Tag: 204.2682

Radioiodinated Styrylbenzenes and Thioflavins as Probes for Amyloid Aggregates was written by Zhuang, Z.-P.;Kung, M.-P.;Hou, C.;Skovronsky, D. M.;Gur, T. L.;Ploessl, K.;Trojanowski, J. Q.;Lee, V. M.-Y.;Kung, H. F.. And the article was included in Journal of Medicinal Chemistry in 2001.Formula: C12H16N2O This article mentions the following:

We report for the first time that small mol.-based radioiodinated ligands, showing selective binding to Aβ aggregates, cross the intact blood-brain barrier by simple diffusion. Four novel ligands showing preferential labeling of amyloid aggregates of Aβ(1-40) and Aβ(1-42) peptides, commonly associated with plaques in the brain of people with Alzheimer’s disease (AD), were developed. Two ¹²⁵I-labeled styrylbenzenes, (E,E)-1-iodo-2,5-bis(3-hydroxycarbonyl-4-hydroxy)styrylbenzene, I (ISB), and (E,E)-1-iodo-2,5-bis(3-hydroxycarbonyl-4-methoxy)styrylbenzene, II (IMSB), and two ¹²⁵I-labeled thioflavins, 2-[4′-(dimethylamino)phenyl]-6-iodobenzothiazole, III (TZDM), and 2-[4′-(4”-methylpiperazin-1-yl)phenyl]-6-iodobenzothiazole, IV (TZPI), were prepared at a high specific activity (2200 Ci/mmol). In vitro binding studies of these ligands showed excellent binding affinities with K_d values of 0.08, 0.13, 0.06, and 0.13 nM for aggregates of Aβ(1-40) and 0.15, 0.73, 0.14, and 0.15 nM for aggregates of Aβ(1-42), resp. Interestingly, under a competitive-binding assaying condition, different binding sites on Aβ(1-40) and Aβ(1-42) aggregates, which are mutually exclusive, were observed for styrylbenzenes and thioflavins. Autoradiog. studies of postmortem brain sections of a patient with Down’s syndrome known to contain primarily Aβ(1-42) aggregates in the brain showed that both [¹²⁵I]-III and [¹²⁵I]-IV labeled these brain sections, but [¹²⁵I]-II, selective for Aβ(1-40) aggregates, exhibited very low labeling of the comparable brain section. Biodistribution studies in normal mice after an iv injection showed that [¹²⁵I]-III and [¹²⁵I]-IV exhibited excellent brain uptake and retention, the levels of which were much higher than those of [¹²⁵I]-I and [¹²⁵I]-II. These findings strongly suggest that the new radioiodinated ligands may be useful as biomarkers for studying Aβ(1-40) as well as Aβ(1-42) aggregates of amyloidogenesis in AD patients. In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1Formula: C12H16N2O).

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Formula: C12H16N2O

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Efficient synthesis of a new class of N-nucleosides of 4H-thiochromeno[2,3-d]pyrimidine-10-sulfone as potential anticancer and antibacterial agents was written by Alshammari, Abdulrahman G.;El-Gazzar, Abdel-Rhman B. A.;Hafez, Hend N.. And the article was included in International Journal of Organic Chemistry in 2013.Product Details of 27913-99-1 This article mentions the following:

A highly practical and efficient preparation of 6-methyl-4H-thiochromene and 7-methyl-thiochromene[2,3-d]pyrimidine derivatives, e.g. I (X = NH, NMe, O), was developed via a multi-component reaction of 3-methyl-thiophenol, aldehydes, and malononitrile. A series of pyrimidine nucleoside, thiochromene[2,3-d]pyrimidine and thiochromene[2,3-d]pyrimidine-10-sulfone was efficiently obtained. These hybrid compounds were evaluated as potential antibacterial and anticancer agents and showed encouraging biol. activities. Some of these derivatives showed broad-spectrum antitumor activity against the nine tumor sub-panels tested, and demonstrated significant activity in the in vitro antitumor screening expressed by MG-MID log₁₀GI₅₀ value of -4.55, -4.67 and -4.73 of compounds I (X = NH, NMe, O), resp. In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1Product Details of 27913-99-1).

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Product Details of 27913-99-1

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors was written by Hassan, Ghaneya S.;Georgey, Hanan H.;Mohammed, Esraa Z.;George, Riham F.;Mahmoud, Walaa R.;Omar, Farghaly A.. And the article was included in European Journal of Medicinal Chemistry in 2021.Application of 27913-99-1 This article mentions the following:

