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2-Phenyl-4-quinolone and 9-oxo-9,10-dihydroacridine derivatives were synthesized and screened as potential antitumor promoters by examining the ability of the compounds to inhibit Epstein-Barr virus early antigen (EBV-EA) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. Interestingly, compounds 14, 15, and 17 showed similar inhibitory effects (89-92%, 66-69%, and 24-29% at 1000, 500, and 100 mol ratio to TPA, respectively) against EBV-EA with potencies comparable to those of glycyrrhetic acid, a known natural antitumor-promoter.
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http://dx.doi.org/10.1016/j.bmc.2005.04.078 | DOI Listing |
Pathol Oncol Res
June 2023
TaiRx, Inc., Taipei, Taiwan.
CVM-1118 (foslinanib) is a phosphoric ester compound selected from 2-phenyl-4-quinolone derivatives. The NCI 60 cancer panel screening showed CVM-1125, the major active metabolite of CVM-1118, to exhibit growth inhibitory and cytotoxic effects at nanomolar range. CVM-1118 possesses multiple bioactivities, including inducing cellular apoptosis, cell cycle arrest at G/M, as well as inhibiting vasculogenic mimicry (VM) formation.
View Article and Find Full Text PDFMolecules
January 2023
Graduate Institute of Cancer Molecular Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei 11031, Taiwan.
Our previous study found that 2-phenyl-4-quinolone (2-PQ) derivatives are antimitotic agents, and we adopted the drug design concept of scaffold hopping to replace the 2-aromatic ring of 2-PQs with a 4-aromatic ring, representing 4-phenyl-2-quinolones (4-PQs). The 4-PQ compounds, whose structural backbones also mimic analogs of podophyllotoxin (PPT), maybe a new class of anticancer drugs with simplified PPT structures. In addition, 4-PQs are a new generation of anticancer lead compounds as apoptosis stimulators.
View Article and Find Full Text PDFBiotech Histochem
July 2019
c Department of Health and Nutrition Biotechnology, Asia University, Taichung , Taiwan.
KHC-4 is a 2-phenyl-4-quinolone analogue that exhibits anticancer activity. Aberrant activation of β-catenin signaling contributes to prostate cancer development and progression. Therefore, targeting β-catenin expression could be a useful approach to treating prostate cancer.
View Article and Find Full Text PDFChem Biol Interact
June 2018
Department of Chemical Engineering and Institute of Biotechnology and Chemical Engineering, I-Shou University, Kaohsiung, Taiwan. Electronic address:
Breast cancer is a major public health problem throughout the world. In this report, we investigated whether CHM-1, a novel synthetic antimitotic agent could be developed into a potent antitumor agent for treating human breast cancer. CHM-1 induced growth inhibition in MDA-MB-231, MDA-MB-453 and MCF-7 cells in a concentration-dependent manner.
View Article and Find Full Text PDFOncol Rep
March 2018
Department of Biochemistry, China Medical University, Taichung 404, Taiwan, R.O.C.
The present study aimed to investigate the biological effects of the new compound 2‑phenyl‑4‑quinolone (YT‑1) on human leukemia cells. Cell viability was determined by propidium iodide (PI) exclusion method followed by flow cytometry. Our results showed that YT‑1 inhibited the cell viability and resulted in morphologic changes to the U937, HL‑60 and K562 cells, respectively.
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