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Publikationer i urvalet

19 träffar

Bibliografisk träff 2024-01-31

Structure-Guided Design and Synthesis of Pyridinone-Based Selective Bromodomain and Extra-Terminal Domain (BET)-First Bromodomain (BD1) Inhibitors.

Li Y, Shen Z, Ratia K, Zhao J, Huang F, Dubrovyskyii O, Indukuri D, Fu J, Lozano Ramos O, Thatcher GRJ, Xiong R.

J Med Chem · journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.3c01837

Bibliografisk träff 2023-12-14

Novel Triazolopyridine-Based BRD4 Inhibitors as Potent HIV-1 Latency Reversing Agents.

Wang YK, Huang XS, Sun H, Ma MD, Yu HP, Hu W, Li ZY, Li Z, Luo RH, Tian RR, Xiao TF, Yang LM, Zheng YT, Li X.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.3c00373

Bibliografisk träff 2022-12-29

Design, synthesis, and biological evaluation of quinoxalinone derivatives as potent BRD4 inhibitors.

Xu KY, Wang XT, Cheng L, Cui QH, Shi JT, Zhang LW, Chen SW.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2022.117152

Bibliografisk träff 2022-09-29

A comprehensive review of BET-targeting PROTACs for cancer therapy.

Zhou XL, Zhao F, Xu YT, Guan YY, Yu T, Zhang YZ, Duan YC, Zhao Y.

Bioorg Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1016/j.bmc.2022.117033

Bibliografisk träff 2022-06-11

Design and development of a novel series of oral bivalent BET inhibitors with potent anticancer activities.

Luo M, Wu Q, Yang Y, Sun L, Huan X, Tian C, Xiong B, Miao Z, Wang Y, Chen D.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114519

Bibliografisk träff 2021-10-29

Discovery of 1-(5-(1H-benzo[d]imidazole-2-yl)-2,4-dimethyl-1H-pyrrol-3-yl)ethan-1-one derivatives as novel and potent bromodomain and extra-terminal (BET) inhibitors with anticancer efficacy.

Kong B, Zhu Z, Li H, Hong Q, Wang C, Ma Y, Zheng W, Jiang F, Zhang Z, Ran T, Bian Y, Yang N, Lu T, Zhu J, Tang W, Chen Y.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.113953

Bibliografisk träff 2021-04-03

Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family.

Fang L, Hu Z, Yang Y, Chen P, Zhou J, Zhang H.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2021.116133

Bibliografisk träff 2020-12-29

Targeting MYC: From understanding its biology to drug discovery.

Ross J, Miron CE, Plescia J, Laplante P, McBride K, Moitessier N, Möröy T.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2020.113137

Bibliografisk träff 2020-08-31

Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer.

Yang Y, Fang L, Chen P, Zhang H, Zhou J.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.0c00294

Bibliografisk träff 2020-06-15

Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.

Li Y, Zhao J, Gutgesell LM, Shen Z, Ratia K, Dye K, Dubrovskyi O, Zhao H, Huang F, Tonetti DA, Thatcher GRJ, Xiong R.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.0c00456

Bibliografisk träff 2020-05-07

Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain.

Sheppard GS, Wang L, Fidanze SD, Hasvold LA, Liu D, Pratt JK, Park CH, Longenecker K, Qiu W, Torrent M, Kovar PJ, Bui M, Faivre E, Huang X, Lin X, Wilcox D, Zhang L, Shen Y, Albert DH, Magoc TJ, Rajaraman G, Kati WM, McDaniel KF.

J Med Chem · research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1021/acs.jmedchem.0c00628

Bibliografisk träff 2020-04-07

Discovery of 8-Methyl-pyrrolo[1,2-a]pyrazin-1(2H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors.

Li Z, Xiao S, Yang Y, Chen C, Lu T, Chen Z, Jiang H, Chen S, Luo C, Zhou B.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.9b01784

Bibliografisk träff 2019-11-26

Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5-a]pyrazin-8(7H)-one as Novel BRD4 Inhibitors.

