| Literature DB >> 21247401 |
Hanumegowda Raju1, Siddappa Chandrappa, Doddakunche S Prasanna, Hanumappa Ananda, Tandaga S Nagamani, Sonnahallipura M Byregowda, Kanchugarakoppal S Rangappa.
Abstract
In search of synthetic chemotherapeutic substances capable of inhibiting, retarding, or reversing the process of multistage carcinogenesis, we synthesised a series of novel 1-(4-methoxybenzyl)-3-cyclopropyl-1H-pyrazol-5-amine derivatives 9(a-h) by a nucleophilic substitution reaction and characterized by (1)H and (13)C nuclear magnetic resonance (NMR), liquid chromatography mass spectrometry (LC/MS), Fourier-transform infrared (FTIR), and elemental analysis. These novel compounds were evaluated for their efficacy in inhibiting VERO normal and MCF-7 breast cancer cells proliferation by trypan blue exclusion assay, MTT assay, [(3)H] thymidine incorporation assay and DNA fragmentation analysis. Among the series, some compounds exhibited interesting growth inhibitory effects against cell lines. From the Structure-Activity Relationship studies, it has been revealed that, both novel patented compounds and therapeutic protocols of N-terminal pyrazole ring structures play key role in the antiproliferative activity.Entities:
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Year: 2011 PMID: 21247401 DOI: 10.2174/157489211795328459
Source DB: PubMed Journal: Recent Pat Anticancer Drug Discov ISSN: 1574-8928 Impact factor: 4.169