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Your search keyword '"Yan, Zi-Hong"' showing total 3 results
Start Over Author "Yan, Zi-Hong" Publisher elsevier science
3 results on '"Yan, Zi-Hong"'

1. Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.

Author

Yan ZH, Wu HQ, Chen WX, Wu Y, Piao HR, He QQ, Chen FE, De Clercq E, and Pannecouque C

Subjects
Cell Survival drug effects, Cells, Cultured, HIV-1 drug effects, Humans, Models, Molecular, Molecular Docking Simulation, Molecular Structure, Nitriles, Precursor Cell Lymphoblastic Leukemia-Lymphoma drug therapy, Precursor Cell Lymphoblastic Leukemia-Lymphoma pathology, Precursor Cell Lymphoblastic Leukemia-Lymphoma virology, Pyrimidines chemical synthesis, Pyrimidines chemistry, Structure-Activity Relationship, Tumor Cells, Cultured, Virus Replication drug effects, Anti-HIV Agents chemical synthesis, Anti-HIV Agents pharmacology, Benzamides chemical synthesis, Benzamides pharmacology, Drug Design, HIV Reverse Transcriptase antagonists & inhibitors, Pyrimidines pharmacology, Reverse Transcriptase Inhibitors chemical synthesis, Reverse Transcriptase Inhibitors pharmacology
Abstract

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 compounds 7f and 7g showed excellent activity against wild-type HIV-1 with low nanomolar EC50 values of 0.005 and 0.009 μM, respectively, which were comparable to or more potent than all the reference drugs zidovudine (AZT), lamivudine (3TC), nevirapine (NEV), efavirenz (EFV), delaviridine (DLV) and etravirine (ETV). In particular, 7g also displayed strong activity against the double mutant strain 103N + 181C with an EC50 value of 8.2 μM. The preliminary structure-activity relationship (SAR) and molecular docking analysis of this new series of CHX-DAPYs were also investigated., (Copyright © 2014 Elsevier Ltd. All rights reserved.)

Published
2014
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2. Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.

Author

Yan ZH, Huang XY, Wu HQ, Chen WX, He QQ, Chen FE, De Clercq E, and Pannecouque C

Subjects
Binding Sites, Cell Line, HIV Reverse Transcriptase metabolism, Humans, Molecular Docking Simulation, Protein Structure, Tertiary, Pyrimidines chemistry, Pyrimidines metabolism, Reverse Transcriptase Inhibitors metabolism, Structure-Activity Relationship, HIV Reverse Transcriptase antagonists & inhibitors, HIV-1 enzymology, Reverse Transcriptase Inhibitors chemistry
Abstract

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. All the target compounds except for compound 3k displayed inhibitory activity against HIV-1 wild-type with EC50 values ranging from 7.21±1.99 to 0.067±0.006 μM. Among them, compound 3d showed the most potent anti-HIV-1 activity (EC50=0.067±0.006 μM, SI>592), which was approximately 2-fold more potent than the reference drugs nevirapine (NVP) and delaviridine (DLV) in the same assay. In addition, the binding modes with HIV-1 RT and the preliminary SAR studies of these new derivatives were also investigated., (Copyright © 2014 Elsevier Ltd. All rights reserved.)

Published
2014
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3. Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.

Author

Wu HQ, Yan ZH, Chen WX, He QQ, Chen FE, De Clercq E, Balzarini J, Daelemans D, and Pannecouque C

Subjects
Binding Sites, HIV Reverse Transcriptase metabolism, Humans, Molecular Docking Simulation, Protein Binding, Protein Structure, Tertiary, Pyrimidines chemical synthesis, Pyrimidines metabolism, Pyrimidinones chemistry, Pyrimidinones metabolism, Reverse Transcriptase Inhibitors chemistry, Reverse Transcriptase Inhibitors metabolism, Structure-Activity Relationship, HIV Reverse Transcriptase antagonists & inhibitors, HIV-1 enzymology, Pyrimidines chemistry, Pyrimidinones chemical synthesis, Reverse Transcriptase Inhibitors chemical synthesis
Abstract

A series of C6-rigid S-DABO analogs characterized by a substituted benzoyl group at C6 position of the pyrimidine ring has been synthesized and biological evaluation as NNRTIs against wild-type HIV-1 strain IIIB, double RT mutant (K103N+Y181C) strain RES056 as well as HIV-2 strain ROD in MT-4 cell cultures. Most of the compounds exhibited moderate antiviral activities. Among them, compound 7q displayed the highest anti-HIV-1 activity with an EC50 value of 0.26μM and a selectivity index (SI) of 541. The preliminary structure-activity relationship (SAR) of these new S-DABOs was investigated, the target RT was confirmed and docking study was performed., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Published
2013
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