In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Discovery of a potent glutathione peroxidase 4 inhibitor as a selective ferroptosis inducer, published in 2021-09-23, which mentions a compound: 948552-36-1, mainly applied to chloroacetyl anilino arylacetamide ferroptosis inducer preparation antitumor activity; glutathione peroxidase inhibitor structure activity relationship, Name: 1H-Pyrazole-5-carbaldehyde.
Potent and selective ferroptosis regulators promote an intensive understanding of the regulation and mechanisms underlying ferroptosis, which is highly associated with various diseases. In this study, through a stepwise structure optimization, a potent and selective ferroptosis inducer was developed targeting to inhibit glutathione peroxidase 4 (GPX4), and the structure-activity relationship (SAR) of these compounds I [R1 = allyl, cyclohexyl, allyl, etc.; n = 0 and 1], II [wherein, Het = 1H-pyrazol-3-yl, 2-methylpyrazol-3-yl, 1H-indol-4-yl, etc.] and III [X = N and S; R2 = fluoro, methoxy, 5-methyloxazolyl, etc.] was uncovered. Compound III [X = S; R2 = 5-methyloxazolyl] exhibited outstanding GPX4 inhibitory activity with a percent inhibition up to 71.7% at 1.0 μM compared to 45.9% of RSL-3. At the cellular level, III [X = S; R2 = 5-methyloxazolyl] could significantly induce lipid peroxide (LPO) increase and effectively induce ferroptosis with satisfactory selectivity (the value of 31.5). The morphol. anal. confirmed the ferroptosis induced by III [X = S; R2 = 5-methyloxazolyl]. Furthermore, III [X = S; R2 = 5-methyloxazolyl] significantly restrained tumor growth in a mouse 4T1 xenograft model without obvious toxicity.
When you point to this article, it is believed that you are also very interested in this compound(948552-36-1)Name: 1H-Pyrazole-5-carbaldehyde and due to space limitations, I can only present the most important information.