Discovery of potent, selective, and orally available WEE1 inhibitors that demonstrate increased DNA damage and mitosis in tumor cells leading to tumor regression in vivo

被引：0

作者：

Sun, Shaoxian ^{[1
]}

Silvergleid, Sarah ^{[1
]}

Gerasyuto, Aleksey I. ^{[1
]}

Wang, Jiashi ^{[1
]}

Pelletier, Robert D. ^{[1
]}

Placzek, Andrew ^{[1
]}

Knight, Jennifer L. ^{[1
]}

Clark, Anthony ^{[1
]}

Wright, Hamish ^{[1
]}

Yin, Wu ^{[1
]}

Elk, Jackson Chief ^{[1
]}

Bell, Jeff ^{[1
]}

Bos, Pieter H. ^{[1
]}

Boyles, Nicholas A. ^{[1
]}

Therrien, Eric ^{[1
]}

Jensen, Kristian ^{[1
]}

Akinsanya, Karen ^{[1
]}

机构：

[1] Schrodinger Inc, New York, NY USA

来源：

CANCER RESEARCH | 2022年 / 82卷 / 12期

关键词：

D O I：

暂无

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

2570

引用

页数：2

共 7 条

[1] Development of novel, potent orally available Wee1 inhibitors with robust antitumor efficacy in vivo
Gavory, Gerald
O'Dowd, Colin
Rozycka, Ewelina
Boyd, Caroline
Gorges, Beronia
McLean, Estelle
Rountree, Shane
Sheperd, Steven
Burton, Stephanie
McFarland, Mary
Janssen, Dominic
Treder, Adam
Wilkinson, Andy
Burkamp, Frank
Harrison, Tim
MOLECULAR CANCER RESEARCH, 2017, 15
[2] Potent anti-tumor activity correlated with inhibition of DNA damage response genes with highly selective and orally bioavailable CDK12 covalent inhibitors
Poddutoori, R.
Rajagopalan, S.
Mukherjee, S.
Marappan, S.
Samiulla, D.
Nayak, S.
Sivakumar, S.
Ravindra, M.
Gore, S.
Dhudashiya, A.
Charamanna, K.
Daginakatte, G.
Chelur, S.
Ramachandra, M.
Samajdar, S.
EUROPEAN JOURNAL OF CANCER, 2018, 103 : E94 - E95
[3] Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models
Luecking, Ulrich
Wortmann, Lars
Wengner, Antje M.
Lefranc, Julien
Lienau, Philip
Briem, Hans
Siemeister, Gerhard
Boemer, Ulf
Denner, Karsten
Schaefer, Martina
Koppitz, Marcus
Eis, Knut
Bartels, Florian
Bader, Benjamin
Bone, Wilhelm
Moosmayer, Dieter
Holton, Simon J.
Eberspaecher, Uwe
Grudzinska-Goebel, Joanna
Schatz, Christoph
Deeg, Gesa
Mumberg, Dominik
von Nussbaum, Franz
JOURNAL OF MEDICINAL CHEMISTRY, 2020, 63 (13) : 7293 - 7325
[4] Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE):: Discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1′ substituents
Lu, Zhonghui
Ott, Gregory R.
Anand, Rajan
Liu, Rui-Qin
Covington, Maryanne B.
Vaddi, Krishna
Qian, Mingxin
Newton, Robert C.
Christ, David D.
Trzaskos, James
Duan, James J. -W.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (06) : 1958 - 1962
[5] Potent, selective and orally bioavailable inhibitors of tumor necrosis factor-a converting enzyme (TACE):: Discovery of novel indole, benzofuran, imidazopyridine and pyrazolopyridine P1′ substituents
Lu, Zhonghui
Anand, Rajan
Liu, Richard
Covington, Maryanne
Vaddi, Krishna
Qian, Mingxin
Duan, James J-W.
Ott, Gregory R.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 230 : U2666 - U2667
[6] Discovery of potent and selective inhibitors of the protein tyrosine phosphatases PTPN2 and PTPN1 to trigger anti-tumor immunity through sensitization of tumor cells and activation of immune cells
Pervolaraki, Kalliopi
Katkeviciute, Egle
Lambin, Dominique
Boland, Sandro
Kilonda, Amuri
Pericolle, Vincent
Nijs, Marnik
Haeck, Wanda
Metzger, Kristine
Klaassen, Hugo
Marchand, Arnaud
Chaltin, Patrick
Versele, Matthias
Spalinger, Marianne
Scharl, Michael
CANCER RESEARCH, 2023, 83 (07)
[7] XL518, a potent selective orally bioavailable MEK1 inhibitor, downregulates the RAS/RAF/MEK/ERK pathway in vivo, resulting in tumor growth inhibition and regression in pre-clinical models
Johnston, Stuart
MOLECULAR CANCER THERAPEUTICS, 2007, 6 (12) : 3595S - 3595S

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