6:2 FTI [F(CF 2 ) 6 CH 2 CH 2 I] is a principal industrial raw material used to manufacture 6:2 FTOH [F(CF 2 ) 6 CH 2 CH 2 OH] and 6:2 FTOH-based products and could enter aerobic environments from possible industrial emissions where it is manufactured. This is the first study to assess 6:2 FTI aerobic soil biotransformation, quantify transformation products, and elucidate its biotransformation pathways. 6:2 FTI biotransformation led to 6:2 FTOH as a key intermediate, which was subsequently biotransformed to other significant transformation products, including PFPeA [F-(CF 2 ) 4 COOH, 20 mol % at day 91], 5:3 acid [F-(CF 2 ) 5 CH 2 CH 2 COOH, 16 mol %], PFHxA [F(CF 2 ) 5 COOH, 3.8 mol %], and 4:3 acid [F(CF 2 ) 4 CH 2 CH 2 COOH, 3.0 mol %]. 6:2 FTI biotransformation also led to a significant level of PFHpA [F(CF 2 ) 6 COOH, 16 mol % at day 91], perhaps via another putative intermediate, 6:2 FTUI [F(CF 2 ) 6 CHCHI],whose molecular identity and further biotransformation were not verified because of the lack of an authentic standard. Total recovery of the aforementioned per-and polyfluorocarboxylates accounted for 59 mol % of initially applied 6:2 FTI by day 91, in comparison to 56 mol % when soil was dosed with 6:2 FTOH, which did not lead to PFHpA. Thus, were 6:2 FTI to be released from its manufacture and undergo soil microbial biotransformation, it could form PFPeA, PFHpA, PFHxA, 5:3 acid, and 4:3 acid in the environment.

Protein kinases are validated drug targets for a number of therapeutic areas, as kinase deregulation is known to play an essential role in many disease states. Many investigated protein kinase inhibitors are natural product small molecules or their derivatives. Many marine-derived natural products from various marine sources, such as bacteria and cyanobacteria, fungi, animals, algae, soft corals, sponges, etc. have been found to have potent kinase inhibitory activity, or desirable pharmacophores for further development. This review covers the new compounds reported from the beginning of 2014 through the middle of 2019 as having been isolated from marine organisms and having potential therapeutic applications due to kinase inhibitory and associated bioactivities. Moreover, some existing clinical drugs based on marine-derived natural product scaffolds are also discussed.

The application of an OSMAC (One Strain-Many Compounds) approach on the sponge-derived fungus Aspergillus sp. LS34, using two different media including solid rice medium and potato dextrose broth (PDB) resulted in the isolation and identification of two new compounds, named asperspin A (1) and asperther A (2) along with seven known compounds 3–9. Compounds 1–5 were detected in fungal extracts from rice medium, while compounds 6–9 were isolated from PDB medium. Their structures were unambiguously characterized by HRESIMS and NMR spectroscopic data. The growth inhibitory activity of these compounds against four pathogenic bacteria (Vibrio parahaemolyticus, Vibrio harveyi, Escherichia coli, and Staphylococcus aureus) were evaluated. All the compounds were also tested for their cytotoxicity against seven cancer cell lines, including CCRF-CEM, K562, BGC823, AGS, HCT-116, MDA-MB-453, and COR-L23. Among them, compound 9 showed strong activity against CCRF-CEM and K562 cells with IC50 values of 1.22 ± 0.05 µM and 10.58 ± 0.19 µM, respectively. Notably, compound 7 also showed pronounced activity against S. aureus with an MIC value of 3.54 µM.

Topoisomerase (Topo) and histone deacetylase (HDAC) are considered to be effective targets for the treatment of cancer. In this study, 16 new N‐(2‐aminophenyl)benzamide acridine analogues (8 a‐8 p) were designed and synthesized as Topo I and subtype‐selective HDAC inhibitors. Most of the compounds displayed good antiproliferative activity against CCRF‐CEM, K562 and U937 cells. Among them, 8 a demonstrated the highest anti‐proliferative activity (IC50=0.12‐0.35 μM). Further studies showed that 8 a and some analogues displayed Topo I inhibitory activity and exhibited selective inhibition for HDAC1 (class I HDAC). Additionally, 8 a can significantly induce DNA damage and histone H3 acetylation in these tested cancer cells. Moreover, 8 a triggered dose‐dependent G0/G1 cell cycle arrest and induced cellular apoptosis. This study provides new perspectives for the further structural optimization of N‐(2‐aminophenyl)benzamide acridine analogues for use in cancer research.

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Cycloabiesesquine A, representing a unique carbon skeleton among the sesquiterpenoids, was isolated from Abies delavayi and by extensive spectroscopic and computational methods, its structure was elucidated as (7S,8R,12R)-4,8-dihydroxy-1,3,5,10-tetraen-8,12-cyclobisabolan-9-one.

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