Zobrazeno 1 - 10
of 33
pro vyhledávání: '"kinase inhibitor design"'
Publikováno v:
Molbank, Vol 2020, Iss 4, p M1161 (2020)
A routine synthesis was performed to furnish the title compound which incorporates a versatile difluoromethyl group on the aniline substitution of a 4-anilinoquinoline kinase inhibitor motif. In addition, the small molecule crystal structure (of the
Externí odkaz:
https://doaj.org/article/3498346bf7c04255b431b0a8374f0b68
Publikováno v:
Molecules, Vol 27, Iss 2, p 570 (2022)
Deep machine learning is expanding the conceptual framework and capacity of computational compound design, enabling new applications through generative modeling. We have explored the systematic design of covalent protein kinase inhibitors by learning
Externí odkaz:
https://doaj.org/article/c8ce73d2ffa74a5b8c69c3bf7145cc83
Publikováno v:
Molbank, Vol 2019, Iss 4, p M1087 (2019)
We describe a straightforward synthesis of the title compound, incorporating a relatively rare 2-methyl-2H-1,2,3-triazole heterocylic motif as a potential kinase inhibitor motif. The small molecule crystal structure has been resolved, revealing an in
Externí odkaz:
https://doaj.org/article/90388ed5c4e043eb93aacdd15df54d39
Autor:
Christopher R. M. Asquith, Tuomo Laitinen, Carrow I. Wells, Graham J. Tizzard, William J. Zuercher
Publikováno v:
Molecules, Vol 25, Iss 7, p 1697 (2020)
We report the synthesis of several related 4-anilinoquinazolines as inhibitors of cardiac troponin I–interacting kinase (TNNi3K). These close structural analogs of 3-((6,7-dimethoxyquinazolin-4-yl)amino)-4-(dimethylamino)-N-methylbenzenesulfonamide
Externí odkaz:
https://doaj.org/article/2594383d1f2f4e0a883a37ecd9bd7e6b
Autor:
Christopher R. M. Asquith, James M. Bennett, Lianyong Su, Tuomo Laitinen, Jonathan M. Elkins, Julie E. Pickett, Carrow I. Wells, Zengbiao Li, Timothy M. Willson, William J. Zuercher
Publikováno v:
Molecules, Vol 24, Iss 22, p 4016 (2019)
SGC-GAK-1 (1) is a potent, selective, cell-active chemical probe for cyclin G-associated kinase (GAK). However, 1 was rapidly metabolized in mouse liver microsomes by cytochrome P450-mediated oxidation, displaying rapid clearance in liver microsomes
Externí odkaz:
https://doaj.org/article/00a1c9ab19194d05a4e83df24ad114f0
Publikováno v:
Trends in Pharmacological Sciences. 40(11):818-832
Kinases are attractive anticancer targets due to their central role in the growth, survival, and therapy resistance of tumor cells. This review explores the two primary kinase classes, the eukaryotic protein kinases (ePKs) and the atypical protein ki
Akademický článek
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Publikováno v:
Molbank, Vol 2019, Iss 4, p M1087 (2019)
We describe a straightforward synthesis of the title compound, incorporating a relatively rare 2-methyl-2H-1,2,3-triazole heterocylic motif as a potential kinase inhibitor motif. The small molecule crystal structure has been resolved, revealing an in
Autor:
Iwan J. P. de Esch, Thomas Wurdinger, Georgi K. Kanev, Bart A. Westerman, Rob Leurs, Albert J. Kooistra, Chris de Graaf
Publikováno v:
Kanev, G K, de Graaf, C, de Esch, I J P, Leurs, R, Würdinger, T, Westerman, B A & Kooistra, A J 2019, ' The Landscape of Atypical and Eukaryotic Protein Kinases ', Trends in Pharmacological Sciences, vol. 40, no. 11, pp. 818-832 . https://doi.org/10.1016/j.tips.2019.09.002
Kinases are attractive anticancer targets due to their central role in the growth, survival, and therapy resistance of tumor cells. This review explores the two primary kinase classes, the eukaryotic protein kinases (ePKs) and the atypical protein ki
Publikováno v:
Molbank, Vol 2020, Iss M1161, p M1161 (2020)
A routine synthesis was performed to furnish the title compound which incorporates a versatile difluoromethyl group on the aniline substitution of a 4-anilinoquinoline kinase inhibitor motif. In addition, the small molecule crystal structure (of the