BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

129 related articles for article (PubMed ID: 34665631)

  • 1. Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile.
    Jin T; Xu L; Wang P; Hu X; Zhang R; Wu Z; Du W; Kan W; Li K; Wang C; Zhou Y; Li J; Liu T
    J Med Chem; 2021 Oct; 64(20):15069-15090. PubMed ID: 34665631
    [TBL] [Abstract][Full Text] [Related]  

  • 2. Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.
    Tong L; Song P; Jiang K; Xu L; Jin T; Wang P; Hu X; Fang S; Gao A; Zhou Y; Liu T; Li J; Hu Y
    Eur J Med Chem; 2019 Jul; 173():44-62. PubMed ID: 30986571
    [TBL] [Abstract][Full Text] [Related]  

  • 3. Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors.
    Huang M; Huang Y; Guo J; Yu L; Chang Y; Wang X; Luo J; Huang Y; Tu Z; Lu X; Xu Y; Zhang Z; Zhang Z; Ding K
    Eur J Med Chem; 2021 Feb; 211():113023. PubMed ID: 33248853
    [TBL] [Abstract][Full Text] [Related]  

  • 4. Discovery of pyrido[3,2-d]pyrimidin-6(5H)-one derivatives as checkpoint kinase 1 (CHK1) inhibitors with potent antitumor efficacy.
    Hu S; Jiang C; Jin Q
    Eur J Med Chem; 2024 Apr; 269():116351. PubMed ID: 38547734
    [TBL] [Abstract][Full Text] [Related]  

  • 5. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.
    Myers SM; Miller DC; Molyneux L; Arasta M; Bawn RH; Blackburn TJ; Cook SJ; Edwards N; Endicott JA; Golding BT; Griffin RJ; Hammonds T; Hardcastle IR; Harnor SJ; Heptinstall AB; Lochhead PA; Martin MP; Martin NC; Newell DR; Owen PJ; Pang LC; Reuillon T; Rigoreau LJM; Thomas HD; Tucker JA; Wang LZ; Wong AC; Noble MEM; Wedge SR; Cano C
    Eur J Med Chem; 2019 Sep; 178():530-543. PubMed ID: 31212132
    [TBL] [Abstract][Full Text] [Related]  

  • 6. Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.
    Liang X; Liu X; Wang B; Zou F; Wang A; Qi S; Chen C; Zhao Z; Wang W; Qi Z; Lv F; Hu Z; Wang L; Zhang S; Liu Q; Liu J
    J Med Chem; 2016 Mar; 59(5):1984-2004. PubMed ID: 26789553
    [TBL] [Abstract][Full Text] [Related]  

  • 7. Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).
    Osborne JD; Matthews TP; McHardy T; Proisy N; Cheung KM; Lainchbury M; Brown N; Walton MI; Eve PD; Boxall KJ; Hayes A; Henley AT; Valenti MR; De Haven Brandon AK; Box G; Jamin Y; Robinson SP; Westwood IM; van Montfort RL; Leonard PM; Lamers MB; Reader JC; Aherne GW; Raynaud FI; Eccles SA; Garrett MD; Collins I
    J Med Chem; 2016 Jun; 59(11):5221-37. PubMed ID: 27167172
    [TBL] [Abstract][Full Text] [Related]  

  • 8. Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.
    Degorce SL; Barlaam B; Cadogan E; Dishington A; Ducray R; Glossop SC; Hassall LA; Lach F; Lau A; McGuire TM; Nowak T; Ouvry G; Pike KG; Thomason AG
    J Med Chem; 2016 Jul; 59(13):6281-92. PubMed ID: 27259031
    [TBL] [Abstract][Full Text] [Related]  

  • 9. Design, Synthesis, and Biological Evaluation of Orally Bioavailable CHK1 Inhibitors Active against Acute Myeloid Leukemia.
    Jin T; Wang P; Long X; Jiang K; Song P; Wu W; Xu G; Zhou Y; Li J; Liu T
    ChemMedChem; 2021 May; 16(9):1477-1487. PubMed ID: 33591599
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
    Lainchbury M; Matthews TP; McHardy T; Boxall KJ; Walton MI; Eve PD; Hayes A; Valenti MR; de Haven Brandon AK; Box G; Aherne GW; Reader JC; Raynaud FI; Eccles SA; Garrett MD; Collins I
    J Med Chem; 2012 Nov; 55(22):10229-40. PubMed ID: 23082860
    [TBL] [Abstract][Full Text] [Related]  

