Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Synthesis and Anticancer Activity of 3a,4-dihydro-3H-indeno[1, 2-c]pyrazole-2-carboxamide Analogues

Author(s): Mohamed Jawed Ahsan.


A series of 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues were synthesized and characterized by IR, NMR and elemental analysis. All the compounds were screened for anticancer activity as per National Cancer Institute (NCI US) Protocol on leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate and breast cancers cell lines. The compound 3-(4-fluorophenyl)-N-(2,6-dimethylphenyl)-6,7- dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide (4h) was found to be the most active compound of the series highly active on Leukemia K-562 and SR cell line [Growth Percent (GP) = 26.95 and 33.45 respectively]. The molecular docking mode for compound, 3-(4-Fluorophenyl)-N-(2,6-dimethylphenyl)-6,7-dimethoxy-3a,4-dihydro-3Hindeno[ 1,2-c]pyrazole-2-carboxamide (4h) showed efficient binding with EGFR tyrosine kinase.

Keywords: Antitumor activity, Claisen Schmidt condensation, Molecular docking, Pyrazolines, Tyrosine kinase

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Article Details

Year: 2012
Page: [823 - 827]
Pages: 5
DOI: 10.2174/157018012803307996
Price: $58