Fangzhou Yang, Bin Jia, Hongli Wen, Xiufang Yang, Yangmin Ma
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Antibacterial and Antitumor Activities of Synthesized Sarumine Derivatives.
Our aim in this study was to explain the biological activity of the latest azafluoranthene. The natural product sarumine (12) and its derivatives (13-17) were synthesized and evaluated for their antibacterial and antitumor activities. The synthesis involved a simplified reaction pathway based on biaryl-sulfonamide-protected cyclization, and the compounds were characterized and studied using spectroscopic methods (1HNMR and 13CNMR). Most of the compounds demonstrated improved antibacterial activity. Notably, sarumine demonstrated potent activity against S. aureus and B. subtilis, with an MIC of 8 μg/mL, showing comparable inhibitory effects to the positive control. Furthermore, molecular simulation studies indicated that sarumine exhibited significant binding affinity to FabH. The inhibitory effect of Cl was superior to the others on the structure, and the antitumor activity result also suggested that the inhibitory ability in PC-3 displayed by the R1 derivatives of F and Cl substitutions was better than that of MDA-MB-231. These findings suggest that sarumine and its derivatives may represent new and promising candidates for further study.
期刊介绍：
The International Journal of Molecular Sciences (ISSN 1422-0067) provides an advanced forum for chemistry, molecular physics (chemical physics and physical chemistry) and molecular biology. It publishes research articles, reviews, communications and short notes. Our aim is to encourage scientists to publish their theoretical and experimental results in as much detail as possible. Therefore, there is no restriction on the length of the papers or the number of electronics supplementary files. For articles with computational results, the full experimental details must be provided so that the results can be reproduced. Electronic files regarding the full details of the calculation and experimental procedure, if unable to be published in a normal way, can be deposited as supplementary material (including animated pictures, videos, interactive Excel sheets, software executables and others).
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