Tag: 300-400

Application of 1353553-07-7On October 1, 2020 ,《Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations》 was published in European Journal of Medicinal Chemistry. The article was written by Xiao, Zhen; Zhou, Zhihui; Chu, Cilong; Zhang, Qian; Zhou, Lingjia; Yang, Zunhua; Li, Xin; Yu, Liying; Zheng, Pengwu; Xu, Shan; Zhu, Wufu. The article contains the following contents:

Five series of novel thiophene-pyrimidine derivatives have been synthesized and tested for their anti-proliferative activity against several cancer cell lines in which EGF is highly expressed. Most of the target compounds showed excellent activity against one or more cancer cell lines. The most promising compound I, of which IC50 values on of cell lines A549 and A431 (4.34 ± 0.60μM and 3.79 ± 0.57μM) were similar to the lead compound Olmutinib, showed strong activity and selectivity to EGFRT790M and EGFRT790M/L858R. Inhibition data of human normal hepatoma cell line LO2 indicated that most target compounds were less toxic to normal cells and had selective inhibitory effects on cancer cells. In addition, the structure-activity relationship was analyzed and the mechanism of apoptosis induced by the compound I was studied. The results showed that compound I induced late apoptosis of A431 cancer cells in a dose-dependent manner. The results came from multiple reactions, including the reaction of 2-Chloro-4-(3-nitrophenoxy)thieno[3,2-d]pyrimidine(cas: 1353553-07-7Application of 1353553-07-7)

2-Chloro-4-(3-nitrophenoxy)thieno[3,2-d]pyrimidine(cas: 1353553-07-7) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Application of 1353553-07-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Recommanded Product: 122567-97-9On October 15, 2021 ,《Multistep Continuous Flow Synthesis of Stavudine》 was published in Journal of Organic Chemistry. The article was written by Sagandira, Cloudius R.; Akwi, Faith M.; Sagandira, Mellisa B.; Watts, Paul. The article contains the following contents:

Herein, we demonstrate an elegant multistep continuous flow synthesis for stavudine (d4T), a potent nucleoside chemotherapeutic agent for human immunodeficiency virus, acquired immunodeficiency syndrome (AIDS) and AIDS-related conditions. This was accomplished via six chem. transformations in five sequential continuous flow reactors from an affordable starting material, 5-methyluridine. In the first instance, single step continuous flow synthesis was demonstrated with an average of 97% yield, 21.4 g/h throughput per step, and a total of 15.5 min residence time. Finally, multistep continuous flow synthesis of d4T in 87% total yield with a total residence time of 19.9 min and 117 mg/h throughput without intermediate purification was demonstrated. In the part of experimental materials, we found many familiar compounds, such as ((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate(cas: 122567-97-9Recommanded Product: 122567-97-9)

((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate(cas: 122567-97-9) belongs to pyrimidine. 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: 122567-97-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Lim, Sang Min; Xie, Ting; Westover, Kenneth D.; Ficarro, Scott B.; Tae, Hyun Seop; Gurbani, Deepak; Sim, Taebo; Marto, Jarrod A.; Janne, Pasi A.; Crews, Craig M.; Gray, Nathanael S. published their research in Bioorganic & Medicinal Chemistry Letters on August 15 ,2015. The article was titled 《Development of small molecules targeting the pseudokinase Her3》.Related Products of 213743-31-8 The article contains the following contents:

Her3 is a member of the human epidermal growth factor receptor (EGFR) tyrosine kinase family, and it is often either overexpressed or deregulated in many types of human cancer. Her3 has not been the subject of small-mol. inhibitor development because it is a pseudokinase and does not possess appreciable kinase activity. We recently reported on the development of the first selective irreversible Her3 ligand (TX1-85-1) that forms a covalent bond with cysteine 721 which is unique to Her3 among all kinases. We also developed a bi-functional compound (TX2-121-1) containing a hydrophobic adamantane moiety and the same warhead of TX1-85-1 that is capable of inhibiting Her3-dependent signaling and growth. Here we report on the structure-based medicinal chem. effort that resulted in the discovery of these two compounds7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Related Products of 213743-31-8) was used in this study.

