Related Experiment Video

Updated: Jun 11, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
05:17

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors

Michael B Wallace1, Mark E Adams, Toufike Kanouni

  • 1Takeda San Diego, 10410 Science Center Drive, San Diego, CA 92121, United States. michael.wallace@takedasd.com

Bioorganic & Medicinal Chemistry Letters
|July 13, 2010
PubMed

Abstract:

A novel series of pyrrole inhibitors of MEK kinase has been developed using structure-based drug design. Optimization of the series led to the identification of potent inhibitors with good pharmaceutical properties.

More Related Videos

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
05:07

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines

Published on: June 23, 2019

Synthesis of pH Dependent Pyrazole, Imidazole, and Isoindolone Dipyrrinone Fluorophores using a Claisen-Schmidt Condensation Approach
14:11

Synthesis of pH Dependent Pyrazole, Imidazole, and Isoindolone Dipyrrinone Fluorophores using a Claisen-Schmidt Condensation Approach

Published on: June 10, 2021

Related Experiment Videos

Last Updated: Jun 11, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
05:17

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
05:07

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines

Published on: June 23, 2019

Synthesis of pH Dependent Pyrazole, Imidazole, and Isoindolone Dipyrrinone Fluorophores using a Claisen-Schmidt Condensation Approach
14:11

Synthesis of pH Dependent Pyrazole, Imidazole, and Isoindolone Dipyrrinone Fluorophores using a Claisen-Schmidt Condensation Approach

Published on: June 10, 2021

Related Concept Videos

Basicity of Heterocyclic Aromatic Amines01:25

Basicity of Heterocyclic Aromatic Amines

Heterocyclic amines, where the N atom is a part of an alicyclic system, are similar in basicity to alkylamines. Interestingly, the heterocyclic amine having a nitrogen atom as part of an aromatic ring has much less basicity than its corresponding alicyclic counterpart. For this reason, as presented in Figure 1, piperidine (pKb = 2.8) is significantly more basic than pyridine (pKb = 8.8).
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...

Articles linked to this work by shared authors, journal, and citation graph.

Discovery of BMS-986449: A Potent, Selective Degrader of the Transcription Factors IKZF2 (Helios) and IKZF4 (Eos) to Target Regulatory T Cells in Solid Tumors.

Journal of medicinal chemistry·2026

Hematological Malignancy Trials in Chinese Mainland, 2013-2022: A Landscape Analysis with Exploratory Macro-Level Temporal Correlations.

Clinical and translational science·2026

Vonoprazan-based dual therapy with amoxicillin or doxycycline versus bismuth-containing quadruple therapy for Helicobacter pylori eradication: a prospective, multicenter, open-label, randomized controlled trial.

Frontiers in cellular and infection microbiology·2026

A unified catalytic mechanism in bifunctional DNA glycosylases with an evolutionarily conserved aspartate-lysine dyad.

Nature communications·2026

Integrating Health Communication into Basic Medical Courses: A Qualitative Study for Enhancing Professional Competencies in Undergraduate Medical Students.

Advances in medical education and practice·2026

Intelligent quantification of Mn(VII) using a YOLO v3 artificial intelligence-driven smartphone monitoring platform based on nitrogen-doped blue fluorescence carbon dots.

The Analyst·2026

Discovery of potent, selective, and orally bioavailable monocyclic pyridine-based PKMYT1 inhibitors that synergize with CHK1 inhibition in replication-stressed cancer cells.

Bioorganic & medicinal chemistry letters·2026

Quinolin(on)es and pyridin(on)es as promising scaffolds against mycobacterial infections.

Bioorganic & medicinal chemistry letters·2026

Amyloid-β aggregation inhibitory activity and neuroprotective effects of metabolites of Trichoderma pluripenicillatum.

Bioorganic & medicinal chemistry letters·2026

Electrophilic aromatic halogenation of perylenequinones: a strategy to improve photodynamic properties.

Bioorganic & medicinal chemistry letters·2026

Discovery of novel dual STAT3/TrxR1 inhibitors via pharmacophore fusion as potent lead compounds for colorectal cancer.

Bioorganic & medicinal chemistry letters·2026

6-(2-Hydroxybenzoyl)pyrazolo[1,5-a]pyrimidine-3‑carbonitriles as novel reactive oxygen species-generating anticancer agents inducing ER stress and DNA damage in EGFR-mutant non-small cell lung cancer.

Bioorganic & medicinal chemistry letters·2026

Strategy for modular assembly of tetravalent, multispecific antibodies.

Protein science : a publication of the Protein Society·2026

Synthesis, Conformational Analysis, and Evaluation of 6R- and 6S‑Methylmannoimidazoles as Mannosidase Inhibitors.

ACS omega·2026

Correction to "Design, Synthesis, and Biological Evaluation of Novel Tetrandrine Derivatives Targeting AKT1 for Hepatocellular Carcinoma Therapy: Integration of Network Pharmacology, Molecular Dynamics Simulation, and Experimental Validation".

ACS omega·2026

Synthesis and Fundamental Evaluation of [67Ga]Ga-NOTA‑D‑KV6 as a Potential Cationic Amphiphilic Peptide Probe for Tumor Imaging.

ACS omega·2026

Computational Design of RNA Aptamers Targeting Oncogenic miR-10b Using T‑SELEX and Molecular Dynamics-Based Stability Metrics.

ACS omega·2026

Structure-based molecular modeling of a novel S-Remiketamine scaffold and derived arylcyclohexanone analogues: NMDA receptor dynamics, MM-GBSA ranking, and CES1-Oriented structural compatibility.

Frontiers in chemistry·2026
See all related articles
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies
Jove
Visualize
Contact Us