Yang Y, Chen P, Zhao L, Zhang F, Zhang H, Zhou J.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.9b00474

Bibliografisk träff 2019-02-05

Clinical candidates modulating protein-protein interactions: The fragment-based experience.

Valenti D, Hristeva S, Tzalis D, Ottmann C.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2019.01.084

Bibliografisk träff 2018-11-16

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.

Xing J, Zhang R, Jiang X, Hu T, Wang X, Qiao G, Wang J, Yang F, Luo X, Chen K, Shen J, Luo C, Jiang H, Zheng M.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2018.11.018

Bibliografisk träff 2018-05-09

Straightforward hit identification approach in fragment-based discovery of bromodomain-containing protein 4 (BRD4) inhibitors.

Borysko P, Moroz YS, Vasylchenko OV, Hurmach VV, Starodubtseva A, Stefanishena N, Nesteruk K, Zozulya S, Kondratov IS, Grygorenko OO.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2018.05.010

Bibliografisk träff 2018-04-11

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.

Fidanze SD, Liu D, Mantei RA, Hasvold LA, Pratt JK, Sheppard GS, Wang L, Holms JH, Dai Y, Aguirre A, Bogdan A, Dietrich JD, Marjanovic J, Park CH, Hutchins CW, Lin X, Bui MH, Huang X, Wilcox D, Li L, Wang R, Kovar P, Magoc TJ, Rajaraman G, Albert DH, Shen Y, Kati WM, McDaniel KF.

Bioorg Med Chem Lett · research support, non-u.s. gov't; research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1016/j.bmcl.2018.04.020

Bibliografisk träff 2017-10-12

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.

McDaniel KF, Wang L, Soltwedel T, Fidanze SD, Hasvold LA, Liu D, Mantei RA, Pratt JK, Sheppard GS, Bui MH, Faivre EJ, Huang X, Li L, Lin X, Wang R, Warder SE, Wilcox D, Albert DH, Magoc TJ, Rajaraman G, Park CH, Hutchins CW, Shen JJ, Edalji RP, Sun CC, Martin R, Gao W, Wong S, Fang G, Elmore SW, Shen Y, Kati WM.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.7b00746

Bibliografisk träff 2017-03-07

Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors.

Zhao L, Yang Y, Guo Y, Yang L, Zhang J, Zhou J, Zhang H.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2017.03.008

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Publikationer i urvalet

Structure-Guided Design and Synthesis of Pyridinone-Based Selective Bromodomain and Extra-Terminal Domain (BET)-First Bromodomain (BD1) Inhibitors.

Novel Triazolopyridine-Based BRD4 Inhibitors as Potent HIV-1 Latency Reversing Agents.

Design, synthesis, and biological evaluation of quinoxalinone derivatives as potent BRD4 inhibitors.

A comprehensive review of BET-targeting PROTACs for cancer therapy.

Design and development of a novel series of oral bivalent BET inhibitors with potent anticancer activities.

Discovery of 1-(5-(1H-benzo[d]imidazole-2-yl)-2,4-dimethyl-1H-pyrrol-3-yl)ethan-1-one derivatives as novel and potent bromodomain and extra-terminal (BET) inhibitors with anticancer efficacy.

Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family.

Targeting MYC: From understanding its biology to drug discovery.

Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer.

Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.

Discovery of <i>N</i>-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1<i>H</i>-pyrrolo[2,3-<i>c</i>]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain.

Discovery of 8-Methyl-pyrrolo[1,2-<i>a</i>]pyrazin-1(2<i>H</i>)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors.

Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5-<i>a</i>]pyrazin-8(7H)-one as Novel BRD4 Inhibitors.

Clinical candidates modulating protein-protein interactions: The fragment-based experience.

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.

Straightforward hit identification approach in fragment-based discovery of bromodomain-containing protein 4 (BRD4) inhibitors.

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.

Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors.