134 related articles for article (PubMed ID: 38640588)
1. Discovery of novel pyridone-benzamide derivatives possessing a 1-methyl-2-benzimidazolinone moiety as potent EZH2 inhibitors for the treatment of B-cell lymphomas.
Wu D; Zeng X; Zhao Y; Qin M; Gong P
Bioorg Med Chem; 2024 May; 105():117725. PubMed ID: 38640588
[TBL] [Abstract][Full Text] [Related]
2. Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
Zhou B; Liang X; Mei H; Qi S; Jiang Z; Wang A; Zou F; Liu Q; Liu J; Wang W; Hu C; Chen Y; Wang Z; Wang B; Wang L; Liu J; Liu Q
J Med Chem; 2021 Oct; 64(20):15170-15188. PubMed ID: 34664960
[TBL] [Abstract][Full Text] [Related]
3. Design, synthesis and activity evaluation of quinolinone derivatives as EZH2 inhibitors.
Cai J; You H; Qin X; Wang Y; Li W
Bioorg Med Chem Lett; 2024 Jun; 105():129726. PubMed ID: 38580135
[TBL] [Abstract][Full Text] [Related]
4. Six Years (2012-2018) of Researches on Catalytic EZH2 Inhibitors: The Boom of the 2-Pyridone Compounds.
Fioravanti R; Stazi G; Zwergel C; Valente S; Mai A
Chem Rec; 2018 Dec; 18(12):1818-1832. PubMed ID: 30338896
[TBL] [Abstract][Full Text] [Related]
5. Identification of novel EZH2 inhibitors through pharmacophore-based virtual screening and biological assays.
Wu Y; Hu J; Ding H; Chen L; Zhang Y; Liu R; Xu P; Du D; Lu W; Liu J; Liu Y; Liu YC; Lu J; Zhang J; Yao Z; Luo C
Bioorg Med Chem Lett; 2016 Aug; 26(15):3813-7. PubMed ID: 27289323
[TBL] [Abstract][Full Text] [Related]
6. 2,2- dimethylbenzopyran derivatives containing pyridone structural fragments as selective dual-targeting inhibitors of HIF-1α and EZH2 for the treatment of lung cancer.
Xu H; Zhang J; Zhuang J; Chen Y; Chen L; Wang J; Cao R; Liu F; Wang K; Zhang X; Wang L; Chen G
Bioorg Chem; 2024 Jun; 147():107419. PubMed ID: 38703440
[TBL] [Abstract][Full Text] [Related]
7. EZH2 W113C is a gain-of-function mutation in B-cell lymphoma enabling both PRC2 methyltransferase activation and tazemetostat resistance.
Chu L; Tan D; Zhu M; Qu Y; Ma X; Song BL; Qi W
J Biol Chem; 2023 Apr; 299(4):103073. PubMed ID: 36858198
[TBL] [Abstract][Full Text] [Related]
8. Selective inhibition of EZH2 by ZLD10A blocks H3K27 methylation and kills mutant lymphoma cells proliferation.
Song X; Zhang L; Gao T; Ye T; Zhu Y; Lei Q; Feng Q; He B; Deng H; Yu L
Biomed Pharmacother; 2016 Jul; 81():288-294. PubMed ID: 27261606
[TBL] [Abstract][Full Text] [Related]
9. Selective inhibition of EZH2 by ZLD1039 blocks H3K27 methylation and leads to potent anti-tumor activity in breast cancer.
Song X; Gao T; Wang N; Feng Q; You X; Ye T; Lei Q; Zhu Y; Xiong M; Xia Y; Yang F; Shi Y; Wei Y; Zhang L; Yu L
Sci Rep; 2016 Feb; 6():20864. PubMed ID: 26868841
[TBL] [Abstract][Full Text] [Related]
10. Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation.
Yap DB; Chu J; Berg T; Schapira M; Cheng SW; Moradian A; Morin RD; Mungall AJ; Meissner B; Boyle M; Marquez VE; Marra MA; Gascoyne RD; Humphries RK; Arrowsmith CH; Morin GB; Aparicio SA
Blood; 2011 Feb; 117(8):2451-9. PubMed ID: 21190999
[TBL] [Abstract][Full Text] [Related]
11. Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.
