Design and synthesis of novel nucleobase-based barbiturate derivatives as potential anticancer agents

Bhaveshkumar D. Dhorajiya, Ahmed Salah Ibrahim, Farid A. Badria, Bharatkumar Z. Dholakiya

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

Cancer today remains one of the most deadly diseases in the world. In search of novel anticancer agents, a series of newly hybrid molecules were designed and synthesized by combining the structural features of nucleobase and barbiturate derivatives using the concept of green chemistry. This approach was accomplished efficiently using the aqueous medium to give the corresponding products in a high yield. The newly synthesized compounds were characterized by spectral analysis FT-IR, 1H NMR, 13C-NMR, HMBC, MASS and elemental analysis. Evaluations of these molecules over four cell lines panel of human cancer cells have identified several compounds with significant anticancer activities against one or more cell lines. Compounds TBC and TBA proved to exhibit a wide cytotoxic effect on the tested four cell lines at (IC50 16-24 μM) and (IC50 25-34 μM), respectively. Other compounds, e.g., 1,3-BA, showed a selective cytotoxicity against HepG2 at 7 μM. Taken together, this study has led to the development of a convenient, a highly yielded, and an environmentally friendly synthetic method of highly promising leads for cancer fighting.

Original languageEnglish (US)
Pages (from-to)839-847
Number of pages9
JournalMedicinal Chemistry Research
Volume23
Issue number2
DOIs
StatePublished - Feb 1 2014

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Antineoplastic Agents
Cells
Derivatives
Cell Line
Inhibitory Concentration 50
Neoplasms
Nuclear magnetic resonance
Molecules
Cytotoxicity
Spectrum analysis
barbituric acid
Chemical analysis
Proton Magnetic Resonance Spectroscopy
Carbon-13 Magnetic Resonance Spectroscopy
N-(2-cyanoethylene)urea

Keywords

  • Barbiturates
  • Cytotoxicity
  • Keywords: Green chemistry

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

Cite this

Design and synthesis of novel nucleobase-based barbiturate derivatives as potential anticancer agents. / Dhorajiya, Bhaveshkumar D.; Ibrahim, Ahmed Salah; Badria, Farid A.; Dholakiya, Bharatkumar Z.

In: Medicinal Chemistry Research, Vol. 23, No. 2, 01.02.2014, p. 839-847.

Research output: Contribution to journalArticle

Dhorajiya, Bhaveshkumar D. ; Ibrahim, Ahmed Salah ; Badria, Farid A. ; Dholakiya, Bharatkumar Z. / Design and synthesis of novel nucleobase-based barbiturate derivatives as potential anticancer agents. In: Medicinal Chemistry Research. 2014 ; Vol. 23, No. 2. pp. 839-847.
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