PUBLICATIONS

Two chalcone series, including 3,4,5-trimethoxyphenylchalcones and 3,4-dimethoxyphenylchalcones, were synthesized using Claisen-Schmidt condensation. All synthesized compounds were evaluated for their cytotoxic activity against A549. Thirteen chalcones showed potent against A549 with 3,4,5-trimethoxychalcone scaffold (1, 2, 4-11, 13, 15, and 20). New compound 6 was a promising lead compound. Three compounds (7, 10, 14) were docked into the EGFR-TK active site to address the binding site of the chalcone. Molecular docking studies displayed that 7 formed four hydrogen bondings with residues LYS745, GLU762, ASP855, and MET793 and -sulfur interaction as the key responsible for anti-cancer activity. 

Two new quinone derivatives, epoxyquinophomopsins A (1) and B (2), were purified from the EtOAc extract of endophytic fungus Phomopsis sp isolated from Morus cathayana. The structures of both compounds were determined based on 1D and 2D NMR and mass spectral data, as well as by x-ray diffraction analysis for 1. Compounds 1 and 2 were screened against eight receptor- (RTKs) and eight non-receptor tyrosine kinases (nRTKs). Both compounds showed strong inhibitory properties against Bruton’s Tyrosine Kinase (nRTK) with their kinase activity were 19% and 20%, respectively. Only compound 1 that showed strong inhibitory properties against RTKs EGFR and HER-4 with its kinase activity were 16 and 15%, respectively. Thus, both compounds have potential as tyrosine kinase inhibitors.