In the present study, a series of novel substituted pyrazole chalcones and pyrazole oximes (CF 1-15) were synthesized and characterized. Logp values were determined to assess their hydrophobicity. MTT (methyl tetrazolium) assay was performed on A-549 (lung cancer) cell lines. The MTT assay results showed the effect of various substituents on the pyrazole template that could influence their cytotoxic effect. Out of the 15 compounds screened against A-549 cell lines, the compound CF-6 showed appreciable cytotoxicity against the standard doxorubicin.
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In the present review, an attempt has been made to summarize the development of various Tankyrase inhibitors, focussing on Wnt/beta-Catenin pathways along with other cancer targets. The last decade witnessed a plethora of research related to the role of various genetic and epigenetic events that are responsible for the progression of multistage cancers. As a result, the discovery of various signalling pathways responsible for the development of different types of cancers has resulted in the development of molecularly targeted anticancer agents. Out of the many signalling pathways, the Wnt/beta-Catenin pathways have attracted the attention of many research groups owing to their involvement in cell proliferation, role in apoptosis induction, cellular differentiation, and cell migration. The abnormal activation of these pathways has been documented in a variety of tumour cells. Another crucial factor that makes this pathway attractive to the researchers is its direct involvement with poly ADP ribose polymerases. Tankyrases are poly ADP (Adenosine Diphosphate) ribose polymerases that have the capacity to inhibit Wnt/beta-Catenin pathways and become an attractive target for anticancer drugs.
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