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Synthesis, In Vitro Anticancer Activity and In Silico Study of some Benzylidene Hydrazide Derivatives

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Abstract:

Some benzylidenehydrazides (3a-e) have been synthesized in three reaction steps from anthranilic acid in good yields, about 70% - 99%. The structures of the synthesized compounds were analyzed using spectroscopic methods. The compounds were evaluated its activity against human lung cancer, A549 cell line by MTT method and studied its molecular docking onto the protein tyrosine kinase (PDB ID: 1M17) by using Molegro® vs. 5.5. The data showed that N-(2-(2-(4-nitrobenzylidene)hydrazinecarbonyl)phenyl)benzamide (3d) which synthesized in 70% yield and has the highest activity on inhibiting the growth of A549 cell line with IC50 10.9μg/mL, which was linier with our in silico study. Compound 3d has the smallest RS value -94.44 kcal/mol, lower than selected Ligand, Erlotinib.

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Periodical:

Key Engineering Materials (Volume 840)

Pages:

277-283

DOI:

https://doi.org/10.4028/www.scientific.net/KEM.840.277

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Online since:

April 2020

Authors:

Melanny Ika Sulistyowaty*, galih putra, Tutuk Budiati, Katsuyoshi Matsunami

Keywords:

A549 Cell Line, Benzylidene Hydrazides, Docking Study, Synthesis, Tyrosine Kinase

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© 2020 Trans Tech Publications Ltd. All Rights Reserved

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