Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: lddd@benthamscience.org

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Library of Synthetic Compounds Based on Pyrazole Unit: Design and Screening Against Breast and Colorectal Cancer

Author(s): Farid Abrigach, Mohamed Khoutoul, Noureddine Benchat, Smaail Radi, Nihed Draoui, Olivier Feron, Olivier Riant and Rachid Touzani

Affiliation: Faculte Pluridisciplinaire de Nador, Universite Mohammed Premier, BP: 300, Selouane 62700, Nador, Moroccoe

Keywords: Anti-cancer, LOVO, MDA-MB231, MTT assay, Normoxie conditions and drug design, Pyrazole.

Graphical Abstract:


Abstract:

Pyrazolic compounds represent a large source of anticancer compounds, based on the choice of the scaffold structure, the nature of the substituents and the sites of coordination. Here, we discuss our recent progresses in identifying new active molecules from a synthetic library of 14 nitrogen compounds. All these compounds exert antiproliferative activity against breast and colorectal cancer cell lines with varying IC50 values (the half-maximal inhibitory concentration, which is a measure of the effectiveness of a compound in inhibiting biological or biochemical function). We found a onelog order difference in activity among the different tested compounds. The most active compound 7 showed an IC50 values equal to 8.5µg/ml in both MDA-MB 231(breast cancer) and LOVO (colorectal cancer) cell lines.

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Article Details

VOLUME: 11
ISSUE: 8
Page: [1010 - 1016]
Pages: 7
DOI: 10.2174/1570180811666140512220842