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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
chemistry
Synthesis of novel 1,3,4-trisubstituted pyrazole derivatives and their evaluation as antitumor and antiangiogenic agents
Chemical and Pharmaceutical Bulletin, Volume 51, No. 7, Year 2003
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Description
Several 1,3,4-trisubstituted pyrazole derivatives were synthesized and screened for their cytotoxic effect in a primary 3 tumor cell line test at 10-4 M drug concentration. Compounds 19 and 20 reduced the growth of one or more of these cell lines to less than 32% and escalated up to evaluation in the full panel of 60 human tumor cell lines at a minimum of 5 concentrations at 10 fold dilutions. Compound N′-(1-{1-[4-nitrophenyl]-3-phenyl-1H- pyrazol-4-yl}methylene)-2-chlorobenzohydrazide 19 proved to be the most active of these derivatives with full panel median growth inhibition (GI50), total growth concentration (TGI) and median lethal concentration (LC 50) mean graph mid-point (MG-MID) of 3.79, 12.5 and 51.5 μM, respectively. In addition, compounds 19, 39, 40, 41, 43, 45, 47 were tested for their antiangiogenic properties by testing their ability to inhibit human umbilical vein endothelial cells (HUVECs) proliferation, cord formation and migration in response to chemoattractant. 3-Acetyl-2-(1-(4-nitrophenyl)-3- phenylpyrazol-4-yl)-5-(4-pyridyl)-1,3,4-oxadiazoline 39 showed significant antiangiogenic profile at non-cytotoxic doses, with HUVEC proliferation inhibition IC50 of 7.60 μM, chemotaxis IC50 of 0.86 μM and was superior to the reference celecoxib 2 in both tests. Furthermore, in contrary to the references TNP-470 and celecoxib, all the tested compounds interfered with the migratory function of HUVECs in response to vascular endothelium growth factor (VEGF) rather than the endothelial cells proliferation. © 2003 Pharmaceutical Society of Japan.
Authors & Co-Authors
Abadi, Ashraf Hassan
Egypt, Cairo
Faculty of Pharmacy
Eissa, Amal Abdel Haleem Mohamed
Egypt, Cairo
Faculty of Pharmacy
Hassan, Ghaneya Sayed
Egypt, Cairo
Faculty of Pharmacy
Statistics
Citations: 201
Authors: 3
Affiliations: 1
Identifiers
Doi:
10.1248/cpb.51.838
ISSN:
00092363
e-ISSN:
13475223
Research Areas
Cancer