Computer-Aided Design, Synthesis and Validation of 2-Phenylquinazolinone Fragments as CDK9 Inhibitors with Anti-HIV-1 Tat-Mediated Transcription Activity

From Small to Powerful: The Fragments Universe and its “Chem-Appeal”

(2013) Luca Sancineto et al.   CURRENT MEDICINAL CHEMISTRY

Blocking HIV-1 Replication by Targeting the Tat-Hijacked Transcriptional Machinery

(2013) Serena Massari et al.   CURRENT PHARMACEUTICAL DESIGN

Substituted 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidines Are Highly Active CDK9 Inhibitors: Synthesis, X-ray Crystal Structures, Structure–Activity Relationship, and Anticancer Activities

(2013) Hao Shao et al.   JOURNAL OF MEDICINAL CHEMISTRY

The CDK9 C-helix Exhibits Conformational Plasticity That May Explain the Selectivity of CAN508

(2012) Sonja Baumli et al.   ACS Chemical Biology

Novel, Selective CDK9 Inhibitors for the Treatment of HIV Infection

(2012) G. Nemeth et al.   CURRENT MEDICINAL CHEMISTRY

Perspective of Cyclin-dependent kinase 9 (CDK9) as a Drug Target

(2012) Vladimir Krystof et al.   CURRENT PHARMACEUTICAL DESIGN

Comparative Structural and Functional Studies of 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 Inhibitors Suggest the Basis for Isotype Selectivity

(2012) Alison J. Hole et al.   JOURNAL OF MEDICINAL CHEMISTRY

CDK2 Regulates HIV-1 Transcription by Phosphorylation of CDK9 on Serine 90

(2012) Denitra Breuer et al.   Retrovirology

Use of ATP analogs to inhibit HIV-1 transcription

(2012) Aarthi Narayanan et al.   VIROLOGY

Structural Investigation of the Naphthyridone Scaffold: Identification of a 1,6-Naphthyridone Derivative with Potent and Selective Anti-HIV Activity

(2011) Oriana Tabarrini et al.   ChemMedChem

An efficient synthesis of 2,3-dihydroquinazolin-4(1H)-one derivatives under catalyst-free and solvent-free conditions

(2011) Lijiu Gao et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

2-Arylthiomorpholine derivatives as potent and selective monoamine oxidase B inhibitors

(2010) Susan Lühr et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Halogen Bonds Form the Basis for Selective P-TEFb Inhibition by DRB

(2010) Sonja Baumli et al.   CHEMISTRY & BIOLOGY

Discovery and Characterization of 2-Anilino-4- (Thiazol-5-yl)Pyrimidine Transcriptional CDK Inhibitors as Anticancer Agents

(2010) Shudong Wang et al.   CHEMISTRY & BIOLOGY

Novel environmentally benign procedure for the synthesis of 2-aryl- and 2-hetaryl-4(3H)-quinazolinones

(2010) T G Deligeorgiev et al.   COLORATION TECHNOLOGY

Promoter-proximal pausing and its release: Molecular mechanisms and physiological functions

(2010) Kunitoshi Chiba et al.   EXPERIMENTAL CELL RESEARCH

6-desfluoroquinolones as HIV-1 Tat-mediated transcription inhibitors

(2010) Oriana Tabarrini et al.   Future Medicinal Chemistry

Iodine: Selectively promote the synthesis of mono substituted quinazolin-4(3H)-ones and 2,3-dihydroquinazolin-4(1H)-ones in one-pot

(2010) Li-Yan Zeng et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

Structure-Based Design of Potent and Selective 2-(Quinazolin-2-yl)phenol Inhibitors of Checkpoint Kinase 2

(2010) John J. Caldwell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystal structure of HIV-1 Tat complexed with human P-TEFb

(2010) Tahir H. Tahirov et al.   NATURE

The molecular biology of HIV latency: breaking and restoring the Tat-dependent transcriptional circuit

(2010) Jonathan Karn   Current Opinion in HIV and AIDS

Identification of Flavopiridol Analogues that Selectively Inhibit Positive Transcription Elongation Factor (P-TEFb) and Block HIV-1 Replication

(2009) Akbar Ali et al.   CHEMBIOCHEM

Cyclin Dependent Kinases as Attractive Targets to Prevent Transcription from Viral Genomes

(2009) Fatah Kashanchi et al.   CURRENT PHARMACEUTICAL DESIGN

Novel HIV-1 therapeutics through targeting altered host cell pathways

(2009) William Coley et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

A New Efficient Method for the Three-Component Synthesis of 4(3H)-Quinazolinones

(2009) Minoo Dabiri et al.   HETEROCYCLES

A 1,8-Naphthyridone Derivative Targets the HIV-1 Tat-Mediated Transcription and Potently Inhibits the HIV-1 Replication

(2009) Serena Massari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular control of HIV-1 postintegration latency: implications for the development of new therapeutic strategies

(2009) Laurence Colin et al.   Retrovirology

The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation

(2008) Sonja Baumli et al.   EMBO JOURNAL

Viral reservoirs, residual viremia, and the potential of highly active antiretroviral therapy to eradicate HIV infection

(2008) Lin Shen et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Perspective on Free-Energy Perturbation Calculations for Chemical Equilibria

(2008) William L. Jorgensen et al.   Journal of Chemical Theory and Computation

Acetylation of Conserved Lysines in the Catalytic Core of Cyclin-Dependent Kinase 9 Inhibits Kinase Activity and Regulates Transcription

(2008) A. Sabo et al.   MOLECULAR AND CELLULAR BIOLOGY

Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: revisited 20 years later

(2008) Christophe Pannecouque et al.   Nature Protocols

Cyclin-dependent kinase 9: a key transcriptional regulator and potential drug target in oncology, virology and cardiology

(2008) S WANG et al.   TRENDS IN PHARMACOLOGICAL SCIENCES