TITLE:
Synthesis, Characterization and Anti-Angiogenic Effects of Novel 5-Amino Pyrazole Derivatives on Ehrlich Ascites Tumor [EAT] Cells in-Vivo
AUTHORS:
H. Raju, S. Chandrappa, M. K. Ramakrishna, T. S. Nagamani, H. Ananda, S. M. Byregowda, K. S. Rangappa
KEYWORDS:
1H-Pyrazol, Aryl Isothiocyanates, Ehrlich Ascites Tumor [EAT] Cells, Anti-Angiogenesis
JOURNAL NAME:
Journal of Cancer Therapy,
Vol.1 No.1,
March
24,
2010
ABSTRACT: In search of synthetic chemotherapeutic
substances capable of inhibiting, retarding, or reversing the process of
multi-stage carcinogenesis, we synthesized a series of novel 5-amino pyrazole
derivatives 11(a-h) by a nucleophilic substitution reaction and characterized
by 1H 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 Ehrlich ascites tumor
[EAT] cells in-vivo. In the present study we designed, synthesized, characterized and
investigate the anti-angiogenic effects of these compounds, on Ehrlich ascites
tumor [EAT] cells in-vivo. The compounds were subsequently tested for their
ability to inhibit neovascularisation in chorio allantoin membrane (CAM) model.
From the Structure Activity Relationship (SAR) studies, it reveals that, the
substitution at N-terminal in pyrazole ring plays key role in the antitumor and
anti-angiogenic effects.