Six new highly oxygenated chloroazaphilone derivatives, isochromophilones A-F (1-6), were obtained from the mangrove-derived fungus Diaporthe sp. SCSIO 41011, together with six known analogues (7-12). The structures of 1-6 including absolute configurations were determined by detailed NMR, MS spectroscopic analyses, and electronic circular dichroism spectra. Compounds 1 and 2 represent the first reported azaphilones lacking a carbonyl group at C-6. Compound 8 exhibited cytotoxic activities against three renal carcinoma cell lines, ACHN, OS-RC-2, and 786-O cells, with IC values ranging from 3.0 to 4.4 μM, and 4 showed activity against 786-O cells with an IC of 8.9 μM. Further studies indicated that 4 induced apoptosis in 786-O cells in a dose- and time-dependent manner.

Recent advances in the chemistry and biology of structurally diverse azaphilones from 2012 to 2019.

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Four novel 1-oxa-8,10-diazaspiro[5.5]undecane containing diketopiperazine alkaloids from Aspergillus versicolor SCSIO 41016.

Eleven diketopiperazine and fumiquinazoline alkaloids (1-11) together with a tetracyclic triterpenoid helvolic acid (12) were obtained from the cultures of a deep-sea derived fungus Aspergillus sp. SCSIO Ind09F01. The structures of these compounds (1-12) were determined mainly by the extensive NMR, ESIMS spectra data and by comparison with previously described compounds. Besides, anti-tuberculosis, cytotoxic, antibacterial, COX-2 inhibitory and antiviral activities of these compounds were evaluated. Gliotoxin (3), 12,13-dihydroxy-fumitremorgin C (11) and helvolic acid (12) exhibited very strong anti-tuberculosis activity towards Mycobacterium tuberculosis with the prominent MIC values of <0.03, 2.41 and 0.894 μM, respectively, which was here reported for the first time. Meanwhile gliotoxin also displayed significant selective cytotoxicities against K562, A549 and Huh-7 cell lines with the IC values of 0.191, 0.015 and 95.4 μM, respectively.