Novel benzochromenes: design, synthesis, cytotoxicity, molecular docking and mechanistic investigations-Reference-Cited by-同舟云学术

Novel benzochromenes: design, synthesis, cytotoxicity, molecular docking and mechanistic investigations

Published:2024-01 Issue:2 Volume:16 Page:105-123
ISSN:1756-8919
Container-title:Future Medicinal Chemistry
language:en
Short-container-title:Future Medicinal Chemistry

Author:

Abdulrahman Fatma G¹^ORCID,Abulkhair Hamada S²³^ORCID,Zidan Riham A⁴,Alwakeel Asmaa I⁵,Al-Karmalawy Ahmed A³⁶^ORCID,Husseiny Ebtehal M¹^ORCID

Affiliation:

1. Pharmaceutical Organic Chemistry Department, Al-Azhar University, Nasr City, 11754, Cairo, Egypt

2. Pharmaceutical Organic Chemistry Department, Al-Azhar University, Nasr City, 11884, Cairo, Egypt

3. Pharmaceutical Chemistry Department, Horus University–Egypt, International Coastal Road, New Damietta, 34518, Egypt

4. Department of Biochemistry, Al-Azhar University, Cairo, Egypt

5. Department of Pharmacology & Toxicology, Al Azhar University, Cairo, Egypt

6. Pharmaceutical Chemistry Department, Ahram Canadian University, Giza, 12566, 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.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Link

https://www.future-science.com/doi/pdf/10.4155/fmc-2023-0198

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