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In search of new potent bioactive compounds, a series of dehydroabietic acid-based thiadiazole-phosphonate compounds were designed and synthesized by the Mannich-type reaction. All target compounds were characterized by Fourier transform infrared, 1H nuclear magnetic resonance (NMR), 13C NMR, 31P NMR, electrospray ionization-mass spectrometry, and UV-vis spectroscopy. The preliminary bioassay experiments showed that, at the concentration of 50 μg ml-1, some of the target compounds exhibited excellent antifungal activity against the five fungi tested, in which several compounds displayed even better antifungal effects than the commercial antifungal drug azoxystrobin, which served as the positive control in this study.

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In an attempt to search for new natural product-based antitumor agents, a series of novel thiazolidinone derivatives of dehydroabietic acid-based B ring-fused-thiazole were designed and synthesized. The primary antitumor tests showed that compounds 5m exhibited almost the best inhibitory activity against the tested cancer cells. The computational study suggested NOTCH1, IGF1R, TLR4, and KDR were the core targets of the title compounds, and the IC 50 of SCC9 and Cal27 is strong correlation with the binding ability of TLR4 and compounds. 5-Fluorouracil 29.4±1.3 18.9±1.4 7.5±0.3 IC 50 values are taken as means standard deviation from three experiments. Computational study Prediction of 5a -5n therapeutic targets in the 3 cancer cell lines About 240 -252 targets in human cells of each compound were obtained by PharmMapper Server, and 145 common targets were found in each group of 5a -5n targets. A total of 660 targets associated with the 3 oral cavity cancer cells lines, were collected by OMIM database and Genecards database after eliminating duplicates. Finally, 16 -19 potential therapeutic targets of each compound were obtained from the intersection of compound targets and the cancer cell lines associated targets. The results are summarized in Supplementary Table S1 -S3.

In an attempt to search for new natural product-based antitumor agents, a series of novel thiazolidinone derivatives of dehydroabietic acid-based B ring-fused-thiazole were designed and synthesized. The primary antitumor tests showed that compounds 5m exhibited almost the best inhibitory activity against the tested cancer cells. The computational study suggested NOTCH1, IGF1R, TLR4, and KDR were the core targets of the title compounds, and the IC50 of SCC9 and Cal27 is strong correlation with the binding ability of TLR4 and compounds.