An article 2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation WOS:000480235700064 published article about P53; ANTAGONISTS; ACTIVATION; DISCOVERY; GROWTH; CANCER in [Bazanov, Daniil R.; Savitskaya, Victoria Yu; Proskurnina, Marina, V; Lozinskaya, Natalia A.] Moscow MV Lomonosov State Univ, Dept Chem, 1 Leninskie Gory, Moscow 119992, Russia; [Pervushin, Nikolay, V; Kopeina, Gelina S.] Moscow MV Lomonosov State Univ, Dept Med, 1 Leninskie Gory, Moscow 119992, Russia; [Anikina, Lada, V; Proskurnina, Marina, V; Lozinskaya, Natalia A.] RAS, Inst Physiol Act Subst, 1 Northern Passage, Chernogolovka 142432, Moscow Region, Russia in 2019.0, Cited 26.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Computed Properties of C9H10O3
Imidazoline-based small molecule inhibitors of p53-MDM2 interaction intended for the treatment of p53 wild-type tumors are the promising structures for design of anticancer drugs. Based on fragment approach we have investigated a key role of substituents in cis-imidazoline core for biological activity of nutlin family compounds. Although the necessity of the substituents in the phenyl rings of cis-imidazoline has been shown, there are no studies in which the replacements of a halogen by other substituents have been investigated. A series of simple cis-imidazoline derivatives containing halogen, hydroxy and alkoxy-substituents were synthesized. The biological activity of the compounds was studied using assays of cytotoxicity (MTT) and p53 level. It was found that the hydroxyl-derivatives were not cytotoxic whereas the alkoxy analogues were the same or more active as halogen-substituted compounds in cell viability test. The synthesized alkoxy derivatives induced an increase of p53 level and did not promote necrotic cell death in the concentration up to 40 mu M.
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Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com