新型哌啶-查尔酮类衍生物的设计、合成及抗宫颈癌和逆转顺铂耐药活性

本文采用活性亚结构拼接原理，设计并合成了15个新型含哌啶的查尔酮类衍生物，利用¹H NMR、¹³C NMR和HR-MS对结构进行表征，并初步评价了其抗宫颈癌和抗顺铂耐药宫颈癌活性作用。结果表明，化合物6g具有一定的抗肿瘤活性和逆转顺铂耐药作用；并采用Elisa法、联合顺铂用药、Western Blot和分子对接对化合物6g与VEGFR-2和P-gp靶点进行了初步的研究。本研究为基于VEGFR-2和P-gp双靶点新型分子靶向查尔酮类衍生物的设计提供了一条思路。

Design, synthesis and anti-cervical cancer and reversal of cisplatin resistance activity of novel piperidine-chalcone derivatives

In this paper, 15 novel piperidine-containing chalcone derivatives were designed and synthesized using the active substructure splicing principle, and their structures were characterized by 1H-NMR, 13C-NMR and HR-MS, and their anti-cervical cancer and anti-cisplatin-resistant cervical cancer active effects were preliminarily evaluated. The results showed that compound 6g has some antitumor activity and reversal of cisplatin resistance, and preliminary studies of compound 6g with VEGFR-2 and P-gp targets were performed using Elisa assay, co-dosing with cisplatin, Western Blot and molecular docking. This study provides an idea for the design of novel molecularly targeted chalcone derivatives based on the dual targets of VEGFR-2 and P-gp.