Related Experiment Video
Updated: Jul 5, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Novel benzochromenes: design, synthesis, cytotoxicity, molecular docking and mechanistic investigations
Fatma G Abdulrahman1, Hamada S Abulkhair2,3, Riham A Zidan4
1Pharmaceutical Organic Chemistry Department, Al-Azhar University, Nasr City, 11754, Cairo, Egypt.
Abstract:
Aim: A novel series of fused benzochromenes with expected cytotoxicity and HIF-1α inhibition was identified. Materials & methods: A bioisosterism-aided approach was applied to design new benzochromenes and assess their cytotoxicity against three cancer cell lines. The probable mechanistic effect and the in silico docking and pharmacokinetic profiles of the most effective derivatives were evaluated. Results: Compounds 3, 4, 5, 8 and 11 showed potent antiproliferative activity and excellent selectivity. Compound 8 showed significant HIF-1α inhibition with an IC50 value of 3.372 μM. It also enhanced apoptosis and arrested the HepG2 cell cycle at both the G0/G1 and S stages. Conclusion: Compound 8 was identified as a new potential anticancer candidate.
More Related Videos
Related Concept Videos
Electrophilic Aromatic Substitution: Chlorination and Bromination of Benzene
Structure-Activity Relationships and Drug Design
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...
Structure of Benzene: Kekulé Model
He proposed that benzene has a cyclic structure of six carbon atoms attached to one hydrogen atom each, with three alternating pi bonds.
Directing and Steric Effects in Disubstituted Benzene Derivatives
Directing Effect of Substituents: meta-Directing Groups
Electrophilic Aromatic Substitution: Fluorination and Iodination of Benzene

