{"title":"7-(取代氨基)-5-甲硫基唑并[1,5-a]嘧啶：合成、体外细胞毒性和分子对接","authors":"","doi":"10.1016/j.tetlet.2024.155324","DOIUrl":null,"url":null,"abstract":"<div><div>A method for the synthesis of new 7-(substituted amino)-5-methylthioazolo[1,5-<em>a</em>]pyrimidines has been developed. Based on the MTT test, IC<sub>50</sub> values were calculated for the obtained compounds against lung carcinoma (A549), liver carcinoma (HepG2), embryonal rhabdomyosarcoma (Rd) and human embryonic kidney (HEK 293) cell lines. Some compounds from the series demonstrated activity close to the reference drug, but with a certain selectivity. Based on the results of MTT assay and molecular docking studies for the catalytic subunits of PI3K, two isoforms (PI3Kβ and PI3Kδ) were assumed as the targets for the new series of azolo[1,5-<em>a</em>]pyrimidines with cytotoxic effect on the rhabdomyosarcoma cell line.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":null,"pages":null},"PeriodicalIF":1.5000,"publicationDate":"2024-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"7-(Substituted amino)-5-methylthioazolo[1,5-a]pyrimidines: Synthesis, cytotoxic properties in vitro and molecular docking\",\"authors\":\"\",\"doi\":\"10.1016/j.tetlet.2024.155324\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>A method for the synthesis of new 7-(substituted amino)-5-methylthioazolo[1,5-<em>a</em>]pyrimidines has been developed. Based on the MTT test, IC<sub>50</sub> values were calculated for the obtained compounds against lung carcinoma (A549), liver carcinoma (HepG2), embryonal rhabdomyosarcoma (Rd) and human embryonic kidney (HEK 293) cell lines. Some compounds from the series demonstrated activity close to the reference drug, but with a certain selectivity. Based on the results of MTT assay and molecular docking studies for the catalytic subunits of PI3K, two isoforms (PI3Kβ and PI3Kδ) were assumed as the targets for the new series of azolo[1,5-<em>a</em>]pyrimidines with cytotoxic effect on the rhabdomyosarcoma cell line.</div></div>\",\"PeriodicalId\":438,\"journal\":{\"name\":\"Tetrahedron Letters\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.5000,\"publicationDate\":\"2024-10-14\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Tetrahedron Letters\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0040403924004192\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, ORGANIC\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Tetrahedron Letters","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0040403924004192","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
7-(Substituted amino)-5-methylthioazolo[1,5-a]pyrimidines: Synthesis, cytotoxic properties in vitro and molecular docking
A method for the synthesis of new 7-(substituted amino)-5-methylthioazolo[1,5-a]pyrimidines has been developed. Based on the MTT test, IC50 values were calculated for the obtained compounds against lung carcinoma (A549), liver carcinoma (HepG2), embryonal rhabdomyosarcoma (Rd) and human embryonic kidney (HEK 293) cell lines. Some compounds from the series demonstrated activity close to the reference drug, but with a certain selectivity. Based on the results of MTT assay and molecular docking studies for the catalytic subunits of PI3K, two isoforms (PI3Kβ and PI3Kδ) were assumed as the targets for the new series of azolo[1,5-a]pyrimidines with cytotoxic effect on the rhabdomyosarcoma cell line.
期刊介绍：
Tetrahedron Letters provides maximum dissemination of outstanding developments in organic chemistry. The journal is published weekly and covers developments in techniques, structures, methods and conclusions in experimental and theoretical organic chemistry. Rapid publication of timely and significant research results enables researchers from all over the world to transmit quickly their new contributions to large, international audiences.
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