Category: 175137-21-0

1-Aryl-3-[4-(thieno[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as VEGFR-2 tyrosine kinase inhibitors: synthesis, biological evaluation, and molecular modelling studies was written by Soares, Pedro;Costa, Raquel;Froufe, Hugo J. C.;Calhelha, Ricardo C.;Peixoto, Daniela;Ferreira, Isabel C. F. R.;Abreu, Rui M. V.;Soares, Raquel;Queiroz, Maria-Joao R. P.. And the article was included in BioMed Research International in 2013.Category: pyrimidines This article mentions the following:

The vascular endothelial growth factor receptor-2 (VEGFR-2) is a tyrosine kinase receptor involved in the growth and differentiation of endothelial cells that are implicated in tumor-associated angiogenesis. In this study, novel 1-aryl-3-[4-(thieno[3,2-d]pyrimidin-4-yloxy)phenyl]ureas, e.g., I, were synthesized and evaluated for the VEGFR-2 tyrosine kinase inhibition. Three of these compounds showed good VEGFR-2 inhibition presenting low IC₅₀ values (150-199 nM) in enzymic assays, showing also a significant proliferation inhibition of VEGF-stimulated human umbilical vein endothelial cells (HUVECs) at low concentrations (0.5-1 娓璏), using the Bromodeoxyuridine (BrdU) assay, not affecting cell viability. The determination of the total and phosphorylated (active) VEGFR-2 was performed by western blot, and it was possible to conclude that the compounds significantly inhibit the phosphorylation of the receptor at 1 娓璏 pointing to their antiproliferative mechanism of action in HUVECs. The mol. rationale for inhibiting the tyrosine kinase domain of VEGFR-2 was also performed and discussed using mol. docking studies. In the experiment, the researchers used many compounds, for example, 4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0Category: pyrimidines).

4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Macrocyclization as a Source of Desired Polypharmacology. Discovery of Triple PI3K/mTOR/PIM Inhibitors was written by Martinez-Gonzalez, Sonia;Alvarez, Rosa M.;Martin, Jose I.;Garcia, Ana Belen;Riesco-Fagundo, Concepcion;Varela, Carmen;Rodriguez Hergueta, Antonio;Gonzalez Cantalapiedra, Esther;Albarran, M. I.;Gomez-Casero, Elena;Cebria, Antonio;Aguirre, Enara;Ajenjo, Nuria;Cebrian, David;Di Geronimo, Bruno;Cunningham, Darren;O閳ョ澇eill, Michael;Dave, Harish P. G.;Blanco-Aparicio, Carmen;Pastor, Joaquin. And the article was included in ACS Medicinal Chemistry Letters in 2021.Recommanded Product: 4-Chloro-7-methylthieno[3,2-d]pyrimidine This article mentions the following:

The PI3K/AKT/mTOR and PIM kinase pathways contribute to the development of several hallmarks of cancer. Cotargeting of these pathways has exhibited promising synergistic therapeutic effects in liquid and solid tumor types. To identify mols. with combined activities, we cross-screened our collection of PI3K/(鍗TOR) macrocycles (MCXs) and identified the MCX thieno[3,2-d]pyrimidine derivative 2 as a moderate dual PI3K/PIM-1 inhibitor. We report the medicinal chem. exploration and biol. characterization of a series of thieno[3,2-d]pyrimidine MCXs, which led to the discovery of IBL-302 (31), a potent, selective, and orally bioavailable triple PI3K/mTOR/PIM inhibitor. IBL-302, currently in late preclin. development (AUM302), has recently demonstrated efficacy in neuroblastoma and breast cancer xenografts. Addnl., during the course of our experiments, we observed that macrocyclization was essential to obtain the desired multitarget profile. As a matter of example, the open precursors 35-37 were inactive against PIM whereas MCX 28 displayed low nanomolar activity. In the experiment, the researchers used many compounds, for example, 4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0Recommanded Product: 4-Chloro-7-methylthieno[3,2-d]pyrimidine).

