Compound 56

Compound 56, 4-[(3-Bromophenyl)amino]-6,7-diethoxyquinazoline, is a potent and specific inhibitor of the tyrosine kinase of the epidermal growth factor receptor (EGFR) showing an IC₅₀ of 0.006 nM. It competitively binds at the adenosine-triphosphate (ATP) site of EGFR. Compound 56 is capable of inhibiting the phosphorylation of EGF-dependent EGFR, suppressing the proliferation and clonogenicity of a wide panel of EGFR-overexpressing human cancer lines, and blocking EGF-mediated mitogenesis and oncogenic transformation in fibroblasts overexpressing EGFR. Besides inhibiting EGFR tyrosine kinase, It also inhibits the tyrosine kinase of human epidermal growth factor receptor 2 (HER2/neu) but with a less potency.

Reference

Bridges AJ, Zhou H, Cody DR, Rewcastle GW, McMichael A, Showalter HD, Fry DW, Kraker AJ, and Denny WA. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor.J Med Chem 1966; 39 (1): 267-276

Monique Bos, Jhn Mendelsohn, Young-Mee Kim, Joan Albanell, David W. Fry, and Jose Baelga. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res 1997;3:2099-2106

The analysis of microsatellites and compound microsatellites in 56 complete genomes of Herpesvirales.[Pubmed:25172209]

Gene. 2014 Nov 1;551(1):103-9.

Simple sequence repeats (SSRs), or microsatellites, are special DNA/RNA sequences with repeated unit of 1-6 bp. The genomes of Herpesvirales have many repeating structures, which is an excellent system to study the evolution and roles of microsatellites and compound microsatellites in viruses. Therefore, 56 genomes of Herpesvirales were selected and the occurrence, composition and complexity of different repeats were investigated in the genomes. A total of 63,939 microsatellites and 5825 compound microsatellites were extracted from 56 genomes. It found that GC content has a significant strong correlation with both the counts of microsatellites (CM) and the counts of compound microsatellites (CCM). However, genome size has a moderate correlation only with CM and almost no correlation with CCM. The compound microsatellites occurring in genic regions are obviously more than that in intergenic regions. In general, the number of compound microsatellite decreases with the increase of complexity (C) (the count of individual microsatellites being part of a compound microsatellite) and the complexity hardly exceeds C=4. The vast majority of compound microsatellites exist in intergenic regions, when C>/=10. The distributions of SSRs tend to be organism-specific rather than host-specific in herpesvirus genomes. The diversity of microsatellites and compound microsatellites may be helpful for a better understanding of the viral genetic diversity, genotyping, and evolutionary biology in herpesviruses genomes.

Magnetic Properties of a Single-Molecule Lanthanide-Transition-Metal Compound Containing 52 Gadolinium and 56 Nickel Atoms.[Pubmed:26923173]

Angew Chem Int Ed Engl. 2016 Mar 24;55(14):4532-6.

Monodisperse metal clusters provide a unique platform for investigating magnetic exchange within molecular magnets. Herein, the core-shell structure of the monodisperse molecule magnet of [Gd52 Ni56 (IDA)48 (OH)154 (H2 O)38 ]@SiO2 (1 a@SiO2 ) was prepared by encapsulating one high-nuclearity lanthanide-transition-metal compound of [Gd52 Ni56 (IDA)48 (OH)154 (H2 O)38 ](NO3 )18 164 H2 O (1) (IDA=iminodiacetate) into one silica nanosphere through a facile one-pot microemulsion method. 1 a@SiO2 was characterized using transmission electron microscopy, N2 adsorption-desorption isotherms, and inductively coupled plasma-atomic emission spectrometry. Magnetic investigation of 1 and 1 a revealed J1 =0.25 cm(-1) , J2 =-0.060 cm(-1) , J3 =-0.22 cm(-1) , J4 =-8.63 cm(-1) , g=1.95, and z J=-2.0x10(-3) cm(-1) for 1, and J1 =0.26 cm(-1) , J2 =-0.065 cm(-1) , J3 =-0.23 cm(-1) , J4 =-8.40 cm(-1) g=1.99, and z J=0.000 cm(-1) for 1 a@SiO2 . The z J=0 in 1 a@SiO2 suggests that weak antiferromagnetic coupling between the compounds is shielded by silica nanospheres.