biostudies-literatureUnknown12(1)Shahedi MA mild and efficient method was developed for the synthesis of new derivatives of thiazolo[3,2-a] pyrimidin-3(2H)-ones from available starting materials based on the oxidation of catechols to ortho-quinone by Myceliophthora thermophila laccase (Novozym 51,003) and 1,4-addition of active methylene carbon to these in situ generated intermediates in moderate to good yields (35-93%). The structure of the products was confirmed through ¹H NMR, ¹³C NMR, HMBC, HSQC, DEPT-135, and mass spectroscopy techniques. These novel compounds were evaluated as active antitumor agents against human colorectal adenocarcinoma and liver adenocarcinoma cell lines. All compounds displayed potent inhibition activities against the HT-29 cell line with IC₅₀ values of 9.8-35.9 µM, supeScientific reports22326https://www.ebi.ac.uk/biostudies/studies/S-EPMC9790884biostudies-literatureDiarylation of thiazolopyrimidines by laccase and their in vitro evaluation as antitumor agents.PMC9790884Habibi ZYousefi MBrask JMohammadi MShahedi MMinaei-Tehrani AShahani RSamadi FYfalseDiarylation of thiazolopyrimidines by laccase and their in vitro evaluation as antitumor agents.A mild and efficient method was developed for the synthesis of new derivatives of thiazolo[3,2-a] pyrimidin-3(2H)-ones from available starting materials based on the oxidation of catechols to ortho-quinone by Myceliophthora thermophila laccase (Novozym 51,003) and 1,4-addition of active methylene carbon to these in situ generated intermediates in moderate to good yields (35-93%). The structure of the products was confirmed through ¹H NMR, ¹³C NMR, HMBC, HSQC, DEPT-135, and mass spectroscopy techniques. These novel compounds were evaluated as active antitumor agents against human colorectal adenocarcinoma and liver adenocarcinoma cell lines. All compounds displayed potent inhibition activities against the HT-29 cell line with IC₅₀ values of 9.8-35.9 µM, supe2022-01-01T00:00:00Z2022 Dec2025-04-22T05:42:29.333Z2024-11-08T13:28:40.187ZS-EPMC97908843656733210.1038/s41598-022-26820-9