Category: 90213-66-4

In 2014,Gehringer, Matthias; Forster, Michael; Pfaffenrot, Ellen; Bauer, Silke M.; Laufer, Stefan A. published 《Novel hinge-binding motifs for janus kinase 3 inhibitors: a comprehensive structure-activity relationship study on tofacitinib bioisosteres》.ChemMedChem published the findings.Related Products of 90213-66-4 The information in the text is summarized as follows:

The Janus kinases (JAKs) are a family of cytosolic tyrosine kinases crucially involved in cytokine signaling. JAKs have been demonstrated to be valid targets in the treatment of inflammatory and myeloproliferative disorders, and two inhibitors, tofacitinib and ruxolitinib, recently received their marketing authorization. Despite this success, selectivity within the JAK family remains a major issue. Both approved compounds share a common 7H-pyrrolo[2,3-d]pyrimidine hinge binding motif, and little is known about modifications tolerated at this heterocyclic core. In the current study, a library of tofacitinib bioisosteres was prepared and tested against JAK3. The compounds possessed the tofacitinib piperidinyl side chain, whereas the hinge binding motif was replaced by a variety of heterocycles mimicking its pharmacophore. In view of the promising expectations obtained from mol. modeling, most of the compounds proved to be poorly active. However, strategies for restoring activity within this series of novel chemotypes were discovered and crucial structure-activity relationships were deduced. The compounds presented may serve as starting point for developing novel JAK inhibitors and as a valuable training set for in silico models. In the experimental materials used by the author, we found 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Related Products of 90213-66-4)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Related Products of 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Synthesis and biological evaluation of 6-phenylpurine linked hydroxamates as novel histone deacetylase inhibitors》 was written by Chen, Dizhong; Soh, Chang Kai; Goh, Wei Huang; Wang, Zilong; Wang, Haishan. Product Details of 90213-66-4 And the article was included in Bioorganic Chemistry in 2020. The article conveys some information:

A series of 6-phenylpurine based hydroxamates I (R = morpholin-4-yl, diethylaminyl, dimethylaminyl, pyrrolidin-1-yl; R1 = Et, iso-Pr, Pr, cyclopentyl, pentan-3-yl; R2 = 3-[(hydroxycarbamoyl)methyl]oxidanyl, 4-[4-(hydroxycarbamoyl)butoxy]methyl, 3-[4-(hydroxycarbamoyl)piperidin-1-yl]methyl, etc.) have been designed, synthesized and evaluated. Compound I (R = morpholin-4-yl; R1 = isopropyl; R2 = 3-[3-(hydroxycarbamoyl)propyl]oxidanyl (A)) and its analogs are potent histone deacetylase (HDAC) but weak PI3K/mTOR inhibitors. These compounds demonstrated broad anti-cancer activities against 38 cancer cell lines with leukemia, lymphoma, and the majority of liver cancer cell lines exhibiting the most sensitivity towards these compounds Compound (A) demonstrated modulation of HDAC targets in vitro in a dose-dependent manner. It has good in vitro ADME profile that translated into a greatly improved pharmacokinetic profile., the compound (A) also demonstrated modulation of HDACs in tumors in a PC-3 xenograft model. It was further evaluated in combination therapies in vitro. It exhibited additive or synergistic growth inhibition effect in HepG2 cells when combined with a number of approved drugs such as sorafenib, sunitinib, and erlotinib. Hence, compound (A) has the potential to be combined with the above to treat advanced liver cancer. As such, current data warrant further evaluation, optimization, and subsequent in vivo validation of the potential combination therapies. In the experimental materials used by the author, we found 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Product Details of 90213-66-4)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Product Details of 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2008,Seela, Frank; Xu, Kuiying published 《7-halogenated 7-deazapurine 2′-deoxyribonucleosides related to 2′-deoxyadenosine, 2′-deoxyxanthosine, and 2′-deoxyisoguanosine: syntheses and properties》.Helvetica Chimica Acta published the findings.Reference of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine The information in the text is summarized as follows:

