V A Kezin, E S Matyugina, S A Surzhikov, M S Novikov, A A Maslova, I L Karpenko, A V Ivanov, S N Kochetkov, A L Khandazhinskaya
{"title":"[5-Arylaminouracil 衍生物的细胞毒性研究]。","authors":"V A Kezin, E S Matyugina, S A Surzhikov, M S Novikov, A A Maslova, I L Karpenko, A V Ivanov, S N Kochetkov, A L Khandazhinskaya","doi":"10.31857/S0026898424020156, EDN: MYDBYJ","DOIUrl":null,"url":null,"abstract":"<p><p>We have previously shown that 5-arylaminouracil derivatives can inhibit HIV-1, herpesviruses, mycobacteria, and other pathogens through various mechanisms. The purpose of this study was to evaluate the potential of 5-arylaminouracils and their derivatives against leukemia, neuroblastoma, and glial brain tumors. 5-Aminouracils with various substituents and their 5'-norcabocyclic and ribo derivatives were screened for cytotoxicity against two neuroblastoma cell lines (SH-SY5Y and IMR-32), K-562 lymphoblastic cells, HL-60 promyeoloblastic cells, and low-passage variants of well-differentiated glioblastoma multiforme (GBM5522 and GBM6138). Cytotoxicity assessment by the standard MTT test showed that most of the compounds lack significant toxicity towards the above cells. However, 5-(4-isopropylphenylamine)uracil and 5-(4-tert-butylphenylamine)uracil exhibited a dose-dependent toxic effect towards the GBM6138 cell line with half-maximal inhibitory concentrations (IC50) of 9 and 2.3 μМ, respectively. Antitumor activity was for the first time demonstrated for compounds of this type and can serve as a starting point for further research.</p>","PeriodicalId":39818,"journal":{"name":"Molekulyarnaya Biologiya","volume":"58 2","pages":"325-332"},"PeriodicalIF":0.0000,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"[Cytotoxicity Studies of 5-Arylaminouracil Derivatives].\",\"authors\":\"V A Kezin, E S Matyugina, S A Surzhikov, M S Novikov, A A Maslova, I L Karpenko, A V Ivanov, S N Kochetkov, A L Khandazhinskaya\",\"doi\":\"10.31857/S0026898424020156, EDN: MYDBYJ\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>We have previously shown that 5-arylaminouracil derivatives can inhibit HIV-1, herpesviruses, mycobacteria, and other pathogens through various mechanisms. The purpose of this study was to evaluate the potential of 5-arylaminouracils and their derivatives against leukemia, neuroblastoma, and glial brain tumors. 5-Aminouracils with various substituents and their 5'-norcabocyclic and ribo derivatives were screened for cytotoxicity against two neuroblastoma cell lines (SH-SY5Y and IMR-32), K-562 lymphoblastic cells, HL-60 promyeoloblastic cells, and low-passage variants of well-differentiated glioblastoma multiforme (GBM5522 and GBM6138). Cytotoxicity assessment by the standard MTT test showed that most of the compounds lack significant toxicity towards the above cells. However, 5-(4-isopropylphenylamine)uracil and 5-(4-tert-butylphenylamine)uracil exhibited a dose-dependent toxic effect towards the GBM6138 cell line with half-maximal inhibitory concentrations (IC50) of 9 and 2.3 μМ, respectively. Antitumor activity was for the first time demonstrated for compounds of this type and can serve as a starting point for further research.</p>\",\"PeriodicalId\":39818,\"journal\":{\"name\":\"Molekulyarnaya Biologiya\",\"volume\":\"58 2\",\"pages\":\"325-332\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-03-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Molekulyarnaya Biologiya\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.31857/S0026898424020156, EDN: MYDBYJ\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Medicine\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molekulyarnaya Biologiya","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.31857/S0026898424020156, EDN: MYDBYJ","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Medicine","Score":null,"Total":0}
[Cytotoxicity Studies of 5-Arylaminouracil Derivatives].
We have previously shown that 5-arylaminouracil derivatives can inhibit HIV-1, herpesviruses, mycobacteria, and other pathogens through various mechanisms. The purpose of this study was to evaluate the potential of 5-arylaminouracils and their derivatives against leukemia, neuroblastoma, and glial brain tumors. 5-Aminouracils with various substituents and their 5'-norcabocyclic and ribo derivatives were screened for cytotoxicity against two neuroblastoma cell lines (SH-SY5Y and IMR-32), K-562 lymphoblastic cells, HL-60 promyeoloblastic cells, and low-passage variants of well-differentiated glioblastoma multiforme (GBM5522 and GBM6138). Cytotoxicity assessment by the standard MTT test showed that most of the compounds lack significant toxicity towards the above cells. However, 5-(4-isopropylphenylamine)uracil and 5-(4-tert-butylphenylamine)uracil exhibited a dose-dependent toxic effect towards the GBM6138 cell line with half-maximal inhibitory concentrations (IC50) of 9 and 2.3 μМ, respectively. Antitumor activity was for the first time demonstrated for compounds of this type and can serve as a starting point for further research.