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Updated: Sep 4, 2025
Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Rational synthesis, anticancer activity, and molecular docking studies of novel benzofuran liked thiazole hybrids
Sanjay D Hadiyal1,2, Jaydeep N Lalpara2, Bhavin B Dhaduk2
1Department of Chemistry, Saurashtra University, Rajkot, Gujarat, 360005, India.
Abstract:
A novel series of benzofuran bearing thiazole hybrids were synthesized by the multistep reaction approach. All synthesized molecules were selected by the National Cancer Institute, USA for one-dose anticancer activity against 60 various human cancer cell lines indicating nine types of cancer. Among thirteen compounds, two compounds showed higher lethality, so, it was selected for five-dose anticancer screening against all cancer cell lines. Compound 8g and 8h were displayed remarkable antiproliferative activity with GI50 values ranging from 0.295 to 4.15 μM and LC50 values ranging from 4.43 to > 100 μM. All data are compared with standard drugs fluorouracil and doxorubicin. Compound 8g showed higher potency as a cytotoxic molecule then fluorouracil. Furthermore, all new hybrids were studied for molecular docking into the active binding sites of 1HOV protein.
Insights
Novel benzofuran-thiazole hybrids show potent anticancer activity. Two compounds, 8g and 8h, demonstrated significant antiproliferative effects against various human cancer cell lines, with compound 8g outperforming fluorouracil.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Pharmacology
Background:
- Benzofuran and thiazole scaffolds are recognized for their diverse biological activities.
- Developing novel anticancer agents remains a critical area of pharmaceutical research.
- Hybrid molecules can offer synergistic or enhanced therapeutic profiles.
Purpose of the Study:
- To synthesize and characterize novel benzofuran-thiazole hybrid molecules.
- To evaluate the in vitro anticancer potential of these synthesized compounds.
- To investigate the molecular interactions of promising compounds via molecular docking.
Main Methods:
- Multistep synthetic approach for novel hybrid compounds.
- In vitro anticancer screening against 60 human cancer cell lines (National Cancer Institute, USA).
- Molecular docking simulations against the active binding sites of 1HOV protein.
Main Results:
- Thirteen benzofuran-thiazole hybrids were synthesized and evaluated.
- Compounds 8g and 8h exhibited significant antiproliferative activity (GI50: 0.295–4.15 μM).
- Compound 8g displayed superior cytotoxic potency compared to fluorouracil and was further assessed in five-dose screening.
Conclusions:
- The synthesized benzofuran-thiazole hybrids represent promising anticancer candidates.
- Compounds 8g and 8h warrant further investigation as potential chemotherapeutic agents.
- Molecular docking provides insights into the binding interactions of these novel hybrids with target proteins.