A series of 7-fluorinated 7-deazapurine 2′-deoxyribonucleosides related to 2′-deoxyadenosine, 2′-deoxyxanthosine, and 2′-deoxyisoguanosine as well as intermediates, e.g. I, were synthesized. The 7-fluoro substituent was introduced in 2,6-dichloro-7-deaza-9H-purine with Selectfluor. Apart from 2,6-dichloro-7-fluoro-7-deaza-9H-purine, the 7-chloro compound was formed and used for the glycosylation reaction; the separation of the 7-fluoro from the 7-chloro compound was performed on the level of the unprotected nucleosides. Other halogen substituents were introduced with N-halogenosuccinimides. The 2′-deoxyisoguanosine derivative I was prepared from 2-chloro-7-fluoro-7-deaza-2′-deoxyadenosine via a photochem. induced nucleophilic displacement reaction. The pKa values of the halogenated nucleosides were determined 13C-NMR chem.-shift dependencies of C(7), C(5), and C(8) were related to the electronegativity of the 7-halogen substituents. In aqueous solution, 7-halogenated 2′-deoxyribonucleosides show an approx. 70% S population. In the experiment, the researchers used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Reference of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Reference of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidineThey 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

In 1984,Seela, Frank; Driller, Hansjuergen published 《7-(β-D-Arabinofuranosyl)-2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine – synthesis, selective displacement of halogen, and effect of glyconic protecting groups on the reactivity of the aglycon》.Liebigs Annalen der Chemie published the findings.Application of 90213-66-4 The information in the text is summarized as follows:

Phase-transfer glycosylation of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine with 2,3,5-tri-O-benzyl-α-D-arabinofuranosyl bromide, followed by column chromatog. gave 67% nucleoside I (R = PhCH2) (II), which on debenzylation with BCl3 gave the title compound I (R = H) (III). Nucleophilic displacement on III resulted in selective substitution of Cl in position 4. Under more vigorous conditions the C-4 as well as the C-2 substituents were replaced. In contrast nucleophilic substitution of II was hindered. In addition to this study using 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine, there are many other studies that have used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Application of 90213-66-4) was used in this study.

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) 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 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 1985,Seela, Frank; Driller, Hansjuergen; Liman, Ulrich published 《7-Deaza isosters of 2′-deoxyxanthosine and 2′-deoxyspongosine – synthesis via glycosylation of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine》.Liebigs Annalen der Chemie published the findings.Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine The information in the text is summarized as follows:

Glycosylation of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine with 2-deoxy-3,5-di-O-p-toluoyl-α-D-erythro-pentofuranosyl chloride in DMF in the presence of NaH gave the nucleoside derivative I (R = R1 = Cl; R2 = p-toluoyl) (II) and its α-anomer. II on treatment with NaOMe in MeOH gave I (R = R1 = MeO; R2 = H), which on demethylation with HBr-AcOH in THF gave 7-deaza-2′-deoxyxanthosine (III). II was also converted into 7-deaza-2′-deoxyspongosine (I; R = MeO, R1 = NH2, R2 = H). In the part of experimental materials, we found many familiar compounds, such as 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidineThey 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

In 1987,Seela, Frank; Steker, Herbert; Driller, Hans Juergen; Bindig, Uwe published 《2-Amino-2′-deoxytubercidin and related pyrrolo[2,3-d]pyrimidinyl-2′-deoxyribofuranosides》.Liebigs Annalen der Chemie published the findings.Category: pyrimidines The information in the text is summarized as follows:

Phase-transfer glycosylation of 2-amino-4-chloro-7H-pyrrolo[2,3-d]pyrimidine with 1-chloro-3,5-di-O-(p-toluoyl)-α-D-erythro-pentofuranose (I) yielded the crystalline nucleoside II in a regio- and diastereoselective reaction. Nucleophilic displacement of the 4-chloro substituent of II or the nonprotected analog opened a route to 2-amino-2′-deoxytubercidin (III) or the thionucleoside IV. The anomers of I were isolated from the glycosylation reaction carried out in the absence of the nucleobase. In the part of experimental materials, we found many familiar compounds, such as 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Category: pyrimidines)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The author of 《Designing a chemical inhibitor for the AAA protein spastin using active site mutations》 were Cupido, Tommaso; Pisa, Rudolf; Kelley, Megan E.; Kapoor, Tarun M.. And the article was published in Nature Chemical Biology in 2019. Category: pyrimidines The author mentioned the following in the article:

