Design, Synthesis and Anti‐Cancer Evaluation of Quinoline‐1,2,4‐triazine Hybrids

Author:

Dong Chang‐E1,Qi Cong1,Rui‐Li 1,Xue Xuan‐Yi1,Wei Rong‐Bin12,Liu Wei‐Wei1,Zhai Yuan‐Fen12,Shi Da‐Hua12ORCID

Affiliation:

1. Jiangsu Key Laboratory of Marine Bioresources and Environment Co-Innovation Center of Jiangsu Marine Bio-industry Technology School of Pharmacy Jiangsu Ocean University Lianyungang 222005 People's Republic of China

2. Jiangsu Institute of Marine Resources Development Jiangsu Ocean University Lianyungang 222005 People's Republic of China Tel

Abstract

AbstractNine quinoline‐1,2,4‐triazine hybrids (5 a5 i) were designed, synthesized, and subjected to evaluation as potential anti‐cancer agents. Structures validation of the synthesized analogues was accomplished through comprehensive analysis employing NMR, HRMS, and IR spectroscopy techniques. Furthermore, the molecular structures of compounds 5 a, 5 d and 5 h were authenticated via single crystal X‐ray diffraction. In an extensive screening process against the human pancreatic cancer PANC‐1 cell line utilizing the MTT assay, all quinoline‐1,2,4‐triazine hybrids (5 a5 i) manifested significant anti‐proliferative activity. Compound 5 g demonstrated a significant anti‐proliferative effect with an IC50 value of 26.8 μM, similar to the positive control, 5‐Fu. Subsequent investigations revealed varying degrees of cell viability in MDA‐MB‐231, A549, and UM‐UC‐3 cell lines upon exposure to different concentrations of compound 5 g. These findings lead us to postulate that compound 5 g may impede the migration, invasion, and adhesion of PANC‐1 cells, similar to the effects observed with 5‐Fu.

Funder

Priority Academic Program Development of Jiangsu Higher Education Institutions

Publisher

Wiley

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