On November 18, 2021, Vu, Binh; Dominique, Romyr; Li, Hongju; Fahr, Bruce; Good, Andrew published a patent.Recommanded Product: 1340372-11-3 The title of the patent was Preparation of heteroaryl-substituted indole derivatives for restoring mutant p53 function. And the patent contained the following:
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The disclosure provided compounds of formula I capable of binding to mutant p53 and restoring the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. Compounds of formula I [wherein X1 to X4 independently = N, O, S, (un)substituted C, etc.; X5 = CH, N, or (un)substituted NH; wherein at least one of X1 to X4 is a carbon atom connected to Q1; A = (un)substituted ring; Q1 = C=O, C=S, alkylene, etc.; m = 1, 2, 3, or 4; Y = N, O, or absent; R1 = alkyl, halo, (hetero)aryl, etc.; R2 = alkyl, alkenyl, aryl, etc.; R3 and R4 independently = alkyl, aryl, heteroaryl, etc.; R3 and R4 together with the nitrogen atom to which R3 and R4 are bound form a ring] and pharmaceutically acceptable salts thereof, are claimed and exemplified. Example compound II was prepared a multistep procedure (preparation given). Exemplified I were evaluated for DNA binding activity using recombinant His-tag Y220C p53 DBD protein and TR-FRET anal. with some invention candidates demonstrating SC150 results in the range of 0μM to less than 2μM. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Recommanded Product: 1340372-11-3
The Article related to heteroaryl indole preparation mutant p53 restoration cancer progression, dna binding oncogene p53 stabilization heteroaryl indole, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 1340372-11-3
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics