Fused pyrrolo-pyridines and pyrrolo-(iso)quinoline as anticancer agents

2022 ◽  
Vol 0 (0) ◽  
Author(s):  
Dorina Amariucai-Mantu ◽  
Vasilichia Antoci ◽  
Monica Cornelia Sardaru ◽  
Cristina Maria Al Matarneh ◽  
Ionel Mangalagiu ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Quinoline Derivatives

Abstract This work emphasizes the synthesis strategies and antiproliferative related properties of fused pyrrolo-pyridine (including indolizine and azaindoles) and pyrrolo-(iso)quinoline derivatives recently reported in literature.

Design, synthesis and biological evaluation of new 4-(4-substituted-anilino)quinoline derivatives as anticancer agents

2017 ◽  
Vol 26 (5) ◽  
pp. 929-939 ◽  
Author(s):  
Khaled R. A. Abdellatif ◽  
Eman K. A. Abdelall ◽  
Mohamed A. Abdelgawad ◽  
Dina M. E. Amin ◽  
Hany A. Omar
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Quinoline Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Antiproliferative potential, quantitative structure-activity relationship, cheminformatic and molecular docking analysis of quinoline and benzofuran derivatives

2020 ◽  
Vol 11 (3) ◽  
pp. 223-234
Author(s):  
Praveen Kumar ◽  
Chinnappa Apattira Uthaiah ◽  
Santhosha Sangapurada Mahantheshappa ◽  
Nayak Devappa Satyanarayan ◽  
SubbaRao Venkata Madhunapantula ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Anticancer Agents ◽  
Quantitative Structure Activity Relationship ◽  
Quinoline Derivatives ◽  
Quantitative Structure ◽  
Docking Analysis ◽  
Structure Activity ◽  
Ic50 Values ◽  
Hct 116 ◽  
Molecular Docking Analysis

Quinoline and benzofuran moieties are commonly used for the synthesis of therapeutically beneficial molecules and drugs since they possess a wide range of pharmacological activities including potent anticancer activity as compared to other heterocyclic compounds. Many of well-known antimalarial, antimicrobial, anti-helminthic, analgesic, anti-inflammatory, antiprotozoal, and antitumor compounds contain quinoline/benzofuran skeleton. The aim of this study was to analyze ten new quinoline and eighteen benzofuran derivatives for carcinoma cell line growth inhibition and to predict possible interactions with the target. The anticancer activity of these compounds against colon cancer (HCT-116) and triple-negative breast cancer (MDA-MB-468) cell lines was determined and performed molecular docking to predict the possible interactions. Among ten quinoline derivatives, Q1, Q4, Q6, Q9, and Q10 were found to be the most potent against HCT-116 and MDA-MB-468 with IC50 values ranging from 6.2-99.6 and 2.7-23.6 μM, respectively. Using the IC50 values, a model equation with quantitative structure activity relationship (QSAR) was generated with their descriptors such as HBA1, HBA2, kappa (1, 2 and 3), Balaban index, Wiener index, number of rotatable bonds, log S, log P and total polar surface area (TPSA). The effect of benzofuran derivatives was moderate in cytotoxicity tests and hence only quinolines were considered for further analysis. The molecular docking indicated the mammalian / mechanistic target of rapamycin (mTOR), Topoisomerase I and II as possible targets for these molecules. The predicted results obtained from QSAR and molecular docking analysis of quinoline derivatives showed high correlation in comparison to the results of the cytotoxic assay. Overall, this study indicated that quinolines are more potent as anticancer agents compared to benzofurans. Further, compound Q9 has emerged as a lead molecule which could be the base for further development of more potent anticancer agents.

Recent Progress in the Development of Quinoline Derivatives for the Exploitation of Anti-cancer Agents

2020 ◽  
Vol 20 ◽  
Author(s):  
Ruo-Jun Man ◽  
Nasreen Jeelani ◽  
Chongchen Zhou ◽  
Yu-Shun Yang
Keyword(s):  
Clinical Trials ◽  
Anticancer Agents ◽  
Rational Design ◽  
Biological Macromolecules ◽  
Quinoline Derivatives ◽  
Specific Topic ◽  
Anti Cancer ◽  
The World ◽  
New Challenges ◽  
The Relationship

Background: Along with the progress in medicine and therapies, the exploitation of anti-cancer agents focused more on the vital signaling pathways and key biological macromolecules. With rational design and advanced synthesis, quinoline derivatives have been utilized frequently in medicinal chemistry, especially in developing anti-cancer drugs or candidates. Methods: Using DOI searching, articles published before 2020 all over the world have been reviewed as comprehensively as possible. Results: In this review, we selected the representative quinoline derivate drugs in market or clinical trials, classified them into five major categories with detailed targets according to their main mechanisms, discussed the relationship within the same mechanism, and generated a summative discussion with prospective expectations. For each mechanism, the introduction of the target was presented, with the typical examples of quinoline derivate drugs. Conclusion: This review has highlighted the quinoline drugs or candidates, suited them into corresponding targets in their pathways, summarized and discussed. We hope that this review may help the researchers who are interested in discovering quinoline derivate anticancer agents obtain considerable understanding in this specific topic. Through the flourishing period and the vigorous strategies in clinical trials, quinoline drugs would be potential but facing new challenges in future.

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