTLC

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