1140520-11-1Relevant articles and documents
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase
Wu, Hai-Qiu,Yao, Jin,He, Qiu-Qin,Chen, Wen-Xue,Chen, Fen-Er,Pannecouque, Christophe,De Clercq, Erik,Daelemans, Dirk
, p. 624 - 631 (2015)
A series of new DAPY-DPEs hybrids, combined the important pharmacophores of DAPYs and DPEs, has been synthesized and biologically evaluated for their anti-HIV activities against wild-type HIV-1 strain IIIB, double RT mutant (K103N + Y181C) strain RES056 and HIV-2 strain ROD in MT-4 cell cultures. Many promising candidates with potent inhibitory activity (wild-type) within the EC50 range from 0.16 to 0.013 μM were obtained. In particular, 3c, 3p, 3r and 3s displayed low nM level EC50 values (35, 13, 50 and 17 nM, respectively) and high selectivity (9342, 25131, 2890 and 11338, respectively), which were much more potent than NVP (EC50 = 0.31 μM, SI = 48), 3TC (EC50 = 2.24 μM, SI > 39), DDI (EC50 = 23.20 μM, SI > 9) and DLV (EC50 = 0.65 μM, SI > 67), and comparable to AZT (EC50 = 0.0071 μM, SI > 13144) and EFV (EC50 = 0.0062 μM, SI > 1014). The HIV-1 reverse transcriptase inhibitory assay confirmed that these DAPY-DPEs hybrids targeted HIV-1 RT. Molecular simulation was performed to investigate the potential binding mode of the newly synthesized compounds. And reasonable explanation for the activity results was discussed with docking method.
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
Lead optimization of diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase
Zeng, Zhao-Sen,Liang, Yong-Hong,Feng, Xiao-Qing,Chen, Fen-Er,Pannecouque, Christophe,Balzarini, Jan,De Clercq, Erik
scheme or table, p. 837 - 840 (2011/02/24)
Antiviral agents: A series of CN-CH2-DAPY analogues were identified as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs) against HIV-1. Most of the newly synthesized compounds exhibited strong activity against wild-type HIV-1.
