Abstract

Natural products based novel crown ethers have been prepared by employing biologically active natural structures including tetrahydroisoquinoline, chrysin and biochanin-A as the side arms. The resulting crown scaffolds were evaluated for their anticancer potential against two cancer cell lines i.e. NCI-H460 (non-small lung carcinoma), MCF-7 (breast adenocarcinoma). The comparative study showed that the addition of crown scaffold put marked effects on antiproliferative profile of parent natural precursors and is significant for lung carcinoma in particular. Biochanin-A derived crown ether showed three (03) folds higher antiproliferative activity (IC₅₀ = 6.08 ± 0.07 µM) against lung carcinoma as compared to standard drug cisplatin (IC₅₀ = 19.00 ± 1.24 µM). Cytotoxic trends for NIH-3T3 cell lines were also examined and found reduced as compared to parent natural structures. Hence, these findings could open a new pathway towards developing effective carcinostatic drugs.

• HIGHLIGHTS

• Four natural products based novel crown ethers have been developed.

• Comparative antiproliferative screening of crown ethers and natural precursors.

• Addition of crown showed marked effects on anticancer profile of natural products.

• Crown formation is significant for lung carcinoma potential in particular.

• Biochanin-A derived crown ether found three folds more active than standard drug.

摘要

通过采用具有生物活性的天然结构，包括四氢异喹啉、白杨素和 biochanin-A 作为侧臂，制备了基于天然产物的新型冠醚。评估了所得冠支架对两种癌细胞系即 NCI-H460（非小肺癌）、MCF-7（乳腺癌）的抗癌潜力。比较研究表明，添加冠支架对亲本天然前体的抗增殖作用显着，尤其是对肺癌具有重要意义。_与标准药物顺铂 ( IC ₅₀= 19.00 ± 1.24 µM）。还检查了 NIH-3T3 细胞系的细胞毒性趋势，发现与亲本天然结构相比减少了。因此，这些发现可能为开发有效的抗癌药物开辟了一条新途径。

• 强调

• 已开发出四种基于天然产物的新型冠醚。

• 冠醚和天然前体的比较抗增殖筛选。

• 添加冠对天然产物的抗癌谱显示出显着效果。

• 冠的形成对于肺癌的可能性尤其重要。

• Biochanin-A 衍生的冠醚发现比标准药物活性高三倍。