  • 11. Synthesis and biological evaluation of 2,6-disubstituted-9H-purine, 2,4-disubstitued-thieno[3,2-d]pyrimidine and -7H-pyrrolo[2,3-d]pyrimidine analogues as novel CHK1 inhibitors.
    Tian C; Han Z; Li Y; Wang M; Yang J; Wang X; Zhang Z; Liu J
    Eur J Med Chem; 2018 May; 151():836-848. PubMed ID: 29684894
    [TBL] [Abstract][Full Text] [Related]  

  • 12. Discovery of novel and orally bioavailable CDK 4/6 inhibitors with high kinome selectivity, low toxicity and long-acting stability for the treatment of multiple myeloma.
    Yuan K; Kuang W; Chen W; Ji M; Min W; Zhu Y; Hou Y; Wang X; Li J; Wang L; Yang P
    Eur J Med Chem; 2022 Jan; 228():114024. PubMed ID: 34875521
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.
    Yan G; Pu C; Lan S; Zhong X; Zhou M; Hou X; Yang J; Shan H; Zhao L; Li R
    Eur J Med Chem; 2019 Sep; 178():667-686. PubMed ID: 31228810
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.
    Lapierre JM; Eathiraj S; Vensel D; Liu Y; Bull CO; Cornell-Kennon S; Iimura S; Kelleher EW; Kizer DE; Koerner S; Makhija S; Matsuda A; Moussa M; Namdev N; Savage RE; Szwaya J; Volckova E; Westlund N; Wu H; Schwartz B
    J Med Chem; 2016 Jul; 59(13):6455-69. PubMed ID: 27305487
    [TBL] [Abstract][Full Text] [Related]  

  • 15. Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.
    Pettus LH; Andrews KL; Booker SK; Chen J; Cee VJ; Chavez F; Chen Y; Eastwood H; Guerrero N; Herberich B; Hickman D; Lanman BA; Laszlo J; Lee MR; Lipford JR; Mattson B; Mohr C; Nguyen Y; Norman MH; Powers D; Reed AB; Rex K; Sastri C; Tamayo N; Wang P; Winston JT; Wu B; Wu T; Wurz RP; Xu Y; Zhou Y; Tasker AS; Wang HL
    J Med Chem; 2016 Jul; 59(13):6407-30. PubMed ID: 27285051
    [TBL] [Abstract][Full Text] [Related]  

  • 16. Synthesis and Profiling of a Novel Potent Selective Inhibitor of CHK1 Kinase Possessing Unusual N-trifluoromethylpyrazole Pharmacophore Resistant to Metabolic N-dealkylation.
    Samadder P; Suchánková T; Hylse O; Khirsariya P; Nikulenkov F; Drápela S; Straková N; Vaňhara P; Vašíčková K; Kolářová H; Binó L; Bittová M; Ovesná P; Kollár P; Fedr R; Ešner M; Jaroš J; Hampl A; Krejčí L; Paruch K; Souček K
    Mol Cancer Ther; 2017 Sep; 16(9):1831-1842. PubMed ID: 28619751
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Downregulation of c-Myc expression confers sensitivity to CHK1 inhibitors in hematologic malignancies.
    Jiang KL; Tong LX; Wang T; Wang HL; Hu XB; Xu GY; Jin TT; Kan WJ; Xu L; Li JN; Zhang KX; Song N; Liu JY; Zhang MM; Wu WB; Xiang YQ; Gao AH; Hu YZ; Zhou YB; Liu T; Yang JM; Li J
    Acta Pharmacol Sin; 2022 Jan; 43(1):220-228. PubMed ID: 33782542
    [TBL] [Abstract][Full Text] [Related]  

  • 18. Checkpoint kinase‑1 inhibition and etoposide exhibit a strong synergistic anticancer effect on chronic myeloid leukemia cell line K562 by impairing homologous recombination DNA damage repair.
    Fan Z; Luo H; Zhou J; Wang F; Zhang W; Wang J; Li S; Lai Q; Xu Y; Wang G; Liang A; Xu J
    Oncol Rep; 2020 Nov; 44(5):2152-2164. PubMed ID: 32901871
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study.
    Jiang X; Zhou J; Ai J; Song Z; Peng X; Xing L; Xi Y; Guo J; Yao Q; Ding J; Geng M; Zhang A
    Eur J Med Chem; 2015 Nov; 105():39-56. PubMed ID: 26476749
    [TBL] [Abstract][Full Text] [Related]  

  • 20. Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.
    Laufer R; Li SW; Liu Y; Ng G; Lang Y; Feher M; Brokx R; Beletskaya I; Hodgson R; Mao G; Plotnikova O; Awrey DE; Mason JM; Wei X; Lin DC; Che Y; Kiarash R; Madeira B; Fletcher GC; Mak TW; Bray MR; Pauls HW
    Bioorg Med Chem Lett; 2016 Aug; 26(15):3562-6. PubMed ID: 27335255
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 7.