European Journal of Chemistry

Synthesis, characterization, anticancer activity, optical spectroscopic and docking studies of novel thiophene-2-carboxaldehyde derivatives

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Published: Dec 31, 2016
DOI: https://doi.org/10.5155/eurjchem.7.4.454-462.1505
Keywords:
Molecular docking, Anticancer activity, Drug binding pocket, Antimicrobial activity, Hydrophobic interaction, Fluorescence resonance energy transfer
Section
Research Article
Issue
Vol. 7 No. 4 (2016): December 2016
Dates
Received 2016-10-31
Accepted 2016-11-19
Published 2016-12-31


Main Article Content

Mohamed Ahadu Shareef
Post Graduate and Research Department of Chemistry, The New College, Chennai-600014, Tamil Nadu, India
Mohamed Musthafa
Post Graduate and Research Department of Chemistry, The New College, Chennai-600014, Tamil Nadu, India
Devadasan Velmurugan
Centre of Advanced Study in Crystallography and Biophysics, University of Madras, Chennai-600025, Tamil Nadu, India
Subramani Karthikeyan
Department of Medical Physics, Anna University, Chennai-600025, Tamil Nadu, India
Singaravelu Ganesan
Department of Medical Physics, Anna University, Chennai-600025, Tamil Nadu, India
Syed Ali Padusha
Post Graduate and Research Department of Chemistry, Jamal Mohamed College, Tiruchirappalli-620020, Tamil Nadu, India
Saiyad Musthafa
Post Graduate and Research Department of Zoology, The New College, Chennai-600014, Tamil Nadu, India
Jamal Mohamed
Post Graduate and Research Department of Zoology, The New College, Chennai-600014, Tamil Nadu, India

Abstract

2-((4-Methylpiperazin-1-yl)(thiophen-2-yl)methyl)hydrazinecarboxamide (L1) and (2-(piperazin-1-yl(thiophen-2-yl)methyl)hydrazinecarboxamide (L2) from the family of thiophene-2-carboxaldehyde derivatives have been synthesized. These new compounds have good antibacterial as well as antifungal activity and also less toxic in nature. Exemplary binding characteristics of these novel compounds and pharmacokinetic mechanism were confirmed by optical spectroscopic, anticancer and docking studies. The binding of thiophene-2-carboxaldehyde derivatives to carrier protein, Human Serum Albumin (HSA) has been investigated by studying its quenching mechanism, binding kinetics and the molecular distance (r) between donor (HSA) and acceptor (thiophene-2-carboxaldehyde derivatives) according to Forster’s theory of non-radiative energy transfer (FRET). The micro environment of HSA has also been studied by using synchronous fluorescence spectroscopy technique and the molecular docking technique has been used to explore the hydrogen bonding, hydrophobic interaction between the human serum albumin with L1 and L2 compound.


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Shareef, M. A.; Musthafa, M.; Velmurugan, D.; Karthikeyan, S.; Ganesan, S.; Padusha, S. A.; Musthafa, S.; Mohamed, J. Synthesis, Characterization, Anticancer Activity, Optical Spectroscopic and Docking Studies of Novel Thiophene-2-Carboxaldehyde Derivatives. Eur. J. Chem. 2016, 7, 454-462.

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