Abstract
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 ((1)HNMR and (13)CNMR). 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 R(1) 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.