4.6 Article

7-Chloroquinolinehydrazones as First-in-Class Anticancer Experimental Drugs in the NCI-60 Screen among Different Investigated Series of Aryl, Quinoline, Pyridine, Benzothiazole and Imidazolehydrazones

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PHARMACEUTICALS
卷 16, 期 5, 页码 -

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MDPI
DOI: 10.3390/ph16050691

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hydrazone; 7-chloroquinoline; NCI panel; antitumor; pharmacomodulation; SAR

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This study describes the synthesis and evaluation of new hydrazones with quinoline, pyridine, benzothiazole, and imidazole moieties for their cytotoxic potential against 60 cancer cell lines. The 7-chloroquinolinehydrazones were found to be the most active compounds, exhibiting good cytotoxic activity on a large panel of cell lines from various tumor types. This study provides valuable insights into the structure-activity relationships of these experimental antitumor compounds.
In the context of a continuously increasing global cancer risk, the search for new effective and affordable anticancer drugs remains a constant demand. This study describes chemical experimental drugs able to destroy cancer cells by arresting their growth. New hydrazones with quinoline, pyridine, benzothiazole and imidazole moieties have been synthesized and evaluated for their cytotoxic potential against 60 cancer cell lines. 7-Chloroquinolinehydrazones were the most active in the current study and exhibited good cytotoxic activity with submicromolar GI(50) values on a large panel of cell lines from nine tumor types (leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer). This study provided consistent structure-activity relationships in this series of experimental antitumor compounds.

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