Pyrazoles (1,2-diazole) are privileged heterocycles in drug discovery. Many pyrazole derivatives have been approved as drugs to treat various kinds of diseases. Two C-arylpyrazoles, Ruxolitinib and Crizotinib, are being used to treat MPN (myeloproliferative neoplasm) and NSCLC (non-small cell lung carcinoma) respectively. Ruxolitinib is a Janus kinase 2 (JK2) inhibitor and Crizotinib behaves as a dual cMet/ALK inhibitor. We have designed and synthesized aldehyde and carboxylic acid functionalized pyrazole derivative as a starting material. In the synthesis, we have used commercially available, inexpensive starting materials, and achieved the target molecules in three steps in an appreciable quantity. Both the functional groups give huge scope to make new derivatives to manipulate the biological activities. Carboxylic acid group further gives the freedom to manipulate clogP values of the synthesized molecules. We have synthesized more than 30 new C-arylpyrazole derivatives so far. After synthesizing 50 molecules, cytotoxic activity against various cell lines will be studied.

Synthesis of pyrazole derivatives as potential cytotoxic agents

249th National Meeting (2015)

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