BIOMAT Database Logo BIOMAT Database Logo

Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors. 2010

Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China.

Nine newly 6-cyano-2-naphthyl substituted diarylpyrimidines (DAPY) were synthesized as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. The antiviral and cytotoxicity evaluation indicated that these compounds displayed strong activity against wild-type HIV-1 at nanomolar concentrations with selectivity index SI greater than 23 779. The most active compounds 3c and 3e exhibited activity against the double mutant (103N+181C) strains at an EC₅₀ of 0.16 and 0.15 μM, and were more activity than that of efavirenz.

UI MeSH Term Description Entries
D009284 Naphthols Naphthalene derivatives carrying one or more hydroxyl (-OH) groups at any ring position. They are often used in dyes and pigments, as antioxidants for rubber, fats, and oils, as insecticides, in pharmaceuticals, and in numerous other applications. Hydroxynaphthalene,Hydroxynaphthalenes,Naphthol
D011743 Pyrimidines A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D003198 Computer Simulation Computer-based representation of physical systems and phenomena such as chemical processes. Computational Modeling,Computational Modelling,Computer Models,In silico Modeling,In silico Models,In silico Simulation,Models, Computer,Computerized Models,Computer Model,Computer Simulations,Computerized Model,In silico Model,Model, Computer,Model, Computerized,Model, In silico,Modeling, Computational,Modeling, In silico,Modelling, Computational,Simulation, Computer,Simulation, In silico,Simulations, Computer
D003521 Cyclopropanes Three-carbon cycloparaffin cyclopropane (the structural formula (CH2)3) and its derivatives.
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000480 Alkynes Hydrocarbons with at least one triple bond in the linear portion, of the general formula Cn-H2n-2. Acetylenic Compounds,Alkyne,Acetylenes
D001665 Binding Sites The parts of a macromolecule that directly participate in its specific combination with another molecule. Combining Site,Binding Site,Combining Sites,Site, Binding,Site, Combining,Sites, Binding,Sites, Combining
D015497 HIV-1 The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte. Human immunodeficiency virus 1,HIV-I,Human Immunodeficiency Virus Type 1,Immunodeficiency Virus Type 1, Human
D048588 Benzoxazines OXAZINES with a fused BENZENE ring. Benzoxazine,Benzoxazinoid,Benzoxazinone,Benzoxazinones,Benzoxazinoids

Related Publications

Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Design, synthesis, and SAR of naphthyl-substituted Diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
September 2009, ChemMedChem,
Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
August 2011, Bioorganic & medicinal chemistry,
Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
February 2015, Bioorganic & medicinal chemistry,
Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Molecular Modeling, Synthesis, and Anti-HIV Activity of Novel Isoindolinedione Analogues as Potent Non-nucleoside Reverse Transcriptase Inhibitors.
February 2016, Chemical biology & drug design,
Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
July 2013, European journal of medicinal chemistry,
Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
November 2019, European journal of medicinal chemistry,
Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Non-nucleoside HIV reverse transcriptase inhibitors, Part 6[1]: synthesis and anti-HIV activity of novel 2-[(arylcarbonylmethyl)thio]-6-arylthio DABO analogues.
October 2005, Archiv der Pharmazie,
Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
February 2014, Bioorganic & medicinal chemistry,
Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.
February 2019, ACS medicinal chemistry letters,
Yong-Hong Liang, and Qiu-Qin He, and Zhao-Sen Zeng, and Zhi-Qian Liu, and Xiao-Qing Feng, and Fen-Er Chen, and Jan Balzarini, and Christophe Pannecouque, and Erik De Clercq
Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.
February 2009, Yao xue xue bao = Acta pharmaceutica Sinica,
Copied contents to your clipboard!