Category: 373608-48-1

Design, Synthesis, and Biological Evaluation of Mitochondria-Targeted Flavone-Naphthalimide-Polyamine Conjugates with Antimetastatic Activity was written by Dai, Fujun;Li, Qian;Wang, Yuxia;Ge, Chaochao;Feng, Chenyang;Xie, Songqiang;He, Haoying;Xu, Xiaojuan;Wang, Chaojie. And the article was included in Journal of Medicinal Chemistry in 2017.Synthetic Route of C12H25N3O2 This article mentions the following:

Approx. 90% of cancer-associated deaths result from disseminated tumors, indicating the ineffectiveness of current therapies and the imperative need of antimetastatic drugs. A novel pharmacophore with flavonoid and naphthalimide moieties was constructed by using a fragment-based drug design and a series of eight flavone-naphthalimide-polyamine conjugates were synthesized. In vitro evaluation revealed that compound I with a homospermidine motif displayed better cell selectivity between cancerous and normal liver cells than amonafide did. The in vivo assays on two hepatocellular carcinoma (HCC) models verified that I potently suppressed pulmonary metastasis with improved organ indexes compared to amonafide. Various experiments showed that I as a potential fluorescent chem. probe could target the mitochondria. Preliminary investigation into the mechanism of action of I indicated that it might harness a polyamine transporter for cell entrance, localize in the mitochondria, selectively cause reactive oxygen species (ROS) overproduction in hepatoma cells instead of normal liver cells, and finally lead to HCC cell apoptosis and migration inhibition via multiple ROS-mediated signaling pathways. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Synthetic Route of C12H25N3O2).

tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 鎺矯 and boils at 125閳?30 鎺矯. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Synthetic Route of C12H25N3O2

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

Modular click chemistry libraries for functional screens using a diazotizing reagent was written by Meng, Genyi;Guo, Taijie;Ma, Tiancheng;Zhang, Jiong;Shen, Yucheng;Sharpless, Karl Barry;Dong, Jiajia. And the article was included in Nature (London, United Kingdom) in 2019.Related Products of 373608-48-1 This article mentions the following:

Alkyl and aryl azides were prepared from the corresponding primary alkyl and aryl amines by reaction with fluorosulfonyl azide generated in situ from a fluorosulfonylimidazolium triflate and sodium azide, expanding access to azides and both to the 1,2,3-triazoles derived from them and to functional screens employing them. The method allowed the preparation of a library of >1000 azides from the corresponding amines; the azide library underwent copper-catalyzed azide-alkyne cycloaddition reactions to yield a library of >1000 1,2,3-triazoles. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Related Products of 373608-48-1).

tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Related Products of 373608-48-1

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

YAP-dependent proliferation by a small molecule targeting annexin A2 was written by Shalhout, Sophia Z.;Yang, Peng-Yu;Grzelak, Edyta M.;Nutsch, Kayla;Shao, Sida;Zambaldo, Claudio;Iaconelli, Jonathan;Ibrahim, Lara;Stanton, Caroline;Chadwick, Stormi R.;Chen, Emily;DeRan, Michael;Li, Sijia;Hull, Mitchell;Wu, Xu;Chatterjee, Arnab K.;Shen, Weijun;Camargo, Fernando D.;Schultz, Peter G.;Bollong, Michael J.. And the article was included in Nature Chemical Biology in 2021.Computed Properties of C12H25N3O2 This article mentions the following:

Abstract: The transcriptional coactivator Yes-associated protein 1 (YAP) orchestrates a pro-proliferative transcriptional program that controls the fate of somatic stem cells and the regenerative responses of certain tissues. As such, agents that activate YAP may hold therapeutic potential in disease states exacerbated by insufficient proliferative repair. Here we report the discovery of a small mol., termed PY-60, which robustly activates YAP transcriptional activity in vitro and promotes YAP-dependent expansion of epidermal keratinocytes in mouse following topical drug administration. Chem. proteomics revealed the relevant target of PY-60 to be annexin A2 (ANXA2), a protein that directly associates with YAP at the cell membrane in response to increased cell d. PY-60 treatment liberates ANXA2 from the membrane, ultimately promoting a phosphatase-bound, nonphosphorylated and transcriptionally active form of YAP. This work reveals ANXA2 as a previously undescribed, druggable component of the Hippo pathway and suggests a mechanistic rationale to promote regenerative repair in disease. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Computed Properties of C12H25N3O2).

tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Computed Properties of C12H25N3O2

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

Discovery and Development of First-in-Class ACKR3/CXCR7 Superagonists for Platelet Degranulation Modulation was written by Bayrak, Alp;Mohr, Florian;Kolb, Kyra;Szpakowska, Martyna;Shevchenko, Ekaterina;Dicenta, Valerie;Rohlfing, Anne-Katrin;Kudolo, Mark;Pantsar, Tatu;Guenther, Marcel;Kaczor, Agnieszka A.;Poso, Antti;Chevigne, Andy;Pillaiyar, Thanigaimalai;Gawaz, Meinrad;Laufer, Stefan A.. And the article was included in Journal of Medicinal Chemistry in 2022.Application In Synthesis of tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate This article mentions the following:

The atypical chemokine receptor 3 (ACKR3), formerly known as CXC-chemokine receptor 7 (CXCR7), has been postulated to regulate platelet function and thrombus formation. Herein, we report the discovery and development of first-in-class ACKR3 agonists, which demonstrated superagonistic properties with E_max values of up to 160% compared to the endogenous reference ligand CXCL12 in a β-arrestin recruitment assay. Initial in silico screening using an ACKR3 homol. model identified two hits, C10 (EC₅₀ 19.1 μM) and C11 (EC₅₀ 11.4 μM). Based on these hits, extensive structure-activity relationship studies were conducted by synthesis and testing of derivatives It resulted in the identification of the novel thiadiazolopyrimidinone-based compounds 26 (LN5972, EC₅₀ = 3.4 μM) and 27 (LN6023, EC₅₀ = 3.5 μM). These compounds are selective for ACKR3 vs. CXCR4 and show metabolic stability. In a platelet degranulation assay, these agonists effectively reduced P-selectin expression by up to 97%, suggesting potential candidates for the treatment of platelet-mediated thrombosis. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Application In Synthesis of tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate).

tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.Application In Synthesis of tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate

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