article · Future Medicinal Chemistry
<b>Aim:</b> The structural optimization of our recently reported CDK9 inhibitor to furnish novel aminopyrazolones and methylpyrazolones with improved pharmacokinetics.<b>Materials & methods:</b> The synthesis of the targeted compounds was accomplished via conventional, grinding and microwave-assisted processes. The cytotoxicity of them was assayed against three carcinomas.<b>Results:</b> Analogs <b>2</b>, <b>4</b> and <b>6</b> showed significant cytotoxicity and selectivity toward all tested cells. They also displayed potent CDK9 inhibition. Compound <b>6</b> arrested MCF-7 cycle at G2/M phase by stimulating the apoptotic pathway. The <i>in vivo</i> biodistribution of radiolabeled compound <b>6</b> displayed a potent targeting capability of <sup>131</sup>I in solid tumors.<b>Conclusion:</b> Entity <b>6</b> is a potent CDK9 inhibitor where <sup>131</sup>I-compound <b>6</b> can be used as a significant radiopharmaceutical imaging tool for tumors.
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DOI: 10.1080/17568919.2024.2419363
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