Zirconium oxide nano-catalyzed bis(indolyl)methanes: A sustainable route to anticancer therapies

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-07 DOI:10.1016/j.bmcl.2025.130132

Komal Rathi , Suryakant Kumar , Bidya Bhushan , Varun Rawat , Ashwani Kumar , Aman Bhardwaj , Anand Prakash , Ved Prakash Verma

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Abstract

Bis(indolyl)methanes (BIMs) are a class of compounds known for their diverse biological activities, including potential anticancer properties. Modern synthetic chemistry techniques are examined in this work to develop and manufacture novel anticancer medications with increased effectiveness and fewer side effects. The cytotoxic efficacy of a moderate and very effective method for creating pharmacologically active BIMs 3a–j using ZrO2 nanoparticles as a catalyst was assessed against the MCF-7 breast cancer cell line. Remarkably, compounds 3a and 3b exhibited exceptional potency, with IC₅₀ values of 0.17 and 0.13 μM, respectively, surpassing the activity of standard anticancer agents sorafenib (IC₅₀: 1.23 μM). Another compound 3j demonstrated moderate inhibition effect with an IC₅₀ value of 8.6 μM. These results highlight the potential of BIMs as promising anticancer agents and warrant further investigation into their mechanism of action and therapeutic applications.

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氧化锆纳米催化吲哚基甲烷：抗癌治疗的可持续途径

双吲哚基甲烷（Bis）是一类以其多种生物活性而闻名的化合物，包括潜在的抗癌特性。在这项工作中，研究了现代合成化学技术，以开发和制造具有更高有效性和更少副作用的新型抗癌药物。利用ZrO2纳米颗粒作为催化剂，对MCF-7乳腺癌细胞系进行了细胞毒性评估，该方法可以产生具有药理活性的BIMs 3a-j。值得注意的是，化合物3a和3b的IC50值分别为0.17和0.13 μM，超过了标准抗癌药物索拉非尼的IC50值（1.23 μM）。另一化合物3j的IC50值为8.6 μM，具有中等抑制作用。这些结果突出了bim作为抗癌药物的潜力，值得进一步研究其作用机制和治疗应用。

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.