7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Related Products of 213743-31-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 213743-31-8On October 2, 2000 ,《Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Arnold, L. D.; Calderwood, D. J.; Dixon, R. W.; Johnston, D. N.; Kamens, J. S.; Munschauer, R.; Rafferty, P.; Ratnofsky, S. E.. The article contains the following contents:

Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are potent and selective inhibitors of lck in vitro; some compounds are selective for lck over src. Data are shown for two compounds demonstrating that they are potent and selective inhibitors of IL2 production in cells. In the experiment, the researchers used 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Application of 213743-31-8)

7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. Application of 213743-31-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

HPLC of Formula: 122567-97-9On March 31, 1994, Tortolani, David R.; Russell, John W.; Whiterock, Valerie J.; Hitchcock, Michael J. M.; Ghazzouli, Ismail; Martin, John C.; Mansuri, Muzammil M.; Starrett, John E. Jr. published an article in Journal of Pharmaceutical Sciences. The article was 《Prodrugs of 2′,3′-Didehydro-3′-deoxythymidine (D4T): Synthesis, Antiviral Activity, and Rapid Pharmacokinetic Evaluation》. The article mentions the following:

A series of 5′-derivatives and modified pyrimidine analogs of 2′,3′-didehydro-3′-deoxythymidine (d4T, stavudine) were synthesized to determine their potential as oral prodrugs of d4T. Utilizing a screen developed for the rapid evaluation of a variety of prodrugs in mice, it was determined that 5′-acetate provided comparable plasma levels of d4T after oral administration of the prodrug to that when d4T was administered alone. The relative oral bioavailability of methoxy acetate and cyclohexyl carbonate derivatives was 79 and 41%, resp. The dihydropyridine ester did not provide detectable levels of d4T up to 1 h after oral administration of 6. Thiopyrimidine and aminopyrimidine derivatives also failed to provide measurable levels of d4T after oral administration. 5′-Derivatives showed similar activity to that of d4T against HIV and MuLV, as did 5′-benzoyl-4-thio derivative However, the corresponding 4-thio 5′-alc. derivative was inactive. In the experimental materials used by the author, we found ((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate(cas: 122567-97-9HPLC of Formula: 122567-97-9)

((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate(cas: 122567-97-9) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.HPLC of Formula: 122567-97-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hasegawa, Tetsuya; Seki, Toshinobu; Juni, Kazuhiko; Saneyoshi, Mineo; Kawaguchi, Takeo published their research in Journal of Pharmaceutical Sciences on December 31 ,1993. The article was titled 《Prodrugs of 2′,3′-didehydro-3′-deoxythymidine》.Recommanded Product: 122567-97-9 The article contains the following contents:

Six ester prodrugs of 2′,3′-didehydro-3′-deoxythymidine (I) were prepared, and their physicochem. properties evaluated. Marked differences were observed All of the prodrugs were chem. stable within the pH range 2-7. Hydrolysis of these esters was observed in all cases for 4 rat enzyme systems (plasma, liver, duodenum, and kidney), with I being regenerated. I or the prodrug was administered orally to rats, and the plasma concentrations of I and a corresponding prodrug were measured. The half-life of I after i.v. administration was 35.9 min. The half-life calculated from the terminal phase and the maximum concentration in plasma following oral administration of I were 35.9 min and 48.4 μM, resp. After oral prodrug administration (with water or olive oil as a solvent), though none of the prodrugs was detected in plasma except for 5′-hemisuccinyl derivative of I and 5′-hemiglutaryl derivative of I with olive oil as a solvent, retention time of plasma I concentration was extended and the elevated I concentration in plasma decreased.((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate(cas: 122567-97-9Recommanded Product: 122567-97-9) was used in this study.

((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate(cas: 122567-97-9) belongs to pyrimidine. 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: 122567-97-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

SDS of cas: 213743-31-8On October 2, 2000 ,《Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Burchat, A. F.; Calderwood, D. J.; Hirst, G. C.; Holman, N. J.; Johnston, D. N.; Munschauer, R.; Rafferty, P.; Tometzki, G. B.. The article contains the following contents:

Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are novel, potent and selective inhibitors of lck in vitro. Exploration of C-6 position of the pyrrolo[2,3-d]pyrimidine and the terminal Ph group structure-activity relationship (SAR) is detailed. Compound 1 is orally active in animal models. In the experiment, the researchers used 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8SDS of cas: 213743-31-8)

