Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity

Cited by (195)

Items 101–195 of 195

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2. Chemical parsing: Dissecting cell dependencies with a toolkit of selective BCL-2 family inhibitors
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3. Antibody fragments structurally enable a drug-discovery campaign on the cancer target Mcl-1
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5. Discovery of N -sulfonylated aminosalicylic acids as dual MCL-1/BCL-xL inhibitors
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6. Discovery of novel biaryl sulfonamide based Mcl-1 inhibitors
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8. Mitochondria Localized Anticancer Iridium(III) Prodrugs for Targeted Delivery of Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors and Cytotoxic Iridium(III) Complex
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9. Structure-based Virtual screening, Biological Evaluation and Biophysical Study of Novel Mcl-1 Inhibitors
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10. Exploring indole derivatives as myeloid cell leukaemia-1 (Mcl-1) inhibitors with multi-QSAR approach: a novel hope in anti-cancer drug discovery
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11. Peptide-Based Targeted Covalent Inhibitors
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12. Chemical dissection of selective myeloid leukemia-1 inhibitors: How they were found and evolved
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13. Binding mode of Pyridoclax to myeloid cell leukemia-1 (Mcl-1) revealed by nuclear magnetic resonance spectroscopy, docking and molecular dynamics approaches
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14. Optimization of Benzothiazole and Thiazole Hydrazones as Inhibitors of Schistosome BCL-2
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15. Design, synthesis and biological evaluation of dual Bcl-2/Mcl-1 inhibitors bearing 2-(1H-indol-4-yl)benzoic acid scaffold
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16. In Vivo, In Vitro and In Silico Anticancer Activity of Ilama Leaves: An Edible and Medicinal Plant in Mexico
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17. Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites
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18. Induction of apoptosis by MCL-1 inhibitors in chronic lymphocytic leukemia cells
    Lisa S. Chen, Michael J. Keating, William G. Wierda, Varsha V. Gandhi · 2019 · Leukemia & lymphoma/Leukemia and lymphoma
19. Discovery of Phenylpyrazole Derivatives as a New Class of Selective Inhibitors of MCL‑1 with Antitumor Activity
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20. The Effect of Core Replacement on S64315, a Selective MCL-1 Inhibitor, and Its Analogues
    Szabolcs Sipos, Balázs Bálint, Zoltán B. Szabó, Levente Ondi, Márton Csékei, Zoltán Szlávik, Ágnes Proszenyák, James B. Murray, James E. P. Davidson, I‐Jen Chen et al. · 2021 · ACS Omega
21. Inhibition of cyclin‐dependent kinase 9 synergistically enhances venetoclax activity in mantle cell lymphoma
    Xiaoxian Zhao, Juraj Bodo, Ruoying Chen, Lisa M. Durkin, Andrew James Souers, Darren C. Phillips, Eric D. Hsi · 2020 · eJHaem
22. Recent Advances in the Development of Selective Mcl-1 Inhibitors for the Treatment of Cancer (2017-Present)
    Ying Fan, Xuben Hou, Hao Fang · 2020 · Recent Patents on Anti-Cancer Drug Discovery
23. Modeling the Binding of Anticancer Peptides and Mcl-1
    Shamsa Husain Ahmed Alhammadi, Bincy Baby, Priya Antony, Amie Jobe, Raghad Salman Mohammed Humaid, Fatema Jumaa Ahmed Alhammadi, Ranjit Vijayan · 2024 · International Journal of Molecular Sciences
24. Synthesis, Anti-Cancer Activity, Cell Cycle Arrest, Apoptosis Induction, and Docking Study of Fused Benzo[h]chromeno[2,3-d]pyrimidine on Human Breast Cancer Cell Line MCF-7
    Zainab M. Khoder, Mosaad Sayed Mohamed, Samir M. Awad, Amal Fathi Gharib, Omnia Aly, Marwa Abd El-Fattah Khodair, Samar Said Fatahala, Rania Helmy Abd El-Hameed · 2024 · Molecules
25. Recent advances of small-molecule Mcl-1 inhibitors or degraders as promising anti-cancer agents (2018-present)
    Hongjuan Chen, Zixue Yan, Changqing Xiao, Zilong Tang, Yichao Wan · 2025 · European Journal of Medicinal Chemistry
26. Apoptosis as a Therapeutic Target in Chronic Lymphocytic Leukemia
    Christian Billard · 2015 · Lymphoma and Chronic Lymphocytic Leukemias
27. Crystal structure of Mcl-1 in complex with compound 65
    A.V. Toms, Bruce Follows · 2019 · Worldwide Protein Data Bank
28. In silico approaches to identify novel myeloid cell leukemia-1 (Mcl-1) inhibitors for treatment of cancer
    Ji-Xia Ren, Chengping Li, Xiuling Zhou, Xuesong Cao, Yong Xie · 2017 · Journal of Biomolecular Structure and Dynamics
29. Substituted indole Mcl-1 inhibitors: a patent evaluation (WO2015148854A1)
    Ting Song, Ziqian Wang, Zhichao Zhang · 2016 · Expert Opinion on Therapeutic Patents