Spastin is a microtubule-severing AAA (ATPases associated with diverse cellular activities) protein needed for cell division and intracellular vesicle transport. Currently, we lack chem. inhibitors to probe spastin function in such dynamic cellular processes. To design a chem. inhibitor of spastin, we tested selected heterocyclic scaffolds against wild-type protein and constructs with engineered mutations in the nucleotide-binding site that do not substantially disrupt ATPase activity. These data, along with computational docking, guided improvements in compound potency and selectivity and led to spastazoline, a pyrazolyl-pyrrolopyrimidine-based cell-permeable probe for spastin. These studies also identified spastazoline-resistance-conferring point mutations in spastin. Spastazoline, along with the matched inhibitor-sensitive and inhibitor-resistant cell lines we generated, were used in parallel experiments to dissect spastin-specific phenotypes in dividing cells. Together, our findings suggest how chem. probes for AAA proteins, along with inhibitor resistance-conferring mutations, can be designed and used to dissect dynamic cellular processes. In the experiment, the researchers used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Category: pyrimidines)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2010,Tumkevicius, Sigitas; Dodonova, Jelena; Kazlauskas, Karolis; Masevicius, Viktoras; Skardziute, Lina; Jursenas, Saulius published 《Synthesis and photophysical properties of oligoarylenes with a pyrrolo[2,3-d]pyrimidine core》.Tetrahedron Letters published the findings.Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine The information in the text is summarized as follows:

The Pd-catalyzed Suzuki-Miyaura reaction of 2,4-dichloropyrrolo[2,3-d]pyrimidine with arylboronates was studied. Pd(OAc)2/dicyclohexyl(2-biphenyl)phosphine/K3PO4 was an efficient catalyst system to prepare 4-aryl-2-chloro- and 2,4-diarylpyrrolo[2,3-d]pyrimidines. Novel non-linear mols. consisting of a pyrrolo[2,3-d]pyrimidine core and aryl branches were elucidated as blue light-emitters with fluorescence quantum yields of 4-67% in THF solution The impact of an electron-withdrawing CO2CMe3 group attached to the pyrrole ring of pyrrolopyrimidines on optical properties is discussed. In addition to this study using 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine, there are many other studies that have used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine) was used in this study.

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2014,Su, Qibin; Ioannidis, Stephanos; Chuaqui, Claudio; Almeida, Lynsie; Alimzhanov, Marat; Bebernitz, Geraldine; Bell, Kirsten; Block, Michael; Howard, Tina; Huang, Shan; Huszar, Dennis; Read, Jon A.; Rivard Costa, Caroline; Shi, Jie; Su, Mei; Ye, Minwei; Zinda, Michael published 《Discovery of 1-Methyl-1H-imidazole Derivatives as Potent Jak2 Inhibitors》.Journal of Medicinal Chemistry published the findings.Synthetic Route of C6H3Cl2N3 The information in the text is summarized as follows:

Structure based design, synthesis, and biol. evaluation of a novel series of 1-methyl-1H-imidazole, as potent Jak2 inhibitors to modulate the Jak/STAT pathway, are described. Using the C-ring fragment from our first clin. candidate AZD1480 (I), optimization of the series led to the discovery of compound II, a potent, orally bioavailable Jak2 inhibitor. Compound II displayed a high level of cellular activity in hematopoietic cell lines harboring the V617F mutation and in murine BaF3 TEL-Jak2 cells. Compound II demonstrated significant tumor growth inhibition in a UKE-1 xenograft model within a well-tolerated dose range. In the experimental materials used by the author, we found 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Synthetic Route of C6H3Cl2N3)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Synthetic Route of C6H3Cl2N3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2018,Andrs, Martin; Pospisilova, Monika; Seifrtova, Martina; Havelek, Radim; Tichy, Ales; Vejrychova, Katerina; Polednikova, Michaela; Gorecki, Lukas; Jun, Daniel; Korabecny, Jan; Rezacova, Martina published 《Purin-6-one and pyrrolo[2,3-d]pyrimidin-4-one derivatives as potentiating agents of doxorubicin cytotoxicity》.Future Medicinal Chemistry published the findings.Category: pyrimidines The information in the text is summarized as follows:

Aim: DNA damage response plays an eminent role in patients′ response to conventional chemotherapy and radiotherapy. Its inhibition is of great interest as it can overcome cancer cell resistance and reduce the EDs of DNA damaging agents. Results & methodol.: We have focused our research on phosphatidylinositol 3-kinase-related kinases and prepared 35 novel compounds through a scaffold hopping approach. The newly synthesized inhibitors were tested on a panel of nine cancer and one healthy cell lines alone and in combination with appropriate doses of doxorubicin. Conclusion: Five novel compounds 4f, 10b, 15g, 7e and 15f in combination with doxorubicin showed significant antiproliferative effect on seven cancer cell lines while not affecting the cell growth alone. In the experiment, the researchers used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Category: pyrimidines)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Category: pyrimidinesThey 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