1-Thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives as antitumor agents.

Bioorganic & medicinal chemistry letters 2017 Sep 15

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A class of substituted 1-thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives was found to have potent anti-proliferative activity against a broad range of tumor cell lines. A compound from this class (14) was profiled across a broad panel of hematologic and solid tumor cancer cell lines demonstrating cell cycle arrest at the G0/G1 interphase and has potent anti-proliferative activity against a distinct and select set of cancer cell types with no observed effects on normal human cells. An example is the selective inhibition of human B-cell lymphoma cell line (BJAB). Compound 14 was orally bioavailable and tolerated well in mice. Synthesis and structure activity relationships (SAR) in this series of compounds are discussed. Copyright © 2017 Elsevier Ltd. All rights reserved.

Citation

Alan B Cooper, Stephane Ciblat, Gerald Shipps, Jedd Levine, Matthew Kostura, Vibha Oza, Lea Constantineau-Forget, Martin Dery, Chantal Grand-Maitre, Nicolas Bruneau-Latour, Edith Bellavance, Arshad Siddiqui, Michael Luther. 1-Thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives as antitumor agents. Bioorganic & medicinal chemistry letters. 2017 Sep 15;27(18):4471-4477