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.