Novel Naphthalene-Scaffold VEGFR2 Inhibitors for Solid Tumors

Featuring structure-based discovery data for novel VEGFR2 inhibitors with a naphthalene scaffold, synthesized and evaluated against a broad range of solid tumors. The data originates from research by Tingting Yang, published on figshare in 2026, and is provided in a 3.6 KB CSV file under a CC BY-NC 4.0 license.

Use Cases

• Analyze structure-activity relationships for naphthalene-scaffold compounds against VEGFR2.
• Correlate in vitro IC50 values with in vivo tumor growth inhibition rates for candidate compounds.
• Compare the pharmacokinetics and therapeutic window of novel inhibitors like compound E20 against reference drugs such as lenvatinib.
• Model the impact of scaffold hopping and substitution site variation on compound potency and selectivity.

Strengths

• Data is derived from systematic in vitro and in vivo evaluation, including tumor growth inhibition rates exceeding 90%.
• Includes comparative analysis against a known clinical candidate, lenvatinib.
• Dataset is focused on a specific, promising preclinical candidate (E20) with multitargeted tyrosine kinase inhibition.

Limitations

• The dataset is very small at 3.6 KB, indicating limited scope and likely a summary of key findings rather than raw experimental data.
• Specific data structure, column names, and row counts are not provided, complicating direct analysis.
• Data is focused on a single chemical scaffold and a specific receptor target, limiting generalizability.

Provenance

Source

figshare, authored by Tingting Yang.

Collection Method

Structure-based rational design involving scaffold hopping and substitution site variation, followed by synthesis and biological evaluation.

Freshness

Last updated in March 2026.