Minimalist Natural ORPphilin Macarangin B Delineates OSBP Biological Function.

OSBP ligands from the ORPphilin family are chemically complex natural products with promising anticancer properties. Here, we describe macarangin B, a natural racemic flavonoid selective for OSBP, which stands out from other ORPphilins due to its structural simplicity and distinct biological activity. Using a bioinspired strategy, we synthesized both (,,) and (,,)-macarangin B enantiomers, enabling us to study their interaction with OSBP based on their unique optical properties.

1,1'-Diarylethylene as a Key Additive for the Visible Light Synthesis of Bioactive Dihydrobenzo[]phenanthridine Compounds.

This study introduces a straightforward synthetic approach for generating 7,8-dihydrobenzo[]phenanthridine analogs through visible-light-induced cyclization, showing promise as antitumor agents. Unexpectedly, the incorporation of 1,1'-diarylethylene as an additive significantly boosts yield. Through mechanistic investigations, we uncover its crucial role as a trap for the methyl radical formed after the N-O bond cleavage of acetyl oxime, promoting intramolecular cyclization of a nitrogen-centered imine radical.

Design, Synthesis, Computational Studies, and Anti-Proliferative Evaluation of Novel Ethacrynic Acid Derivatives Containing Nitrogen Heterocycle, Urea, and Thiourea Moieties as Anticancer Agents.

In the present work, the synthesis of new ethacrynic acid () derivatives containing nitrogen heterocyclic, urea, or thiourea moieties via efficient and practical synthetic procedures was reported. The synthesised compounds were screened for their anti-proliferative activity against two different cancer cell lines, namely, HL60 (promyelocytic leukaemia) and HCT116 (human colon carcinoma). The results of the in vitro tests reveal that compounds -, , (-), and exhibit potent anti-proliferative activity against the HL60 cell line, with values of the percentage of cell viability ranging from 20 to 35% at 1 μM of the drug and IC values between 2.

Overcoming Solubility Challenges: Liposomal isoCoQ-Carbazole as a Promising Anti-Tumor Agent for Inoperable and Radiation-Insensitive cancers.

This study evaluated the potential of isoCoQ-Carbazole, a diheterocyclic analog of isoCA-4, as an anti-tumor agent. To overcome its low aqueous solubility, liposomes were developed as a delivery system for the compound. In vitro experiments showed that loaded liposomes exhibited similar activity to the free form on multiple human tumor cell lines.

OSMAC Method to Assess Impact of Culture Parameters on Metabolomic Diversity and Biological Activity of Marine-Derived Actinobacteria.

Actinobacteria are known for their production of bioactive specialized metabolites, but they are still under-exploited. This study uses the "One Strain Many Compounds" (OSMAC) method to explore the potential of three preselected marine-derived actinobacteria: (SH-78) and two sp. strains (SH-82 and SH-57).