Bioassay-guided fractionation of an ethanol extract of a Madagascar collection of the bark of Scutia myrtina led to the isolation of three new anthrone-anthraquinones, scutianthraquinones A, B and C (1-3), one new bisanthrone-anthraquinone, scutianthraquinone D (4), and the known anthraquinone, aloesaponarin I (5). The structures of all compounds were determined using a combination of 1D and 2D NMR experiments, including COSY, TOCSY, HSQC, HMBC, and ROESY sequences, and mass spectrometry. All the isolated compounds were tested against the A2780 human ovarian cancer cell line for antiproliferative activities, and against the chloroquine-resistant Plasmodium falciparum strains Dd2 and FCM29 for antiplasmodial activities. Compounds 1, 2 and 4 showed weak antiproliferative activities against the A2780 ovarian cancer cell line, while compounds 1-4 exhibited moderate antiplasmodial activities against P. falciparum Dd2 and compounds 1, 2, and 4 exhibited moderate antiplasmodial activities against P. falciparum FCM29.
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http://dx.doi.org/10.1016/j.bmc.2009.02.022 | DOI Listing |
Mini Rev Med Chem
January 2025
Department of Physiology and Pharmacology Vittorio Erspamer, Sapienza University of Rome, 00161, Rome, Italy.
Currently, the synthesis of bioactive sulfonamides using amino acid as a starting reagent has become an area of research interest in organic chemistry. Over the years, an amine-sulfonyl chloride reaction has been adopted as a common step in traditional sulfonamide synthetic methods. However, recent developments have shown amino acids to be better precursors than amines in the synthesis of sulfonamides.
View Article and Find Full Text PDFChem Asian J
January 2025
Birla Institute of Technology and Science - Pilani Campus: Birla Institute of Technology & Science Pilani, Pharmacy, BITS Pilani, Pilani campus, Vidya Vihar, 333031, Pilani, INDIA.
In this study, we built on the known inhibitory potential of diaminoquinazolines (DAQs) against different stages of Plasmodium development and designed a convenient two-step synthesis to combine DAQ with the primaquine (PQ) pharmacophore. The PQ-DAQ hybrids displayed potent in vitro activities in the low nanomolar range (IC50 of 135.20-398.
View Article and Find Full Text PDFMolecules
December 2024
Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovačića 1, 10000 Zagreb, Croatia.
As the resistance of to the existing antimalarials increases, there is a crucial need to expand the antimalarial drug pipeline. We recently identified potent antimalarial compounds, namely harmiquins, hybrids derived from the β-carboline alkaloid harmine and 4-amino-7-chloroquinoline, a key structural motif of chloroquine (CQ). To further explore the structure-activity relationship, we synthesised 13 novel hybrid compounds at the position -9 of the β-carboline ring and evaluated their efficacy in vitro against 3D7 and Dd2 strains (CQ sensitive and multi-drug resistant, respectively).
View Article and Find Full Text PDFInt J Nanomedicine
January 2025
Affiliated Hospital, Qinghai University, Xining, Qinghai, People's Republic of China.
Background: Acacetin (AC) is a flavonoid compound with antiperoxidant, anti-inflammatory, and antiplasmodial activity. However, the solubility of AC is poor and nano acacetin (Nano AC) was synthesized. The intestinal mucosal barrier is impaired in sepsis rats, and the protective effects and mechanism of AC and Nano AC on the intestinal mucosal barrier are unclear.
View Article and Find Full Text PDFAppl Sci (Basel)
January 2024
Department of Microbiology and Medical Zoology, University of Puerto Rico School of Medicine, San Juan 00921, Puerto Rico.
Gracilioether M () and 11,12-dihydrogracilioether M (), two polyketides with a [2(5H)-furanylidene]ethanoate moiety, along with known plakortone G () and its new naturally occurring derivative 9,10-dihydroplakortone G (), were isolated from the Caribbean marine sponge . The structures and absolute configuration of , , and were characterized by analysis of HRESIMS and NMR spectroscopic data, chemical derivatization, and side-by-side comparisons with published NMR data of related analogs. Compounds and and a mixture of and were evaluated for cytotoxicity against MCF-7 human breast cancer cells.
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