Development of Potent Mcl-1 Inhibitors: Structural Investigations on Macrocycles Originating from a DNA-Encoded Chemical Library Screen.

Autor: Hekking KFW; Symeres, 6546BB Nijmegen, The Netherlands., Maroto S; Symeres, 6546BB Nijmegen, The Netherlands., van Kekem K; Symeres, 6546BB Nijmegen, The Netherlands., Haasjes FS; Symeres, 6546BB Nijmegen, The Netherlands., Slootweg JC; Symeres, 6546BB Nijmegen, The Netherlands., Oude Alink PGB; Symeres, 6546BB Nijmegen, The Netherlands., Dirks R; Symeres, 6546BB Nijmegen, The Netherlands., Sardana M; Symeres, 6546BB Nijmegen, The Netherlands., Bolster MG; Symeres, 6546BB Nijmegen, The Netherlands., Kuijpers B; Symeres, 6546BB Nijmegen, The Netherlands., Smith D; Symeres, 6546BB Nijmegen, The Netherlands., Doodeman R; Symeres, 6546BB Nijmegen, The Netherlands., Scheepstra M; Symeres, 6546BB Nijmegen, The Netherlands., Zech B; X-Rx, Inc., New York, New York 10016, United States., Mulvihill M; X-Rx, Inc., New York, New York 10016, United States., Renzetti LM; X-Rx, Inc., New York, New York 10016, United States., Babiss L; X-Rx, Inc., New York, New York 10016, United States., Centrella PA; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Clark MA; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Cuozzo JW; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Guié MA; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Sigel E; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Habeshian S; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Hupp CD; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Liu J; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Thomson HA; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Zhang Y; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Keefe AD; X-Chem, Inc., Waltham, Massachusetts 02453, United States., Müller G; Symeres, 6546BB Nijmegen, The Netherlands., Gremmen S; Symeres, 6546BB Nijmegen, The Netherlands.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2024 Feb 22; Vol. 67 (4), pp. 3039-3065. Date of Electronic Publication: 2024 Feb 02.

Discovery of 2,4-1 H -Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors.

Autor: Veerman JJN; ZoBio BV, J.H. Oortweg 19, 2333 CH Leiden, The Netherlands., Bruseker YB; Mercachem BV, Department of Medicinal Chemistry, Kerkenbos 1013, 6546 BB Nijmegen, The Netherlands., Damen E; Mercachem BV, Department of Medicinal Chemistry, Kerkenbos 1013, 6546 BB Nijmegen, The Netherlands., Heijne EH; Mercachem BV, Department of Medicinal Chemistry, Kerkenbos 1013, 6546 BB Nijmegen, The Netherlands., van Bruggen W; Mercachem BV, Department of Medicinal Chemistry, Kerkenbos 1013, 6546 BB Nijmegen, The Netherlands., Hekking KFW; Mercachem BV, Department of Medicinal Chemistry, Kerkenbos 1013, 6546 BB Nijmegen, The Netherlands., Winkel R; Mercachem BV, Department of Medicinal Chemistry, Kerkenbos 1013, 6546 BB Nijmegen, The Netherlands., Hupp CD; X-Chem, Inc., 100 Beaver Street, Waltham, Massachusetts 02453, United States., Keefe AD; X-Chem, Inc., 100 Beaver Street, Waltham, Massachusetts 02453, United States., Liu J; Civetta Therapeutics, 10 Wilson Road, Cambridge, Massachusetts 02138, United States., Thomson HA; X-Chem, Inc., 100 Beaver Street, Waltham, Massachusetts 02453, United States., Zhang Y; X-Chem, Inc., 100 Beaver Street, Waltham, Massachusetts 02453, United States., Cuozzo JW; X-Chem, Inc., 100 Beaver Street, Waltham, Massachusetts 02453, United States., McRiner AJ; X-Chem, Inc., 100 Beaver Street, Waltham, Massachusetts 02453, United States., Mulvihill MJ; HiberCell Inc., New York, New York 10019, United States., van Rijnsbergen P; Mercachem BV, Department of Medicinal Chemistry, Kerkenbos 1013, 6546 BB Nijmegen, The Netherlands., Zech B; AnavoTherapeutics BV, J.H. Oortweg 19, 2333 CH Leiden, The Netherlands., Renzetti LM; Bridge Medicines LLC, New York, New York 10017, United States., Babiss L; Wilmington, North Carolina 28405, United States., Müller G; AnavoTherapeutics BV, J.H. Oortweg 19, 2333 CH Leiden, The Netherlands.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2021 Mar 03; Vol. 12 (4), pp. 555-562. Date of Electronic Publication: 2021 Mar 03 (Print Publication: 2021).

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Discovery of dual kinase inhibitors targeting VEGFR2 and FAK: structure-based pharmacophore modeling, virtual screening, and molecular docking studies.

Autor: Fouad, Marwa A.^1,2 (AUTHOR) marwa.fouad@pharma.cu.edu.eg, Osman, Alaa A.² (AUTHOR), Abdelhamid, Noha M.² (AUTHOR), Rashad, Mai W.² (AUTHOR), Nabawy, Ashrakat Y.² (AUTHOR), El Kerdawy, Ahmed M.^1,2,3 (AUTHOR)

Publikováno v: BMC Chemistry. 2/16/2024, Vol. 18 Issue 1, p1-20. 20p.

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