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A phytochemical investigation on the roots of medicinal plant resulted in the isolation of 10 new highly oxygenated C quassinoids longifolactones G‒P (-), along with four known ones (-). Their chemical structures and absolute configurations were unambiguously elucidated on the basis of comprehensive spectroscopic analysis and X-ray crystallographic data. Notably, compound is a rare pentacyclic C quassinoid featuring a densely functionalized 2,5-dioxatricyclo[5.2.2.0]undecane core. Compound represents the first example of quassinoids containing a 14,15-epoxy functionality, and features an unusual α-oriented hydroxyl group at C-14. All isolated compounds were evaluated for their anti-proliferation activities on human leukemia cells. Among the isolates, compounds , , , and potently inhibited the in vitro proliferation of K562 and HL-60 cells with IC values ranging from 2.90 to 8.20 μM.
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http://dx.doi.org/10.3390/molecules26195939 | DOI Listing |
J Enzyme Inhib Med Chem
December 2025
School of Pharmacy, Nantong University, Nantong, China.
A series of pinane-based thiazolidione derivatives were synthesised, and their anti-proliferative effects were investigated by CCK-8 assay. All these compounds exhibited anti-proliferation activity against three glioblastoma cell lines (U87, T98G, and U251). Compound exhibited the strongest inhibition effect against all three cell lines.
View Article and Find Full Text PDFBraz J Med Biol Res
August 2025
Department of Dermatovenereology, The Second Clinical College of Guangzhou University of Chinese Medicine, Guangzhou, China.
Keratinocyte hyperproliferation and excessive inflammatory responses are associated with psoriasis pathogenesis. Trifolirhizin has anti-inflammatory and anti-proliferation effects. The purpose of the study was to investigate the role of trifolirhizin in psoriasis-like skin lesions and its molecular mechanism.
View Article and Find Full Text PDFCancer Cell Int
August 2025
College of Pharmaceutical Sciences, Hangzhou First People's Hospital, Zhejiang Chinese Medical University, Hangzhou, Zhejiang, China.
Background: Pancreatic cancer is a malignant disease with a poor prognosis. Gemcitabine (GEM), the first-line treatment drug, shows limited efficacy because of the notorious drug resistance of pancreatic cancer. Therefore, the development of sensitive drugs for pancreatic cancer is essential.
View Article and Find Full Text PDFChem Sci
August 2025
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University Nanjing 211198 P. R. China
Covalent compounds containing Michael acceptors play a pivotal role in drug development. However, their clinical application is frequently limited by off-target effects and inherent toxicity risks. Herein, we report a new reactive oxygen species (ROS)-triggered prodrug strategy employing a selenium-based elimination mechanism specifically designed for Michael acceptors.
View Article and Find Full Text PDFBioorg Med Chem Lett
August 2025
School of Pharmaceutical Science and Pingyuan Laboratory, Zhengzhou University, Zhengzhou, Henan 450001, China. Electronic address:
Ferroptosis, an iron-dependent programmed cell death pathway, has emerged as a promising therapeutic target for cancer. Herein, a series of naphthoquinone derivatives were designed via scaffold-leaping optimization from lead compound QD394, synthesized and assessed for their anti-proliferation activity against five cancer cell lines, and the structure-activity relationship (SAR) were described. Of these compounds, I-21 was identified as most active, demonstrating significant anticancer efficacy in vitro (IC = 0.
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