30. Faculty Opinions recommendation of Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia.
    Andrew P. Gilmore · 2019 · Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature
31. Design, synthesis, and antitumor activity of matrine aminophosphonate derivatives as potent mcl-1 inhibitors
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32. Progress on Mcl-1 small molecule inhibitors
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33. Melatonin sensitizes leukemia cells to the MCL1 inhibitors S63845 and A‐1210477 through multiple pathways
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34. Peptide‐Directed Binding for the Discovery of Modulators of α‐Helix‐Mediated Protein–Protein Interactions: Proof‐of‐Concept Studies with the Apoptosis Regulator Mcl‐1
    Andrew Michael Beekman, Maria Anne O'Connell, Lesley A. Howell · 2017 · Angewandte Chemie
35. Close encounter of the covalent kind: Inhibiting MCL1’s proapoptotic activity with covalent inhibitors
    Guillaune Lessene · 2017 · Cell Death Discovery
36. Development and Characterization of Novel Mcl-1 Inhibitors for Treatment of Cancer.
    Ahmed S.A. Mady · 2016 · Deep Blue (University of Michigan)
37. Pharmacologic Features of Drugs Targeting BCL 2 Family Members
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38. Understanding Structural And Functional Mechanisms of Emi1 Inhibition of the Anaphase Promoting Complex
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39. Selective Small Molecule Myeloid Cell Leukemia-1 (MCL-1) Inhibitors: Novel Agents in Cancer Therapy
    Hoda Ibrahim, Deena S. Lasheen, Rabah A.T. Serya, Dalal Abu-ELElla · 2019 · Archives of Pharmaceutical Sciences Ain Shams University
40. Inhibition of Cyclin Dependent Kinase 9 Synergistically Enhanced Venetoclax Activity in Mantle Cell Lymphoma Cells
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41. Discovery and Development of Mcl-1 Inhibitors as Anti-cancer Therapeutics: Hit to Clinical Candidate Optimization
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42. Monte Carlo Optimization-Based QSAR Study of Some Indole-Based Mcl-1 Inhibitors
    Sudipta Nandi, Kalyan Ghosh, Anju Rathore, Adarsh Sahu, Shovanlal Gayen · 2021 · International Journal of Quantitative Structure-Property Relationships
43. Szelektív MCL-1 inhibitorok felfedezése
    András Kotschy · 2021 · Magyar kémiai folyóirat, Kémiai közlemények
44. 2-Oxy-3-Phenylacrylic Acid Derivatives as Potent Mcl-1 Inhibitors for Treatment of Cancer
    Jiayue Xi, Lin Yao, Ruyue Zhang, Ke Chen, Muqiong Li, Dongxu Zhang, Minxuan Cui, Huifang Nie, Pingan Wang, Xiaoye Li et al. · 2021 · Results in Chemistry
45. Faculty Opinions recommendation of Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).
    Varsha V. Gandhi, Prithviraj Bose · 2017 · Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature
