Synthesis and Studies on Some New Fluorine Containing Hydroxypyrazolines and 1H Pyrazoles-as Possible Antiproliferative Agents

A series of twenty four newly synthesized 1-aroyl-3-aryl-5-hydroxy-5-(2,4-dichloro-5-fluorophenyl) pyrazolines (3) and 1H-3-aryl-5-hydroxy-5-(2,4-dichloro-5-fluorophenyl)-pyrazoles (6) were tested for cytostatic and cytotoxic effects on in a primary three cell line-one dose anticancer assay against...

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Bibliographic Details
Published in:Journal of pharmacology & toxicology 2008, Vol.3 (2), p.102-110
Main Authors: Rao, B. Sooryanarayana, ., P.M. Akberali, ., B. Shivarama Holla, ., B.K. Sarojini
Format: Article
Language:English
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Summary:A series of twenty four newly synthesized 1-aroyl-3-aryl-5-hydroxy-5-(2,4-dichloro-5-fluorophenyl) pyrazolines (3) and 1H-3-aryl-5-hydroxy-5-(2,4-dichloro-5-fluorophenyl)-pyrazoles (6) were tested for cytostatic and cytotoxic effects on in a primary three cell line-one dose anticancer assay against NCI-H 460 (Lung), MCF 7(Breast) and SF 268 (CNS). Proliferation of these cancer cell lines was strongly inhibited by eleven compounds. These eleven compounds were then passed on for evaluation in the full panel of 60 cell lines derived from seven cancer types namely, Lung, Colon, Melanoma, Renal, Ovarian, CNS and Leukemia. These compounds showed antiproliferative activity on the whole cell panel. Compound 1H-pyrazole, 6d [3,4-methylenedioxy at C 3] showed highest activity with Growth Inhibition (GI sub(50)) value 100 mu M for almost all the tested cell lines. The Total Growth Inhibition (TGI) and Lethal Concentration (LC sub(50)) values for the most active compound [6d] found to be >100 mu M for Leukemia cell lines and for the other cell lines these values remain
ISSN:1816-496X
DOI:10.3923/jpt.2008.102.110