4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. A Cu-catalyzed and 4-HO-TEMPO-mediated [3 + 3] annulation of commercially available amidines with saturated ketones enables an efficient and facile synthesis of structurally important pyrimidines via a cascade reaction of oxidative dehydrogenation/annulation/oxidative aromatization.Recommanded Product: 4-Chloro-7-methylthieno[3,2-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The efficient one-step chlorination of methylsulfanyl group on pyrimidine ring system with sulfuryl chloride was written by Ham, Young Jin;Lee, Duck-Hyung;Choi, Hwan Geun;Hah, Jung-Mi;Sim, Taebo. And the article was included in Tetrahedron Letters in 2010.Recommanded Product: 4-Chloro-7-methylthieno[3,2-d]pyrimidine This article mentions the following:

A facile one-step transformation of methylsulfanyl and arylsulfanyl groups on pyrimidine ring system into the corresponding chloride group was achieved using sulfuryl chloride in acetonitrile/dichloromethane. In the experiment, the researchers used many compounds, for example, 4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0Recommanded Product: 4-Chloro-7-methylthieno[3,2-d]pyrimidine).

4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Recommanded Product: 4-Chloro-7-methylthieno[3,2-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Discovery of potent LPA₂ (EDG4) antagonists as potential anticancer agents was written by Beck, Hilary P.;Kohn, Todd;Rubenstein, Steven;Hedberg, Christine;Schwandner, Ralf;Hasslinger, Kerstin;Dai, Kang;Li, Cong;Liang, Lingming;Wesche, Holger;Frank, Brendon;An, Songhzu;Wickramasinghe, Dineli;Jaen, Juan;Medina, Julio;Hungate, Randall;Shen, Wang. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.Safety of 4-Chloro-7-methylthieno[3,2-d]pyrimidine This article mentions the following:

The LPA₂ protein is overexpressed in many tumor cells. We report the optimization of a series of LPA₂ antagonists using calcium mobilization assay (aequorin assay) that led to the discovery of the first reported inhibitors selective for LPA₂. Key compounds were evaluated in vitro for inhibition of LPA₂ mediated Erk activation and proliferation of HCT-116 cells. These compounds could be used to evaluate the benefits of LPA₂ inhibition both in vitro and in vivo. In the experiment, the researchers used many compounds, for example, 4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0Safety of 4-Chloro-7-methylthieno[3,2-d]pyrimidine).

4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Safety of 4-Chloro-7-methylthieno[3,2-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The efficient one-step chlorination of methylsulfanyl group on pyrimidine ring system with sulfuryl chloride was written by Ham, Young Jin;Lee, Duck-Hyung;Choi, Hwan Geun;Hah, Jung-Mi;Sim, Taebo. And the article was included in Tetrahedron Letters in 2010.Recommanded Product: 4-Chloro-7-methylthieno[3,2-d]pyrimidine This article mentions the following:

A facile one-step transformation of methylsulfanyl and arylsulfanyl groups on pyrimidine ring system into the corresponding chloride group was achieved using sulfuryl chloride in acetonitrile/dichloromethane. In the experiment, the researchers used many compounds, for example, 4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0Recommanded Product: 4-Chloro-7-methylthieno[3,2-d]pyrimidine).

4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Recommanded Product: 4-Chloro-7-methylthieno[3,2-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Discovery of potent LPA₂ (EDG4) antagonists as potential anticancer agents was written by Beck, Hilary P.;Kohn, Todd;Rubenstein, Steven;Hedberg, Christine;Schwandner, Ralf;Hasslinger, Kerstin;Dai, Kang;Li, Cong;Liang, Lingming;Wesche, Holger;Frank, Brendon;An, Songhzu;Wickramasinghe, Dineli;Jaen, Juan;Medina, Julio;Hungate, Randall;Shen, Wang. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.Safety of 4-Chloro-7-methylthieno[3,2-d]pyrimidine This article mentions the following:

The LPA₂ protein is overexpressed in many tumor cells. We report the optimization of a series of LPA₂ antagonists using calcium mobilization assay (aequorin assay) that led to the discovery of the first reported inhibitors selective for LPA₂. Key compounds were evaluated in vitro for inhibition of LPA₂ mediated Erk activation and proliferation of HCT-116 cells. These compounds could be used to evaluate the benefits of LPA₂ inhibition both in vitro and in vivo. In the experiment, the researchers used many compounds, for example, 4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0Safety of 4-Chloro-7-methylthieno[3,2-d]pyrimidine).

4-Chloro-7-methylthieno[3,2-d]pyrimidine (cas: 175137-21-0) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Safety of 4-Chloro-7-methylthieno[3,2-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia