Results 101 to 110 of about 400 (184)

Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR

Bioorganic & Medicinal Chemistry, 2017
30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing α of DAPYs.
Huan-Huan Lu, Ping Xue, Yuan‐Yuan Zhu, Xiu-Lian Ju, Xiaojiao Zheng, Xun Zhang, Ting Xiao, Christophe Pannecouque, Tingting Li, Shuang‐Xi Gu   +9 more
semanticscholar   +3 more sources

Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors

Bioorganic & Medicinal Chemistry, 2014
A series of CR2(OH)-diarylpyrimidine derivatives (CR2(OH)-DAPYs) featuring a hydrophobic group at CH(OH) linker between wing I and the central pyrimidine were synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures.
Zihong Yan, Xiayun Huang, Hai-Qiu Wu, Wenxue Chen, Qiuqin He, Fen‐Er Chen, Erik De Clercq, Christophe Pannecouque   +7 more
semanticscholar   +3 more sources

A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities

Bioorganic & Medicinal Chemistry, 2015
To improve the conformational flexibility and positional adaptability of the traditional diarylpyrimidines (DAPYs), a family of diarylpyrimidines featuring a C-N diatomic linker between the left wing benzene ring and the central pyrimidine was firstly ...
Shuang‐Xi Gu, Heng Qiao, Yuan‐Yuan Zhu, Qi-Chao Shu, Hui Liu, Xiu-Lian Ju, Erik De Clercq, Jan Balzarini, Christophe Pannecouque   +8 more
semanticscholar   +3 more sources

Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization

European journal of medicinal chemistry, 2017
A novel series of uracil-bearing DAPYs derivatives were designed and synthesized via structure-based molecular hybridization to discover compounds with improved anti-resistance profiles. Anti-HIV activity of the designed compounds was tested in MT-4 cell
Heng Zhang, Ye Tian, Dongwei Kang, Zhipeng Huo, Zhongxia Zhou, Huiqing Liu, Erik De Clercq, Christophe Pannecouque, Peng Zhan, Xinyong Liu   +9 more
semanticscholar   +3 more sources

Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors

European journal of medicinal chemistry, 2019
The fragment hopping approach is widely applied in drug development. A series of diarylpyrimidines (DAPYs) were obtained by hopping the thioacetamide scaffold to novel human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase ...
Sheng Han, Ya-Li Sang, Yan Wu, Yuan Tao, Christophe Pannecouque, Erik De Clercq, Chunlin Zhuang, Fen‐Er Chen   +7 more
semanticscholar   +3 more sources

Follow on-based optimization of the biphenyl-DAPYs as HIV-1 nonnucleoside reverse transcriptase inhibitors against the wild-type and mutant strains

Bioorganic chemistry (Print), 2019
The present work follows our preliminary discovery of biphenyl diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. Further structural optimization of biphenyl-DAPYs led to the identification of a new series of biphenyl ...
Ya-Li Sang, Sheng Han, Shuwen Han, Christophe Pannecouque, Erik De Clercq, Chunlin Zhuang, Fen‐Er Chen   +6 more
semanticscholar   +3 more sources

Fragment Addition-Based Design of Heteroaromatic-Biphenyl-DAPYs as Potent and Orally Available Non-nucleoside Reverse Transcriptase Inhibitors Featuring Significantly Enhanced Safety

Journal of Medicinal Chemistry
Our previously disclosed biphenyl-DAPY 3 emerged as a potent inhibitor against WT HIV-1 and various mutant strains. Yet, its journey toward clinical application was thwarted by pronounced cytotoxicity and low selectivity (CC50 = 6 μM, SI = 3515).
Wenjuan Huang, Christophe Pannecouque, Erik De Clercq, Shuai Wang, Fen‐Er Chen   +4 more
openalex   +2 more sources

Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles.

Journal of Medicinal Chemistry, 2019
Diarylpyrimidine derivatives (DAPYs) exhibit robust anti-HIV-1 potency, although they have been compromised by E138K variant and severe side-effects and been suffering from poor water solubility.
Boshi Huang, Wenmin Chen, Tong Zhao, Zhenyu Li, Xiangyi Jiang, Tiziana Ginex, David Vílchez, F. Luque, Dongwei Kang, Ping Gao, Jian Zhang, Ye Tian, D. Daelemans, E. De Clercq, C. Pannecouque, P. Zhan, Xinyong Liu   +16 more
semanticscholar   +5 more sources

Recent Advances in DAPYs and Related Analogues as HIV-1 NNRTIs

Current Medicinal Chemistry, 2011
HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) nowadays represent most promising anti-AIDS drugs that specifically inhibit HIV-1 reverse transcriptase (RT).
Xuwang Chen, Peng Zhan, Dongyue Li, Erik De Clercq, Xinyong Liu   +4 more
openalex   +2 more sources

Fragment Hopping-Based Design of Novel Biphenyl-DAPY Derivatives as Potent Non-Nucleoside Reverse Transcriptase Inhibitors Featuring Significantly Improved Anti-Resistance Efficacy

Journal of Medicinal Chemistry, 2023
To enhance the anti-resistance efficacy of our previously reported non-nucleoside reverse transcriptase inhibitor (NNRTI) 4, a series of novel biphenyl-DAPY derivatives were developed using the fragment-hopping strategy.
Ya-Li Sang, Christophe Pannecouque, Erik De Clercq, Shuai Wang, Fen‐Er Chen   +4 more
openalex   +2 more sources