46. Faculty Opinions recommendation of Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors.
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47. Theoretical Study on the Binding Properties of Inhibitors to Myeloid Cell Leukemia 1
    Youxin Cui · 2023 · Academic Journal of Medicine & Health Sciences
48. Structural analysis of apoptotic MCL1–HRK complex
    Jiaqi Wang, Longying Jiang, Hudie Wei · 2025 · Biochemical and Biophysical Research Communications
49. MCL1 may not mediate chemoresistance in cancer cells
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50. Small Molecule Inhibitors Targeting Protein–Protein Interactions in the BCL Protein
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51. Protein-protein interaction inhibitors in cancer
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52. Inhibition of BIRC5 and MCL-1 as a potential treatment strategy to overcome drug resistance in Mantle Cell Lymphoma
    Jeremiah C. Pfitzer, Sayak Chakravarti, Suman Mazumder, Fengzhi LI, Ujjal Kumar Mukherjee, Amit Mitra · 2026 · Blood Cancer Journal
53. Molecular basis of BCL2L10/Nrh oncogenic activity in breast cancer
    Adrien Nougarède · 2016 · theses.fr (ABES)
54. Development of new methodologies in organic synthesis for the preparation of bioactive molecules
    Marwa Hussein · 2017 · theses.fr (ABES)
55. Preparation of new fluorinated analogs of GABA and development of new inhibitors of antiapoptotic proteins with anticancer activity
    Ali Soulieman · 2021 · theses.fr (ABES)
56. Etude de la structure et la dynamique de Mcl-1 : application en cancérologie
    Mohammed B. Benabderrahmane · 2020 · theses.fr (ABES)
57. Développement de nouvelles stratégies thérapeutiques dans les cancers de l’ovaire : intérêt de l’inhibiteur d’HDAC belinostat, seul ou associé avec des molécules BH3-mimétiques, et recherche de stratégies ciblées mimant les mécanismes moléculaires médiateurs de son efficacité
    Cécilia Thomine · 2023 · theses.fr (ABES)
58. Discovery of a Novel Tetrahydro-β-Carboline Mcl-1 Inhibitor with Antitumor Activity and Capability to Overcome Cisplatin Resistance
    Dong-Yuan Ning, Ru-yi Luo, Li-Fang Cen, Fang‐Xin Wang, Yang-Han Liu, Yan‐Cheng Liu, Ya-Ni Huang, Hong Liang, Zhen‐Feng Chen · 2026 · Journal of Medicinal Chemistry
59. Development of highly selective, low-toxicity and orally available Mcl-1 inhibitors based on 3,5-dimethyl-4-sulfonimide-1H-pyrrole scaffold via P2/P3 dual pocket binding optimization
    Junjie Wang, Ke Xu, Pengju Zhu, Ziquan Zhao, Shuai Wen, Jinglong Zhao, Yabin Xin, Qidong You, Zhengyu Jiang, Mengchen Lu · 2026 · European Journal of Medicinal Chemistry
60. BindingDB Entry 50006386: Design, synthesis and preliminary biological studies of pyrrolidine derivatives as Mcl-1 inhibitors.
    BindingDB · 2020 · UC San Diego
61. BindingDB Entry 50015578: Interdiction at a protein-protein interface: MCL-1 inhibitors for oncology.
    BindingDB · 2023 · UC San Diego
62. BindingDB Entry 50047317: Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.
    BindingDB · 2017 · UC San Diego
63. BindingDB Entry 50045890: Progress in discovery of small-molecule modulators of protein-protein interactions via fragment screening.
    BindingDB · 2016 · UC San Diego
64. BindingDB Entry 50011578: Discovery of S64315, a Potent and Selective Mcl-1 Inhibitor.
    BindingDB · 2022 · UC San Diego
65. BindingDB Entry 50022746: Macrocyclic-based strategy in drug design: From lab to the clinic.
    BindingDB · 2026 · UC San Diego
66. BindingDB Entry 50008411: Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.
    BindingDB · 2021 · UC San Diego
67. BindingDB Entry 50047882: Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites.
    BindingDB · 2018 · UC San Diego
68. BindingDB Entry 50007010: Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands.
    BindingDB · 2021 · UC San Diego
69. BindingDB Entry 50021792: Histidine-Covalent Stapled Alpha-Helical Peptides Targeting hMcl-1.
    BindingDB · 2025 · UC San Diego
70. BindingDB Entry 50013663: Design, synthesis and biological evaluation of dual Bcl-2/Mcl-1 inhibitors bearing 2-(1H-indol-4-yl)benzoic acid scaffold.
