Aims: The current study is focused on the design and synthesis of 4-aryl/heteroaryl-4H-fused pyrans as
anti-proliferative agents. All the synthesized molecules were screened against a panel of human carcinoma cell lines.
Description: Significant inhibition was exhibited by the compounds against HCT-116 (Colon) and PC-3 (Prostate)
cell lines while A-549 (Lung) cell lines, MiaPaCa-2 (Pancreatic) cell lines and HL-60 (Leukemia Cancer) cell lines
were almost resistant to the exposure of the test compounds. Compound FP-(v)n displayed noteworthy cytotoxicity
towards HCT-116 malignant cells with the IC50 value of 0.67 µM. It induces apoptosis as revealed by several
biological endpoints like apoptotic body formation, through DAPI staining, phase contrast microscopy and
mitochondrial membrane potential loss. Moreover FP-(v)n is a potent apoptotic inducer confirmed by cell cycle
arrest and ROS generation. The cell phase distribution studies indicate an augment from 4.94 % (control sample) to
39.68 % (sample treated with 1.5 µM compound FP-(v)n) in the apoptotic population. Compound FP-(v)n inhibits
the tumor growth in Ehrlich ascites carcinoma (EAC), Ehrlich Tumor (ET, solid) and sarcoma-180 (solid) mice
models. Additionally, it was established to be non-toxic at maximum tolerated dose of 1000 mg/kg in acute oral
toxicity in Swiss-albino mice.
Conclusion: The current study provides an insight into anti-cancer potential of FP-(v)n, which might be valuable in
the treatment of tumor.
Keywords: Apoptosis, pyrans, cytotoxicity, cell lines, cell cycle, sarcoma-180, acute toxicity, anti-cancer efficacy.
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