Discovery of novel [1,2,4]triazolo[4,3-a]quinoxaline aminophenyl derivatives as BET inhibitors for cancer treatment.

Ali, Imran; Lee, Jooyun; Go, Areum; Choi, Gildon; Lee, Kwangho

Ali, Imran; Lee, Jooyun; Go, Areum; Choi, Gildon; Lee, Kwangho.

Affiliation

Ali I; Bio-Organic Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Daejeon 34114, Republic of Korea; Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, Republic of Korea.
Lee J; Bio-Organic Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Daejeon 34114, Republic of Korea.
Go A; Bio-Organic Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Daejeon 34114, Republic of Korea; Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, Republic of Korea.
Choi G; Bio-Organic Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Daejeon 34114, Republic of Korea; Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, Republic of Korea. Electronic address: gchoi@krict.re.kr.
Lee K; Bio-Organic Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Daejeon 34114, Republic of Korea; Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, Republic of Korea. Electronic address: kwangho@krict.re.kr.

Bioorg Med Chem Lett ; 27(20): 4606-4613, 2017 10 15.

Article in En | MEDLINE | ID: mdl-28939121

Subject(s)

Antineoplastic Agents/chemistry; Neoplasms/drug therapy; Nuclear Proteins/antagonists & inhibitors; Quinoxalines/chemistry; Animals; Antineoplastic Agents/pharmacokinetics; Antineoplastic Agents/pharmacology; Antineoplastic Agents/therapeutic use; Binding Sites; Cell Cycle Checkpoints/drug effects; Cell Line, Tumor; Drug Evaluation, Preclinical; Half-Life; Humans; Inhibitory Concentration 50; Molecular Docking Simulation; Nuclear Proteins/metabolism; Protein Structure, Tertiary; Proto-Oncogene Proteins c-myc/metabolism; Quinoxalines/pharmacokinetics; Quinoxalines/pharmacology; Quinoxalines/therapeutic use; Rats; Structure-Activity Relationship; Triazoles/chemistry

Key words

BET; BRD4; Bromodomains; Cancer; Epigenetic readers; Triazoloquinoxaline; [1,2,4]Triazolo[4,3-a]quinoxaline

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Full text: 1 Database: MEDLINE Main subject: Quinoxalines / Nuclear Proteins / Neoplasms / Antineoplastic Agents Language: En Journal: Bioorg Med Chem Lett Year: 2017 Type: Article

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