Synthesis and biological screening of new thiadiazolopyrimidine-based polycyclic compounds

Abstract Novel tri-and tetra-cyclic compounds based on the thiadiazolopyrimidine ring system were synthesized, and their antimicrobial activity was estimated. The obtained results evidenced substantial efficiencies of pyrano-thiadiazolopyrimidine 8a–b 9a–b toward two strains gram-positive bacteria ( S. aureus B. cereus ). Besides, tetracyclic pyrazolopyrimido-thiadiazolopyrimidine derivatives 16a–b 17a–b displayed prominent gram-negative E. coli P. aeruginosa In addition, good efficacy C. albicans . antiquorum sensing (anti-QS) inhibition newly synthesized thiadiazolopyrimidine-based violaceum tested, suggesting satisfactory for , 8b, 9a cytotoxic these screened various cancer cell lines (MCF-7, PC3, Hep-2, HepG2) standard normal fibroblast cells (WI38) by utilizing MTT assay. 16a 16b 17a 17b showed potent against MCF-7 with IC 50 values ranging from 5.69 to 9.36 µM. Also, endorsed structural relationship (SAR) inspected provided a correlation between chemical structure anticancer efficiency. in silico docking studies implemented silencing hormonal signaling breast (PDB Code-5NQR). found be consistent activity.