Novel series of diphenyl-1H-pyrazoles (Z/E)I (Ar = C₆H₅, 4-BrC₆H₄, 2-thienyl, etc.) and pyrazolo[3,4-b]pyridines II and III (R = H, OMe, Cl; X = CH₂, O, NCH₃) were synthesized and evaluated for their antiproliferative activity against breast cancer cell line (MCF7) and Hepatocellular carcinoma cell line (HepG2). The highest MCF7 growth inhibition activity was attained via compounds (Z/E)I (Ar = 4-CH₃OC₆H₄) and III (R = OMe; X = O) (IC₅₀ = 1.29 and 0.93μM, resp.), while compounds II (4-FC₆H₄) and III (R = OMe; X = NMe) were the most active ones against HepG2 (IC₅₀ = 1.57 and 1.33μM, resp.) compared to doxorubicin (IC₅₀ = 1.88 and 7.30μM, resp.). Cell cycle anal. showed arrest at S and G2-M phases in MCF7 cells treated with (Z/E)I (Ar = 4-CH₃OC₆H₄) and III (R = OMe; X = O), and at G2-M and G1/S phases in HepG2 cells treated with II (4-FC₆H₄) and III (R = OMe; X = NMe), resp. Apoptotic effect of compounds (Z/E)I (Ar = 4-CH₃OC₆H₄), II (4-FC₆H₄), III (R = OMe; X = O, NMe) was indicated via their pre-G1 early and late apoptotic effects and augmented levels of caspase-9/MCF7 and caspase-3/HepG2. A worthy safety profile was assessed for compounds (Z/E)I (Ar = 4-CH₃OC₆H₄) and III (R = OMe; X = O) on MCF10A and compounds II (4-FC₆H₄) and III (R = OMe; X = NMe) on THLE2 treated normal cells. Furthermore, compounds (Z/E)I (Ar = 4-CH₃OC₆H₄), II (4-FC₆H₄) and III (R = OMe; X = NMe) displayed a promising selective profile for CDK2 inhibition vs. CDK1, CDK4, and CDK7 isoforms are proved from their selectivity index. Docking in CDK2 ATP binding site, co-crystallized with R-Roscovitine, demonstrated analogous interactions and comparable binding energy with the native ligand. 2D QSAR sighted the possible structural features governing the CDK2 inhibition activity elicited by the studied pyrazolo[3,4-b]pyridines II and III. These findings present compounds (Z/E)I (Ar = 4-CH₃OC₆H₄), II (4-FC₆H₄) and III (R = OMe; X = NMe) as selective CDK2 inhibitors with promising antiproliferative activity against MCF7 and HepG2 cancer cells. In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1Application of 27913-99-1).

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Application of 27913-99-1

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors was written by Hassan, Ghaneya S.;Georgey, Hanan H.;Mohammed, Esraa Z.;George, Riham F.;Mahmoud, Walaa R.;Omar, Farghaly A.. And the article was included in European Journal of Medicinal Chemistry in 2021.Application of 27913-99-1 This article mentions the following:

Novel series of diphenyl-1H-pyrazoles (Z/E)I (Ar = C₆H₅, 4-BrC₆H₄, 2-thienyl, etc.) and pyrazolo[3,4-b]pyridines II and III (R = H, OMe, Cl; X = CH₂, O, NCH₃) were synthesized and evaluated for their antiproliferative activity against breast cancer cell line (MCF7) and Hepatocellular carcinoma cell line (HepG2). The highest MCF7 growth inhibition activity was attained via compounds (Z/E)I (Ar = 4-CH₃OC₆H₄) and III (R = OMe; X = O) (IC₅₀ = 1.29 and 0.93μM, resp.), while compounds II (4-FC₆H₄) and III (R = OMe; X = NMe) were the most active ones against HepG2 (IC₅₀ = 1.57 and 1.33μM, resp.) compared to doxorubicin (IC₅₀ = 1.88 and 7.30μM, resp.). Cell cycle anal. showed arrest at S and G2-M phases in MCF7 cells treated with (Z/E)I (Ar = 4-CH₃OC₆H₄) and III (R = OMe; X = O), and at G2-M and G1/S phases in HepG2 cells treated with II (4-FC₆H₄) and III (R = OMe; X = NMe), resp. Apoptotic effect of compounds (Z/E)I (Ar = 4-CH₃OC₆H₄), II (4-FC₆H₄), III (R = OMe; X = O, NMe) was indicated via their pre-G1 early and late apoptotic effects and augmented levels of caspase-9/MCF7 and caspase-3/HepG2. A worthy safety profile was assessed for compounds (Z/E)I (Ar = 4-CH₃OC₆H₄) and III (R = OMe; X = O) on MCF10A and compounds II (4-FC₆H₄) and III (R = OMe; X = NMe) on THLE2 treated normal cells. Furthermore, compounds (Z/E)I (Ar = 4-CH₃OC₆H₄), II (4-FC₆H₄) and III (R = OMe; X = NMe) displayed a promising selective profile for CDK2 inhibition vs. CDK1, CDK4, and CDK7 isoforms are proved from their selectivity index. Docking in CDK2 ATP binding site, co-crystallized with R-Roscovitine, demonstrated analogous interactions and comparable binding energy with the native ligand. 2D QSAR sighted the possible structural features governing the CDK2 inhibition activity elicited by the studied pyrazolo[3,4-b]pyridines II and III. These findings present compounds (Z/E)I (Ar = 4-CH₃OC₆H₄), II (4-FC₆H₄) and III (R = OMe; X = NMe) as selective CDK2 inhibitors with promising antiproliferative activity against MCF7 and HepG2 cancer cells. In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1Application of 27913-99-1).

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Application of 27913-99-1

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics