Indole diketopiperazine-based hybrids with dual TDP1 and TDP2 inhibitory activities from marine fungus aspergillus
Xia Wei1, Yi Huang2, Zheng-Wu Luo3
1Guangxi Key Laboratory of Bioactive Molecules Research and Evaluation, School of Pharmaceutical Sciences, Guangxi Medical University, Nanning 530021, China; School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
Abstract:
Seven indole diketopiperazine-based hybrids, including four new compounds (1-4) and three known ones (5-7), were successfully isolated from the fungus Aspergillus sp. EGF 15-0-3. Comprehensive spectroscopic analyses, combined with single-crystal X-ray diffraction and electronic circular dichroism calculations, were employed to elucidate their structures, relative configurations, and absolute configurations. Biological evaluation revealed that all obtained compounds except 2 exhibited potential TDP1 inhibitory activity. Notably, compound 3 demonstrated unique dual inhibitory effects against both TDP1 and TDP2, highlighting its promising therapeutic potential.
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