Yang X; Li F; Konze KD; Meslamani J; Ma A; Brown PJ; Zhou MM; Arrowsmith CH; Kaniskan HÜ; Vedadi M; Jin J
J Med Chem; 2016 Aug; 59(16):7617-33. PubMed ID: 27468126
[TBL] [Abstract][Full Text] [Related]
12. Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Vaswani RG; Gehling VS; Dakin LA; Cook AS; Nasveschuk CG; Duplessis M; Iyer P; Balasubramanian S; Zhao F; Good AC; Campbell R; Lee C; Cantone N; Cummings RT; Normant E; Bellon SF; Albrecht BK; Harmange JC; Trojer P; Audia JE; Zhang Y; Justin N; Chen S; Wilson JR; Gamblin SJ
J Med Chem; 2016 Nov; 59(21):9928-9941. PubMed ID: 27739677
[TBL] [Abstract][Full Text] [Related]
13. Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.
He H; Hu X; Teng F; Liu Z; Zhang Q; Feng Z; Feng Q; Yu L
Bioorg Med Chem Lett; 2020 Mar; 30(5):126957. PubMed ID: 31959420
[TBL] [Abstract][Full Text] [Related]
14. Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor.
Honma D; Kanno O; Watanabe J; Kinoshita J; Hirasawa M; Nosaka E; Shiroishi M; Takizawa T; Yasumatsu I; Horiuchi T; Nakao A; Suzuki K; Yamasaki T; Nakajima K; Hayakawa M; Yamazaki T; Yadav AS; Adachi N
Cancer Sci; 2017 Oct; 108(10):2069-2078. PubMed ID: 28741798
[TBL] [Abstract][Full Text] [Related]
15. Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2).
Xu X; Chen J; Wang G; Zhang X; Li Q; Zhou X; Guo F; Li M
Bioorg Med Chem Lett; 2024 Jan; 97():129558. PubMed ID: 37956762
[TBL] [Abstract][Full Text] [Related]
16. Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study.
Italiano A; Soria JC; Toulmonde M; Michot JM; Lucchesi C; Varga A; Coindre JM; Blakemore SJ; Clawson A; Suttle B; McDonald AA; Woodruff M; Ribich S; Hedrick E; Keilhack H; Thomson B; Owa T; Copeland RA; Ho PTC; Ribrag V
Lancet Oncol; 2018 May; 19(5):649-659. PubMed ID: 29650362
[TBL] [Abstract][Full Text] [Related]
17. Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug.
Kung PP; Fan C; Gukasyan HJ; Huang B; Kephart S; Kraus M; Lee JH; Sutton SC; Yamazaki S; Zehnder L
J Med Chem; 2021 Feb; 64(3):1725-1732. PubMed ID: 33529029
[TBL] [Abstract][Full Text] [Related]
18. Identification of catalytic and non-catalytic activity inhibitors against PRC2-EZH2 complex through multiple high-throughput screening campaigns.
Zhou Y; Du DH; Wang J; Cai XQ; Deng AX; Nosjean O; Boutin JA; Renard P; Yang DH; Luo C; Wang MW
Chem Biol Drug Des; 2020 Oct; 96(4):1024-1051. PubMed ID: 32394628
[TBL] [Abstract][Full Text] [Related]
19. Discovery, design, and synthesis of indole-based EZH2 inhibitors.
Gehling VS; Vaswani RG; Nasveschuk CG; Duplessis M; Iyer P; Balasubramanian S; Zhao F; Good AC; Campbell R; Lee C; Dakin LA; Cook AS; Gagnon A; Harmange JC; Audia JE; Cummings RT; Normant E; Trojer P; Albrecht BK
Bioorg Med Chem Lett; 2015 Sep; 25(17):3644-9. PubMed ID: 26189078
[TBL] [Abstract][Full Text] [Related]
20. Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.
Woo J; Kim HY; Byun BJ; Chae CH; Lee JY; Ryu SY; Park WK; Cho H; Choi G
Bioorg Med Chem Lett; 2014 Jun; 24(11):2486-92. PubMed ID: 24767850
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
