1334320-19-2Relevant academic research and scientific papers
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors
Yan, Zi-Hong,Huang, Xia-Yun,Wu, Hai-Qiu,Chen, Wen-Xue,He, Qiu-Qin,Chen, Fen-Er,De Clercq, Erik,Pannecouque, Christophe
, p. 2535 - 2541 (2014/05/06)
A series of CR2(OH)-diarylpyrimidine derivatives (CR 2(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 cultur
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors
Yan, Zi-Hong,Wu, Hai-Qiu,Chen, Wen-Xue,Wu, Yan,Piao, Hu-Ri,He, Qiu-Qin,Chen, Fen-Er,De Clercq, Erik,Pannecouque, Christophe
, p. 3220 - 3226 (2014/06/09)
A series of new diarylpyrimidines (DAPYs) characterized by a halogen atom on the methylene linker between wing I and the central pyrimidine ring was synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures. The two most promising compou
Design and synthesis of a new series of cyclopropylamino-linking diarylpyrimidines as HIV non-nucleoside reverse transcriptase inhibitors
Liu, Yang,Meng, Ge,Zheng, Aqun,Chen, Fener,Chen, Wenxue,Clercq, Erik De,Pannecouque, Christophe,Balzarini, Jan
, p. 334 - 341 (2014/07/22)
A new series of 29 diarylpyrimidine analogues featuring a cyclopropylamino group between the pyrimidine scaffold and the aryl wing have been synthesized. All of the new compounds have been characterized by spectra analysis. The target molecules were evalu
Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs
Gu, Shuang-Xi,He, Qiu-Qin,Yang, Shi-Qiong,Ma, Xiao-Dong,Chen, Fen-Er,Clercq, Erik De,Balzarini, Jan,Pannecouque, Christophe
, p. 5117 - 5124 (2011/10/04)
A series of 26 diarylpyrimidines, characterized by the hydroxymethyl linker between the left wing benzene ring and the central pyrimidine, were synthesized and evaluated for in vitro anti-HIV activity. Most of the compounds exhibited moderate to excellent
Synthesis and Anti-HIV Activity of Aryl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazones as Potent Non-nucleoside Reverse Transcriptase Inhibitors
Ma, Xiao-Dong,Yang, Shi-Qiong,Gu, Shuang-Xi,He, Qiu-Qin,Chen, Fen-Er,DeClercq, Erik,Balzarini, Jan,Pannecouque, Christophe
scheme or table, p. 2225 - 2232 (2012/04/11)
A series of novel diarylpyrimidines (DAPYs) with a ketone hydrazone substituent on the methylene linker between the pyrimidine nucleus and the aryl moiety at the C-4 position were synthesized, and their antiviral activity against human immunodeficiency virus (HIV)-1 in MT-4 cells was evaluated. Most compounds of this class exhibited excellent activity against wild-type HIV-1, with EC50 values in the range of 1.7-13.2nM. Of these compounds, 2-bromophenyl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazone (9k) displayed the most potent anti-HIV-1 activity (EC50=1.7±0.6nM), with excellent selectivity for infected over uninfected cells (SI=5762). In addition, the 4-methyl phenyl analogue 9d (EC50=2.4±0.2nM, SI=18461) showed broad spectrum HIV inhibitory activity, with EC50 values of 2.4±0.2nM against wild-type HIV-1, 5.3±0.4μM against HIV-1 double-mutated strain RES056 (K103N+Y181C), and 5.5μM against HIV-2 ROD strain. Furthermore, structure-activity relationship (SAR) data and molecular modeling results for these compounds are also discussed. Antiviral agents: A series of new diarylpyrimidine (DAPY) derivatives with a ketone hydrazine substituent on the CH2 linker between the pyrimidine nucleus and the phenyl ring were synthesized, and their anti-HIV activity in MT-4 cells was evaluated. Most compounds of this class exhibited excellent activity against wild-type HIV-1, with EC50 values in the range of 1.7-13.2nM.
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV
Feng, Xiao-Qing,Zeng, Zhao-Sen,Liang, Yong-Hong,Chen, Fen-Er,Pannecouque, Christophe,Balzarini, Jan,Clercq, Erik De
experimental part, p. 2370 - 2374 (2010/06/16)
A series of novel diarylpyrimidine analogues featuring a hydroxyiminomethyl group between the pyrimidine scaffold and the aryl wing I have been synthesized and tested in MT-4 cells culture as non-nucleoside reverse transcriptase inhibitors against human immunodeficiency virus (HIV). Most of these new congeners exhibited moderate to excellent activity against wild-type virus with an EC50 value ranging from 0.569 μM to 0.005 μM. 4-(4-((Hydroxyimino) (3-methoxyphenyl)methyl)pyrimidin-2-ylamino)benzonitrile (12n) was identified as the most active compound of this new series (EC50 = 0.025 μM, SI >1223) associated with moderate activity against HIV-1 double mutant strains (K103N + Y181C) (EC50 = 8.72 μM) in addition to its anti-HIV-2 activity with an EC50 value of 8.31 μM. Preliminary structure-activity relationship (SAR) among the newly synthesized DAPYs was also investigated.
