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Updated: Dec 21, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Decision making for promising quinoline-based anticancer agents through combined methodology
Evrencan Özcan1, Salih Ökten2, Tamer Eren1
1Department of Industrial Engineering, Faculty of Engineering, Kırıkkale University, Yahşihan, Kırıkkale, Turkey.
Abstract:
During the development of effective drugs for the treatment of cancer, one of the most important tasks is to identify effective drug candidates having maximum antiproliferation and minimum side effects. This paper considers the problem of selecting the most promising anticancer agents, showing inhibition at low IC50 concentration and low releasing lactate dehydrogenase percentage (cytotoxicity). Recently, we prepared quinoline analogs bearing different functional groups and determined their anticancer potential against the HeLa, C6, and HT29 cancer cell lines using different anticancer assays. Experimentally, seven quinoline derivatives consisting of different substituents were determined as promising anticancer agents. We propose a multicriteria recommendation method to identify the most promising anticancer agents against all tested cell lines with an accurate prediction algorithm according to the available input data. A multicriteria decision-making methodology (MCDM) was used for the solution of the relevant problem in this study. Both the experimental results and MCDM method indicated that 5,7-dibromo-8-hydroxyquinoline (2) and 6,8-dibromo-1,2,3,4-tetrahydroquinoline (6) are the most promising anticancer agents against the HeLa, HT29, and C6 cell lines.
Insights
Researchers identified promising anticancer agents by evaluating quinoline derivatives for antiproliferation and low cytotoxicity. The study highlights two specific compounds as most effective against HeLa, C6, and HT29 cancer cell lines.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Cancer Research
Background:
- Developing effective anticancer drugs requires identifying candidates with high efficacy and low toxicity.
- Quinoline derivatives are a class of compounds with potential therapeutic applications.
Purpose of the Study:
- To identify and rank promising quinoline-based anticancer agents.
- To evaluate anticancer potential against HeLa, C6, and HT29 cancer cell lines.
- To apply a multicriteria decision-making methodology (MCDM) for accurate prediction.
Main Methods:
- Synthesis of novel quinoline derivatives with diverse functional groups.
- Anticancer assays to determine inhibitory concentration (IC50) and cytotoxicity (lactate dehydrogenase release).
- Application of a multicriteria recommendation method (MCDM) for data analysis and prediction.
Main Results:
- Seven quinoline derivatives demonstrated significant anticancer potential.
- 5,7-dibromo-8-hydroxyquinoline (2) and 6,8-dibromo-1,2,3,4-tetrahydroquinoline (6) were identified as the most promising agents.
- The MCDM approach accurately predicted the efficacy of the identified compounds.
Conclusions:
- The study successfully identified potent quinoline-based anticancer agents.
- The combination of experimental data and MCDM provides a robust method for drug candidate selection.
- Compounds 2 and 6 warrant further investigation for cancer treatment development.
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