Rui Li, Ya-Min Ding, Tian Qin, Xuan-Yi Xue, Wei-Wei Liu, Rong-Bin Wei, Yuan-Fen Zhai, Gang Ding, Da-Hua Shi
{"title":"白屈菜-1,3,5-三嗪衍生物的设计、合成和抗癌活性","authors":"Rui Li, Ya-Min Ding, Tian Qin, Xuan-Yi Xue, Wei-Wei Liu, Rong-Bin Wei, Yuan-Fen Zhai, Gang Ding, Da-Hua Shi","doi":"10.1134/S1068162024050066","DOIUrl":null,"url":null,"abstract":"<p><b>Objective:</b> In search of the better anticancer agents, fifteen bakuchiol-1,3,5-triazine derivatives were designed and synthesized through nucleophilic substitution reaction. <b>Methods:</b> The newly synthesized derivatives were evaluated for their <i>in vitro</i> cytotoxic activity against Panc-1, MDA-MB-231, A549, and UM-UC-3 using the MTT assay. <b>Results and Discussion:</b> The data revealed that all of the bakuchiol-1,3,5-triazine derivatives could inhibit the proliferation of Panc-1 cells. Four compounds exhibited better antiproliferative activities than that of bakuchiol. Among them, compound (<b>IVj</b>) displayed potent antiproliferative activity with IC<sub>50</sub> values of 21.83 μM. Compound (<b>IVj</b>) also showed potent inhibitory activity against the proliferation of MDA-MB-231, A549, and UM-UC-3 cells when compared with bakuchiol. Additionally, compound (<b>IVj</b>) exhibited strong inhibitory effects on the migration, invasion, and adhesion of Panc-1 cells. <b>Conclusions:</b> The results showed that, compound (<b>IVj</b>) could be a promising candidate agent for the treatment of cancer.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 5","pages":"1851 - 1862"},"PeriodicalIF":1.1000,"publicationDate":"2024-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, Synthesis, and Anticancer Activities of Bakuchiol-1,3,5-triazine Derivatives\",\"authors\":\"Rui Li, Ya-Min Ding, Tian Qin, Xuan-Yi Xue, Wei-Wei Liu, Rong-Bin Wei, Yuan-Fen Zhai, Gang Ding, Da-Hua Shi\",\"doi\":\"10.1134/S1068162024050066\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><b>Objective:</b> In search of the better anticancer agents, fifteen bakuchiol-1,3,5-triazine derivatives were designed and synthesized through nucleophilic substitution reaction. <b>Methods:</b> The newly synthesized derivatives were evaluated for their <i>in vitro</i> cytotoxic activity against Panc-1, MDA-MB-231, A549, and UM-UC-3 using the MTT assay. <b>Results and Discussion:</b> The data revealed that all of the bakuchiol-1,3,5-triazine derivatives could inhibit the proliferation of Panc-1 cells. Four compounds exhibited better antiproliferative activities than that of bakuchiol. Among them, compound (<b>IVj</b>) displayed potent antiproliferative activity with IC<sub>50</sub> values of 21.83 μM. Compound (<b>IVj</b>) also showed potent inhibitory activity against the proliferation of MDA-MB-231, A549, and UM-UC-3 cells when compared with bakuchiol. Additionally, compound (<b>IVj</b>) exhibited strong inhibitory effects on the migration, invasion, and adhesion of Panc-1 cells. <b>Conclusions:</b> The results showed that, compound (<b>IVj</b>) could be a promising candidate agent for the treatment of cancer.</p>\",\"PeriodicalId\":758,\"journal\":{\"name\":\"Russian Journal of Bioorganic Chemistry\",\"volume\":\"50 5\",\"pages\":\"1851 - 1862\"},\"PeriodicalIF\":1.1000,\"publicationDate\":\"2024-10-09\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Russian Journal of Bioorganic Chemistry\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://link.springer.com/article/10.1134/S1068162024050066\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Russian Journal of Bioorganic Chemistry","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1134/S1068162024050066","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Design, Synthesis, and Anticancer Activities of Bakuchiol-1,3,5-triazine Derivatives
Objective: In search of the better anticancer agents, fifteen bakuchiol-1,3,5-triazine derivatives were designed and synthesized through nucleophilic substitution reaction. Methods: The newly synthesized derivatives were evaluated for their in vitro cytotoxic activity against Panc-1, MDA-MB-231, A549, and UM-UC-3 using the MTT assay. Results and Discussion: The data revealed that all of the bakuchiol-1,3,5-triazine derivatives could inhibit the proliferation of Panc-1 cells. Four compounds exhibited better antiproliferative activities than that of bakuchiol. Among them, compound (IVj) displayed potent antiproliferative activity with IC50 values of 21.83 μM. Compound (IVj) also showed potent inhibitory activity against the proliferation of MDA-MB-231, A549, and UM-UC-3 cells when compared with bakuchiol. Additionally, compound (IVj) exhibited strong inhibitory effects on the migration, invasion, and adhesion of Panc-1 cells. Conclusions: The results showed that, compound (IVj) could be a promising candidate agent for the treatment of cancer.
期刊介绍：
Russian Journal of Bioorganic Chemistry publishes reviews and original experimental and theoretical studies on the structure, function, structure–activity relationships, and synthesis of biopolymers, such as proteins, nucleic acids, polysaccharides, mixed biopolymers, and their complexes, and low-molecular-weight biologically active compounds (peptides, sugars, lipids, antibiotics, etc.). The journal also covers selected aspects of neuro- and immunochemistry, biotechnology, and ecology.
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