Literature DB >> 21247401

Synthesis, characterization and in-vitro antiproliferative effects of novel 5-amino pyrazole derivatives against breast cancer cell lines.

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.

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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


  3 in total

1.  Regioselective synthesis and biological studies of novel 1-aryl-3, 5-bis (het) aryl pyrazole derivatives as potential antiproliferative agents.

Authors:  Hanumappa Ananda; Kothanahally S Sharath Kumar; Mayilaadumveettil Nishana; Mahesh Hegde; Mrinal Srivastava; Raghava Byregowda; Bibha Choudhary; Sathees C Raghavan; Kanchugarakoppal S Rangappa
Journal:  Mol Cell Biochem       Date:  2016-11-24       Impact factor: 3.396

2.  Significant in vivo anti-inflammatory activity of Pytren4Q-Mn a superoxide dismutase 2 (SOD2) mimetic scorpiand-like Mn (II) complex.

Authors:  Carolina Serena; Enrique Calvo; Mari Paz Clares; María Luisa Diaz; Javier U Chicote; Raúl Beltrán-Debon; Ramón Fontova; Alejandro Rodriguez; Enrique García-España; Antonio García-España
Journal:  PLoS One       Date:  2015-03-05       Impact factor: 3.240

3.  In vitro and in vivo pharmacodynamics of three novel antileishmanial lead series.

Authors:  M Van den Kerkhof; D Mabille; E Chatelain; C E Mowbray; S Braillard; S Hendrickx; L Maes; G Caljon
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2018-01-31       Impact factor: 4.077

  3 in total

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