Abstract
ABSTRACT: A new library of different substituted aryl derivatives of isoxazole-pyrazolo[1,5-a]pyrimidine (10a–j) were prepared, confirmed their structures by 1HNMR, 13CNMR and mass spectral data. Furthermore, the preliminary anticancer activities of newly developed compounds (10a–j) were tested against four human cancer cell lines PC3 (prostate), DU-145 (Prostate), A549 (lung) and MCF-7 (breast) by utilizing of MTT method. The obtained results of were compared with standard reference etoposide. Among all, compounds (10a, 10b, 10c, 10e, 10i and 10j) displayed highest anticancer activities than standard. Predominantly, one compound 10a with 3,4,5-trimethoxy substituent on the aryl ring showed excellent activity. The molecular modeling studies indicated the interactions of synthesized compounds with SARM, and DNA via hydrogen bonds and hydrophobic interactions.
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