1-Phenyl-1H-indole derivatives as a new class of Bcl-2/Mcl-1 dual inhibitors: Design, synthesis, and preliminary biological evaluation
Copyright policy )1-Phenyl-1H-indole derivatives as a new class of Bcl-2/Mcl-1 dual inhibitors: Design, synthesis, and preliminary biological evaluation
Bcl-2 proteins, such as B-cell lymphoma (Bcl-2) protein, myeloid cell leukemia sequence 1 (Mcl-1) protein, has been implicated in the progression and survival of multiple tumor types and become a validated and attractive target for cancer therapy. In this work, a series of 1-phenyl-1H-indole derivatives has been designed and synthesized. The preliminary biological studies (binding assay for Bcl-2 proteins and MTT assay) suggested that some active compounds showed potent inhibitory activities on Bcl-2/Mcl-1 without binding on Bcl-XL. Furthermore, Compound 9c and 9h showed better anti-proliferative activity than WL-276.
- Shandong Women’s University China (People's Republic of)
Indoles, Dose-Response Relationship, Drug, Molecular Structure, Antineoplastic Agents, Molecular Docking Simulation, Structure-Activity Relationship, Proto-Oncogene Proteins c-bcl-2, Cell Line, Tumor, Drug Design, Humans, Myeloid Cell Leukemia Sequence 1 Protein, Drug Screening Assays, Antitumor, Cell Proliferation
Indoles, Dose-Response Relationship, Drug, Molecular Structure, Antineoplastic Agents, Molecular Docking Simulation, Structure-Activity Relationship, Proto-Oncogene Proteins c-bcl-2, Cell Line, Tumor, Drug Design, Humans, Myeloid Cell Leukemia Sequence 1 Protein, Drug Screening Assays, Antitumor, Cell Proliferation
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