Synthesis and in vitro antiproliferative activity of novel 1-benzhydrylpiperazine derivatives against human cancer cell lines.
In order to explore the antiproliferative effect associated with the piperazine framework, several 1-benzhydrylpiperazine derivatives 8(a-d), 9(a-d) and 10(a-h) were synthesized. Variation in the functional group at N-terminal of the piperazine led to three sets of compounds, bearing the sulfonyl, amide and thiourea, respectively. Their chemical structures were confirmed by (1)H NMR, LCMS, IR and elemental analysis. The antiproliferative effect of the compounds were evaluated in vitro using the MTT colorimetric method against one normal cell line (NF-103 skin fibroblast cells) and four human cancer cell lines (MCF-7 breast carcinoma cell line, HepG-2 hepatocellular carcinoma cell line, HeLa cervix carcinoma cell line and HT-29 colon carcinoma cell line) for the time period of 24 h. Among the series, four compounds exhibited interesting growth inhibitory effects against all four cell lines.
Ananda Kumar
C S
CS
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570006, Karnataka, India.
Benaka Prasad
S B
SB
Vinaya
K
K
Chandrappa
S
S
Thimmegowda
N R
NR
Kumar
Y C Sunil
YC
Swarup
Sanjay
S
Rangappa
K S
KS
D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D003501:Cyclizine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D013055:Spectrophotometry, Infrared
C029632:norcyclizine; D003501:Cyclizine