Discovery of novel 1,4-disubstituted 1,2,3-triazole phenylalanine derivatives as HIV-1 capsid inhibitors.

CuAAC HIV-1 HIV-1 capsid protein Molecular dynamics simulation Phenylalanine derivatives SAR Surface plasmon resonance

Journal

RSC advances
ISSN: 2046-2069
Titre abrégé: RSC Adv
Pays: England
ID NLM: 101581657

Informations de publication

Date de publication:
2019
Historique:
entrez: 25 2 2020
pubmed: 25 2 2020
medline: 25 2 2020
Statut: ppublish

Résumé

The HIV-1 capsid (CA) protein plays crucial roles in both early and late stages of the viral life cycle, which has intrigued researchers to target it to develop anti-HIV drugs. Accordingly, in this research, we report the design, synthesis and biological evaluation of a series of novel phenylalanine derivatives as HIV-1 CA protein inhibitors using the Cu(I)-catalyzed azide and alkyne 1,3-dipolar cycloaddition (CuAAC) reaction. Among this series of inhibitors, compound

Identifiants

pubmed: 32089839
doi: 10.1039/c9ra05869a
pmc: PMC7034945
mid: NIHMS1051249
doi:

Types de publication

Journal Article

Langues

eng

Pagination

28961-28986

Subventions

Organisme : NIGMS NIH HHS
ID : R01 GM125396
Pays : United States
Organisme : NIMH NIH HHS
ID : T32 MH079785
Pays : United States

Déclaration de conflit d'intérêts

Notes The authors declare no competing financial interest.

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Auteurs

Xiangyi Jiang (X)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.

Gaochan Wu (G)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.

Waleed A Zalloum (WA)

Department of Pharmacy, Faculty of Health Science, /Department of pharmacy, American University of Madaba, P.O Box 2882, Amman, 11821, Jordan.

Megan E Meuser (ME)

Department of Biochemistry & Molecular Biology, Drexel University College of Medicine, Philadelphia, PA, USA.

Alexej Dick (A)

Department of Biochemistry & Molecular Biology, Drexel University College of Medicine, Philadelphia, PA, USA.

Lin Sun (L)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.

Chin-Ho Chen (CH)

Duke University Medical Center, Box 2926, Surgical Oncology Research Facility, Durham, NC, 27710, USA.

Dongwei Kang (D)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.

Lanlan Jing (L)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.

Ruifang Jia (R)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.

Simon Cocklin (S)

Department of Biochemistry & Molecular Biology, Drexel University College of Medicine, Philadelphia, PA, USA.

Kuo-Hsiung Lee (KH)

Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, 27599, USA.

Xinyong Liu (X)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.

Peng Zhan (P)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.

Classifications MeSH