7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.SDS of cas: 213743-31-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《SVM Model for Virtual Screening of Lck Inhibitors》 was written by Liew, Chin Y.; Ma, Xiao H.; Liu, Xianghui; Yap, Chun W.. Related Products of 213743-31-8 And the article was included in Journal of Chemical Information and Modeling on April 30 ,2009. The article conveys some information:

Lymphocyte-specific protein tyrosine kinase (Lck) inhibitors have treatment potential for autoimmune diseases and transplant rejection. A support vector machine (SVM) model trained with 820 pos. compounds (Lck inhibitors) and 70 neg. compounds (Lck noninhibitors) combined with 65 142 generated putative negatives was developed for predicting compounds with a Lck inhibitory activity of IC50 ≤ 10 μM. The SVM model, with an estimated sensitivity of greater than 83% and specificity of greater than 99%, was used to screen 168 014 compounds in the MDDR and was found to have a yield of 45.8% and a false pos. rate of 0.52%. The model was also able to identify novel Lck inhibitors and distinguish inhibitors from structurally similar noninhibitors at a false pos. rate of 0.27%. To the best of our knowledge, the SVM model developed in this work is the first model with a broad applicability domain and low false pos. rate, which makes it very suitable for the virtual screening of chem. libraries for Lck inhibitors. The results came from multiple reactions, including the reaction of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Related Products of 213743-31-8)

7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Related Products of 213743-31-8They have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Quality Control of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amineOn September 30, 2012 ,《Use of kinase inhibitors to correct ΔF508-CFTR function》 was published in Molecular and Cellular Proteomics. The article was written by Trzcinska-Daneluti, Agata M.; Nguyen, Leo; Jiang, Chong; Fladd, Christopher; Uehling, David; Prakesch, Michael; Al-Awar, Rima; Rotin, Daniela. The article contains the following contents:

The most common mutation in cystic fibrosis (CF) is a deletion of Phe at position 508 (ΔF508-CFTR). ΔF508-CFTR is a trafficking mutant that is retained in the ER, unable to reach the plasma membrane. To identify compounds and drugs that rescue this trafficking defect, we screened a kinase inhibitor library enriched for small mols. already in the clinic or in clin. trials for the treatment of cancer and inflammation, using our recently developed high-content screen technol. The top hits of the screen were further validated by (1) biochem. anal. to demonstrate the presence of mature (Band C) ΔF508-CFTR, (2) flow cytometry to reveal the presence of ΔF508-CFTR at the cell surface, (3) short-circuit current (Isc) anal. in Ussing chambers to show restoration of function of the rescued ΔF508-CFTR in epithelial MDCK cells stably expressing this mutant (including EC50 determinations), and importantly (4) Isc anal. of Human Bronchial Epithelial (HBE) cells harvested from homozygote ΔF508-CFTR transplant patients. Interestingly, several inhibitors of receptor Tyr kinases (RTKs), such as SU5402 and SU6668 (which target FGFRs, VEGFR, and PDGFR) exhibited strong rescue of ΔF508-CFTR, as did several inhibitors of the Ras/Raf/MEK/ERK or p38 pathways (e.g. (5Z)-7-oxozeaenol). Prominent rescue was also observed by inhibitors of GSK-3β (e.g. GSK-3β Inhibitor II and Kenpaullone). These results identify several kinase inhibitors that can rescue ΔF508-CFTR to various degrees, and suggest that use of compounds or drugs already in the clinic or in clin. trials for other diseases can expedite delivery of treatment for CF patients. The experimental part of the paper was very detailed, including the reaction process of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Quality Control of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine)

7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. Quality Control of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Calderwood, David J.; Johnston, David N.; Munschauer, Rainer; Rafferty, Paul published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck》.Recommanded Product: 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine The author mentioned the following in the article:

A series of pyrrolo[2,3-d]pyrimidines was synthesized and structure-activity relationship was evaluated as inhibitors of Lck. Lck accommodates a diverse set of substituents at N-7. Altering the substituent at N-7 provided another compound, an orally available lck inhibitor which inhibited TCR mediated IL-2 production after oral dosing. In the experiment, the researchers used 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Recommanded Product: 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine)

7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8) belongs to pyrimidine. 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: 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia