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A Conventional Synthesis and Characterization of some Novel Pyrazoles as Cytotoxic Agents


Affiliations
1 Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura, Delhi-Mathura Highway, Chhattikara-281006, (U.P.), India
 

Present work deals with the synthesis, characterization and cytotoxic screening of novel substituted pyrazole derivatives. Different acetophenones (I) with various substituted aromatic aldehydes (II) were condensed into corresponding chalcones (1a-e), which upon bromination gave chalcone dibromides (2a-e). The treatment of 2a-e with hydrazine hydrate, phenylhydrazine and 2,4-dinitrophenylhydrazine in the presence of TEA (triethanolamine) afforded different di and tri-phenyl substituted novel pyrazoles (3a-d and 4a-h). All the newly synthesized compounds were characterized by UV, FTIR, 1H NMR, mass spectral analysis and elemental analysis. All the compounds were screened for anticancer activity against A549 cell line by SRB assay. Compounds 3d, 4b, 4d, 4f and 4h showed promising cytotoxic potential.

Keywords

Cytotoxicity, Chalcone Dibromides, Pyrazole, SRB, Anticancer, A549 Cell Line.
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  • A Conventional Synthesis and Characterization of some Novel Pyrazoles as Cytotoxic Agents

Abstract Views: 276  |  PDF Views: 93

Authors

Dabas Rohit
Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura, Delhi-Mathura Highway, Chhattikara-281006, (U.P.), India
K. S. Hareen
Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura, Delhi-Mathura Highway, Chhattikara-281006, (U.P.), India
Yadav Mithlesh
Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura, Delhi-Mathura Highway, Chhattikara-281006, (U.P.), India
Pathak Devender
Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura, Delhi-Mathura Highway, Chhattikara-281006, (U.P.), India

Abstract


Present work deals with the synthesis, characterization and cytotoxic screening of novel substituted pyrazole derivatives. Different acetophenones (I) with various substituted aromatic aldehydes (II) were condensed into corresponding chalcones (1a-e), which upon bromination gave chalcone dibromides (2a-e). The treatment of 2a-e with hydrazine hydrate, phenylhydrazine and 2,4-dinitrophenylhydrazine in the presence of TEA (triethanolamine) afforded different di and tri-phenyl substituted novel pyrazoles (3a-d and 4a-h). All the newly synthesized compounds were characterized by UV, FTIR, 1H NMR, mass spectral analysis and elemental analysis. All the compounds were screened for anticancer activity against A549 cell line by SRB assay. Compounds 3d, 4b, 4d, 4f and 4h showed promising cytotoxic potential.

Keywords


Cytotoxicity, Chalcone Dibromides, Pyrazole, SRB, Anticancer, A549 Cell Line.