Victor P. Kislyi , Anna S. Maksimenko , Aida I. Samigullina , Marina N. Semenova , Victor V. Semenov
{"title":"强效抗癌剂 4-(4-甲氧基苯基)-3-(3,4,5-三甲氧基苯基)异噁唑的合成和 X 射线结构","authors":"Victor P. Kislyi , Anna S. Maksimenko , Aida I. Samigullina , Marina N. Semenova , Victor V. Semenov","doi":"10.1016/j.mencom.2024.06.013","DOIUrl":null,"url":null,"abstract":"<div><p>The three-step synthesis of potent anticancer 4-(4-methoxy- phenyl)-3-(3,4,5-trimethoxyphenyl)isoxazole starting from 1,2,3-trimethoxy-5-(nitromethyl)benzene and anisaldehyde was developed. In phenotypic sea urchin embryo assay, this compound exhibited antimitotic antitubulin activity comparable to that of the natural cytostatic combretastatin A4 (CA4). The title isoxazole inhibited <em>in vitro</em> growth of A549 human lung cancer cells and PC-3 human prostate cancer cells with IC<sub>50</sub> values of 8 and 6 nm, respectively, exceeding the effect of CA4.</p></div>","PeriodicalId":18542,"journal":{"name":"Mendeleev Communications","volume":"34 4","pages":"Pages 511-513"},"PeriodicalIF":1.8000,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and X-ray structure of potent anticancer 4-(4-methoxyphenyl)-3-(3,4,5-trimethoxyphenyl)isoxazole\",\"authors\":\"Victor P. Kislyi , Anna S. Maksimenko , Aida I. Samigullina , Marina N. Semenova , Victor V. Semenov\",\"doi\":\"10.1016/j.mencom.2024.06.013\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The three-step synthesis of potent anticancer 4-(4-methoxy- phenyl)-3-(3,4,5-trimethoxyphenyl)isoxazole starting from 1,2,3-trimethoxy-5-(nitromethyl)benzene and anisaldehyde was developed. In phenotypic sea urchin embryo assay, this compound exhibited antimitotic antitubulin activity comparable to that of the natural cytostatic combretastatin A4 (CA4). The title isoxazole inhibited <em>in vitro</em> growth of A549 human lung cancer cells and PC-3 human prostate cancer cells with IC<sub>50</sub> values of 8 and 6 nm, respectively, exceeding the effect of CA4.</p></div>\",\"PeriodicalId\":18542,\"journal\":{\"name\":\"Mendeleev Communications\",\"volume\":\"34 4\",\"pages\":\"Pages 511-513\"},\"PeriodicalIF\":1.8000,\"publicationDate\":\"2024-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Mendeleev Communications\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0959943624001901\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Mendeleev Communications","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0959943624001901","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Synthesis and X-ray structure of potent anticancer 4-(4-methoxyphenyl)-3-(3,4,5-trimethoxyphenyl)isoxazole
The three-step synthesis of potent anticancer 4-(4-methoxy- phenyl)-3-(3,4,5-trimethoxyphenyl)isoxazole starting from 1,2,3-trimethoxy-5-(nitromethyl)benzene and anisaldehyde was developed. In phenotypic sea urchin embryo assay, this compound exhibited antimitotic antitubulin activity comparable to that of the natural cytostatic combretastatin A4 (CA4). The title isoxazole inhibited in vitro growth of A549 human lung cancer cells and PC-3 human prostate cancer cells with IC50 values of 8 and 6 nm, respectively, exceeding the effect of CA4.
期刊介绍：
Mendeleev Communications is the journal of the Russian Academy of Sciences, launched jointly by the Academy of Sciences of the USSR and the Royal Society of Chemistry (United Kingdom) in 1991. Starting from 1st January 2007, Elsevier is the new publishing partner of Mendeleev Communications.
Mendeleev Communications publishes short communications in chemistry. The journal primarily features papers from the Russian Federation and the other states of the former USSR. However, it also includes papers by authors from other parts of the world. Mendeleev Communications is not a translated journal, but instead is published directly in English. The International Editorial Board is composed of eminent scientists who provide advice on refereeing policy.
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