Discovery of small molecule acting as multitarget inhibitor of colorectal cancer by simultaneous blocking of the key COX-2, 5-LOX and PIM-1 kinase enzymes

In conclusion, compound 5g, of simple chemical structure, achieved the target goal of inhibiting three targets leading to inhibition of human CRC cell proliferation. It inhibited the target key enzymes COX-2, 5-LOX and PIM-1\2 kinase in vitro. Besides, it revealed in vitro inhibition of cell proliferation in cancer cell lines via activation of caspase 3\7 dependent-apoptosis in human CRC cell lines. In addition, it elicited in vivo anti-inflammatory activity in formalin-induced paw edema test and in vivo oral safety in gastric ulcerogenic activity test.PMID:34303896 | DOI:10.1016/j.bioorg.2021.105171

Source: Bioorganic Chemistry - July 25, 2021 Category: Chemistry Authors: Mostafa M M El-Miligy Ahmed K Al-Kubeisi Saad R El-Zemity Rasha A Nassra Marwa M Abu-Serie Aly A Hazzaa Source Type: research