Synthesis of some novel benzofuran-2-yl(4,5-dihyro-3,5-substituted diphenylpyrazol-1-yl) methanones and studies on the antiproliferative effects and reversal of multidrug resistance of human MDR1-gene transfected mouse lymphoma cells in vitro

Shrey Parekh, Dhairya Bhavsar, Mahesh Savant, Shailesh Thakrar, Abhay Bavishi, Manisha Parmar, Hardevsinh Vala, Ashish Radadiya, Nilay Pandya, Juliana Serly, J. Molnár, Anamik Shah

Research output: Contribution to journalArticle

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Abstract

A new series of benzofuran-2-yl(4,5-diydro-3,5-substituted diphenylpyrazol-1-yl) methanone derivatives 8a-x by the reaction of the benzofuran-2-carbohydrazides 7 with various chalcone derivatives 3a-x using microwave irradiation has been described. The effect of synthesized compounds 8a-v was studied against human cancer cell lines for their antiproliferative activity and reversal of multidrug resistance on human MDR1-gene transfected mouse lymphoma cells. Among the 24 compounds, the 8c and 8h showed good antiproliferative activity 8b, 8f and 8k were exhibited good MDR reversal activity. The main significance of the process is easy workup process, short reaction time and high yield of the new compounds for biological interest. However, the studies on genetically modified multidrug resistant cancer cells are costly and time consuming.

Original languageEnglish
Pages (from-to)1942-1948
Number of pages7
JournalEuropean Journal of Medicinal Chemistry
Volume46
Issue number5
DOIs
Publication statusPublished - May 2011

Fingerprint

Multiple Drug Resistance
Lymphoma
Genes
Cells
Derivatives
Chalcone
Microwave irradiation
Microwaves
Neoplasms
Cell Line
benzofuran
In Vitro Techniques
carbohydrazide
N-dodecyl-L-lysine amide

Keywords

  • Antiproliferative activity
  • Benzofuran bearing pyrazolines
  • MDR reversal activity
  • Microwave irradiation
  • Mouse lymphoma cells

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

Cite this

Synthesis of some novel benzofuran-2-yl(4,5-dihyro-3,5-substituted diphenylpyrazol-1-yl) methanones and studies on the antiproliferative effects and reversal of multidrug resistance of human MDR1-gene transfected mouse lymphoma cells in vitro. / Parekh, Shrey; Bhavsar, Dhairya; Savant, Mahesh; Thakrar, Shailesh; Bavishi, Abhay; Parmar, Manisha; Vala, Hardevsinh; Radadiya, Ashish; Pandya, Nilay; Serly, Juliana; Molnár, J.; Shah, Anamik.

In: European Journal of Medicinal Chemistry, Vol. 46, No. 5, 05.2011, p. 1942-1948.

Research output: Contribution to journalArticle

Parekh, Shrey ; Bhavsar, Dhairya ; Savant, Mahesh ; Thakrar, Shailesh ; Bavishi, Abhay ; Parmar, Manisha ; Vala, Hardevsinh ; Radadiya, Ashish ; Pandya, Nilay ; Serly, Juliana ; Molnár, J. ; Shah, Anamik. / Synthesis of some novel benzofuran-2-yl(4,5-dihyro-3,5-substituted diphenylpyrazol-1-yl) methanones and studies on the antiproliferative effects and reversal of multidrug resistance of human MDR1-gene transfected mouse lymphoma cells in vitro. In: European Journal of Medicinal Chemistry. 2011 ; Vol. 46, No. 5. pp. 1942-1948.
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