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Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads.
RSC Med Chem. 2022 Jun 3;13(8):963-969. doi: 10.1039/d2md00095d. eCollection 2022 Aug 17.
RSC Med Chem. 2022.
PMID: 36092148
Free PMC article.
Structural Re-engineering of the α-Helix Mimetic JY-1-106 into Small Molecules: Disruption of the Mcl-1-Bak-BH3 Protein-Protein Interaction with 2,6-Di-Substituted Nicotinates.
Drennen B, Scheenstra JA, Yap JL, Chen L, Lanning ME, Roth BM, Wilder PT, Fletcher S.
Drennen B, et al.
ChemMedChem. 2016 Apr 19;11(8):827-33. doi: 10.1002/cmdc.201500461. Epub 2016 Feb 4.
ChemMedChem. 2016.
PMID: 26844930
Free PMC article.
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Rationally Designed Polypharmacology: α-Helix Mimetics as Dual Inhibitors of the Oncoproteins Mcl-1 and HDM2.
Conlon IL, Drennen B, Lanning ME, Hughes S, Rothhaas R, Wilder PT, MacKerell AD Jr, Fletcher S.
Conlon IL, et al. Among authors: drennen b.
ChemMedChem. 2020 Sep 16;15(18):1691-1698. doi: 10.1002/cmdc.202000278. Epub 2020 Jun 25.
ChemMedChem. 2020.
PMID: 32583936
Free PMC article.
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Structure-based design of 3-carboxy-substituted 1,2,3,4-tetrahydroquinolines as inhibitors of myeloid cell leukemia-1 (Mcl-1).
Chen L, Wilder PT, Drennen B, Tran J, Roth BM, Chesko K, Shapiro P, Fletcher S.
Chen L, et al. Among authors: drennen b.
Org Biomol Chem. 2016 Jun 28;14(24):5505-10. doi: 10.1039/c5ob02063h. Epub 2016 Jan 11.
Org Biomol Chem. 2016.
PMID: 26751150
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Towards more drug-like proteomimetics: two-faced, synthetic α-helix mimetics based on a purine scaffold.
Lanning ME, Wilder PT, Bailey H, Drennen B, Cavalier M, Chen L, Yap JL, Raje M, Fletcher S.
Lanning ME, et al. Among authors: drennen b.
Org Biomol Chem. 2015 Aug 28;13(32):8642-6. doi: 10.1039/c5ob00478k. Epub 2015 Jul 24.
Org Biomol Chem. 2015.
PMID: 26204921
Free PMC article.
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