Synthesis and evaluation of benzoylbenzofurans and isoflavone derivatives as sirtuin 1 inhibitors with antiproliferative effects on cancer cells.

Isoflavone derivatives were prepared from benzoylbenzofuran precursors. The synthesized compounds were analyzed by 1D and 2D nuclear magnetic resonance (NMR) spectroscopy, as well as high-resolution mass spectrometry (HRMS) to confirm their structures. The benzoylbenzofuran and isoflavone analogues were evaluated for inhibition of sirtuin 1 (SIRT1) and cell proliferation in MDA-MB-231 triple-negative breast cancer (TNBC) cells.

Phytochemical Profiling and Isolation of Bioactive Compounds from (Rosaceae).

In the study, ultraperformance liquid chromatography-quadrupole time-of-flight-mass spectrometry analysis of leaf and stem extracts led to the identification of various classes of compounds. Further chromatographic purifications resulted in the isolation of 22 compounds that consisted of a new triterpenoid named leucosidic acid A (), an acetophenone derivative , a phloroglucinol derivative , three chromones , seven pentacyclic triterpenoids , a phytosterol glucoside , a flavonoid , and seven flavonoid glycosides . Nineteen of these compounds including the previously undescribed triterpenoid are isolated for the first time from .

Synthesis, anti-microbial, toxicity and molecular docking studies of N-nitroso-N-phenylhydroxylamine (cupferron) and its derivatives.

Bacterial resistance to antimicrobial agents is increasing at an alarming rate globally and requires new lead compounds for antibiotics. In this study, N-phenyl-N-nitroso hydroxylamine (cupferron) and its derivatives have been synthesised using readily available starting materials. The compounds were obtained in high yield and purity.

Flavonoids from the Genus Isolation, Structure, Pharmacological Activities and Structure-Activity Relationships.

Plants of the genus are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure-activity relationship of flavonoids for the period covering 2000-2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells.

Synthesis and Antifungal Activity of Chromones and Benzoxepines from the Leaves of .

This study reports the first total synthesis of the bioactive oxepinochromones 12--acetyleranthin () (angular isomer) and 12--acetylptaeroxylinol () (linear isomer). The antifungal activity of these compounds and their derivatives was determined against and . Most compounds had good selectivity between the two fungi and showed moderate to good activity.

Bioactive Lignans from .

Phytochemical investigation of extracts of the stems of led to the isolation of nine lignans that included four known compounds, namely, hinokinin (), savinin (), medioresinol (), and two cubebins (,), three new butyrolactone lignans (-), and butyrolactol lignans -. The structures of the new compounds were established using 1D and 2D NMR and HRESIMS data. The absolute configurations of the new lignans were determined from their ECD data and the Mosher's ester method.

Synthesis of Isoflavones by Tandem Demethylation and Ring-Opening/Cyclization of Methoxybenzoylbenzofurans.

The unexpected conversion of benzoylbenzofurans into isoflavones through an intramolecular cascade that involves deprotection and ring-opening/cyclization is described. This was discovered in an investigation of the possible transformation of benzoylbenzofurans into coumaronochromones. This route affords isoflavones in two major steps from acetophenones and benzoquinones.

Carbon-14 radiolabeling and tissue distribution evaluation of MMV390048.

The antimalarial compound MMV390048 ([ C]-11) was labeled with carbon-14 isotope via a 3-step synthesis. It was obtained in a 15.5% radiochemical overall yield from carbon-14 labeled methyl iodide with a radiochemical purity of >99%.

Carbon-14 radiolabelling and tissue distribution evaluation of a potential anti-TB compound.

This paper describes a five-step synthesis of a carbon-14-labelled pyrazole compound (11). A total of 2.96 MBq of 11 was obtained with the specific activity of 2242.

Dual radiolabeling as a technique to track nanocarriers: the case of gold nanoparticles.

Gold nanoparticles (AuNPs) have shown great potential for use in nanomedicine and nanotechnologies due to their ease of synthesis and functionalization. However, their apparent biocompatibility and biodistribution is still a matter of intense debate due to the lack of clear safety data. To investigate the biodistribution of AuNPs, monodisperse 14-nm dual-radiolabeled [14C]citrate-coated [198Au]AuNPs were synthesized and their physico-chemical characteristics compared to those of non-radiolabeled AuNPs synthesized by the same method.

Carbon-14 radiolabeling and in vivo biodistribution of a potential anti-TB compound.

A potential anti-TB compound bearing a nitroimidazole moiety from iThemba Pharmaceuticals TB chemical library exhibits promising in vitro activity in the microplate almar blue assay (MABA) with a minimum inhibitory concentration (MIC) value of 3 µg/mL. It is equipotent to the front-line drug Isoniazid, but the compound is less toxic with an IC50 of >100 µg/mL. Therefore, this potential iThemba nitroimidazole, 4-([1,1'-[(14)C6]biphenyl]-4-ylmethyl)-9-nitro-3,4,5,6-tetrahydro-2H-imidazo[2,1-b][1,3,6]oxadiazocine, was radiolabeled with the C-14 isotope.