    BindingDB · 2022 · UC San Diego
71. BindingDB Entry 50009085: The chemical biology of apoptosis: Revisited after 17 years.
    BindingDB · 2021 · UC San Diego
72. BindingDB Entry 50014937: Structure-Based Optimization of 3-Phenyl-
    BindingDB · 2023 · UC San Diego
73. BindingDB Entry 50012840: Discovery of a Copper-Based Mcl-1 Inhibitor as an Effective Antitumor Agent.
    BindingDB · 2022 · UC San Diego
74. BindingDB Entry 7582: Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain.
    BindingDB · 2016 · UC San Diego
75. BindingDB Entry 50018666: Sulfonamide derivatives as potential anti-cancer agents and their SARs elucidation.
    BindingDB · 2024 · UC San Diego
76. BindingDB Entry 50009080: From Inhibition to Degradation: Targeting the Antiapoptotic Protein Myeloid Cell Leukemia 1 (MCL1).
    BindingDB · 2021 · UC San Diego
77. BindingDB Entry 50019097: Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors.
    BindingDB · 2024 · UC San Diego
78. BindingDB Entry 50047293: Structure-based design of N-substituted 1-hydroxy-4-sulfamoyl-2-naphthoates as selective inhibitors of the Mcl-1 oncoprotein.
    BindingDB · 2017 · UC San Diego
79. BindingDB Entry 50007615: Indole: A privileged scaffold for the design of anti-cancer agents.
    BindingDB · 2021 · UC San Diego
80. BindingDB Entry 50020192: Macrocyclic Carbon-Linked Pyrazoles As Novel Inhibitors of MCL-1.
    BindingDB · 2024 · UC San Diego
81. BindingDB Entry 7798: hBfl-1/hNOXA Interaction Studies Provide New Insights on the Role of Bfl-1 in Cancer Cell Resistance and for the Design of Novel Anticancer Agents.
    BindingDB · 2017 · UC San Diego
82. BindingDB Entry 50000984: Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules.
    BindingDB · 2020 · UC San Diego
83. BindingDB Entry 50021046: Targeting Myeloid Leukemia-1 in Cancer Therapy: Advances and Directions.
    BindingDB · 2025 · UC San Diego
84. BindingDB Entry 50014471: Discovery of 3,5-Dimethyl-4-Sulfonyl-1
    BindingDB · 2022 · UC San Diego
85. BindingDB Entry 50022067: Discovery of Novel Mcl-1 Inhibitors with a 3-Substituted-1H-indole-1-yl Moiety Binding to the P1-P3 Pockets to Induce Apoptosis in Acute Myeloid Leukemia Cells.
    BindingDB · 2025 · UC San Diego
86. BindingDB Entry 50015492: Design, Synthesis, and Structural Characterization of Lysine Covalent BH3 Peptides Targeting Mcl-1.
    BindingDB · 2023 · UC San Diego
87. BindingDB Entry 50047579: DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites.
    BindingDB · 2017 · UC San Diego
88. BindingDB Entry 50023106: Chemical dissection of selective myeloid leukemia-1 inhibitors: How they were found and evolved.
    BindingDB · 2026 · UC San Diego
89. BindingDB Entry 50007644: Discovery and Characterization of 2,5-Substituted Benzoic Acid Dual Inhibitors of the Anti-apoptotic Mcl-1 and Bfl-1 Proteins.
    BindingDB · 2021 · UC San Diego
90. BindingDB Entry 50001688: Small-molecule Mcl-1 inhibitors: Emerging anti-tumor agents.
    BindingDB · 2020 · UC San Diego
91. BindingDB Entry 50008474: Hot-Spots of Mcl-1 Protein.
    BindingDB · 2021 · UC San Diego
92. BindingDB Entry 50048154: Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains.
    BindingDB · 2018 · UC San Diego
93. BindingDB Entry 50000004: Discovery and structure-activity relationship studies of N-substituted indole derivatives as novel Mcl-1 inhibitors.
    BindingDB · 2019 · UC San Diego
94. BindingDB Entry 50016046: Development of Mcl-1 inhibitors for cancer therapy.
    BindingDB · 2023 · UC San Diego
95. BindingDB Entry 50018416: Discovery of
    BindingDB · 2024 · UC San Diego