Tag: 100-200

The author of 《Syntheses of heterocyclic compounds. CDXCI. Pyrimidine derivatives. V. Abnormal condensation products of 4-amino-6-chloro-2-methoxypyrimidine with p-nitrobenzenesulfonyl chloride》 were Okui, Kiyoshi; Ito, Kiyohiko; Koizumi, Masuo; Fukumoto, Keiichiro; Kametani, Tetsuji. And the article was published in Journal of Heterocyclic Chemistry in 1972. HPLC of Formula: 3286-56-4 The author mentioned the following in the article:

Condensation of 4-amino-6-chloro-2-methoxypyrimidine with p-O2NC6H4SO2Cl gave, in addition to 6-chloro-2-methoxy-4-(p-nitrobenzenesulfonamido)pyrimidine (I), two abnormal by-products, 1-[2-methoxy-4-(p-nitrobenzenesulfonamido)pyrimidin-6-yl]pyridinium N,N-betaine (II) and N-(p-nitrobenzenesulfonyl)-β-ureido-β-pyridinium arcylamide N,N-betaine (III). The experimental part of the paper was very detailed, including the reaction process of 6-Chloro-2-ethoxypyrimidin-4-amine(cas: 3286-56-4HPLC of Formula: 3286-56-4)

6-Chloro-2-ethoxypyrimidin-4-amine(cas: 3286-56-4) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.HPLC of Formula: 3286-56-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

SDS of cas: 90213-66-4In 2022 ,《Design, synthesis and biological evaluation of 7-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-2,3-dihydro-1H-inden-1-one derivatives as potent FAK inhibitors for the treatment of ovarian cancer》 appeared in European Journal of Medicinal Chemistry. The author of the article were Wei, Wei; Feng, Zhanzhan; Liu, Zhihao; Li, Xinyue; He, Hualong; Ran, Kai; Shi, Yaojie; Zhu, Yongxia; Ye, Tinghong; Gao, Chao; Wang, Ningyu; Yu, Luoting. The article conveys some information:

Focal adhesion kinase (FAK) promotes tumor progression by intracellular signal transduction and regulation of gene expression and protein turnover, which is a compelling therapeutic target for various cancer types, including ovarian cancer. However, the clin. responses of FAK inhibitors remain unsatisfactory. Here, we describe the discovery of FAK inhibitors using a scaffold hopping strategy. Structure-activity relationship (SAR) exploration identified 3-Methoxy-4-((4-((3-oxo-2,3-dihydro-1H-inden-4-yl)oxy)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-N-(piperidin-4-yl)benza-mide as a potent FAK inhibitor, which exhibited inhibitory activities against FAK signaling in vitro. Treatment with 3-Methoxy-4-((4-((3-oxo-2,3-dihydro-1H-inden-4-yl)oxy)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-N-(piperidin-4-yl)benza-mide not only decreased migration and invasion of PA-1 cells, but also reduced expression of MMP-2 and MMP-9. Moreover, 3-Methoxy-4-((4-((3-oxo-2,3-dihydro-1H-inden-4-yl)oxy)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-N-(piperidin-4-yl)benza-mide inhibited tumor growth and metastasis, and no obvious adverse effects were observed during the in vivo study. These results revealed the potential of FAK inhibitor 3-Methoxy-4-((4-((3-oxo-2,3-dihydro-1H-inden-4-yl)oxy)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-N-(piperidin-4-yl)benza-mide for treatment of ovarian cancer. In the experiment, the researchers used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4SDS of cas: 90213-66-4)

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. SDS of cas: 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

SDS of cas: 90213-66-4In 2015 ,《Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor》 appeared in ACS Medicinal Chemistry Letters. The author of the article were Hatcher, John M.; Zhang, Jinwei; Choi, Hwan Geun; Ito, Genta; Alessi, Dario R.; Gray, Nathanael S.. The article conveys some information:

Activating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson’s disease (PD) patients and may represent an attractive therapeutic target. Here the authors report JH-II-127 I, as a potent and selective inhibitor of both wild-type and G2019S mutant LRRK2. Compound I substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 μM in a variety of cell types and is capable of inhibiting Ser935 phosphorylation in mouse brain following oral delivery of doses as low as 30 mg/kg. After reading the article, we found that the author used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4SDS of cas: 90213-66-4)

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. SDS of cas: 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Name: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidineIn 2012 ,《Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization》 appeared in European Journal of Medicinal Chemistry. The author of the article were Xie, Hui; Zeng, Lili; Zeng, Shaogao; Lu, Xin; Zhang, Guicheng; Zhao, Xin; Cheng, Na; Tu, Zhengchao; Li, Zhiyuan; Xu, Hongjiang; Yang, Ling; Zhang, Xiquan; Huang, Min; Zhao, Junling; Hu, Wenhui. The article conveys some information:

We previously reported a highly potent DPP-IV inhibitor 6 with low in vivo efficacy. While trying to maintain consistent in vitro and in vivo biol. activity, we initiated a pharmacokinetic property-driven optimization to improve the metabolic stability and permeability of inhibitor 6. A simple scaffold replacement of thienopyrimidine with pyrrolopyrimidine (21a) led to significantly improved metabolic stability (4% vs. 65% remaining). Further modification of the pyrrolopyrimidine scaffold to produce compound 21j resulted in much better oral bioavailability than 6. Importantly, compound 21j exhibits greater in vivo efficacy than does 6 and Alogliptin and is worthy of further development.2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Name: 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. Name: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2022,Yuan, Kai; Kuang, Wenbin; Chen, Weijiao; Ji, Minghui; Min, Wenjian; Zhu, Yasheng; Hou, Yi; Wang, Xiao; Li, Jiaxing; Wang, Liping; Yang, Peng published an article in European Journal of Medicinal Chemistry. The title of the article was 《Discovery of novel and orally bioavailable CDK 4/6 inhibitors with high kinome selectivity, low toxicity and long-acting stability for the treatment of multiple myeloma》.Application of 3934-20-1 The author mentioned the following in the article:

Multiple myeloma (MM) ranks second in malignant hematopoietic cancers, and the most common anti-MM drugs easily generate resistance. CDK4/6 have been validated to play determinant roles in MM, but no remarkable progress has been obtained from clin. trials of CDK4/6 inhibitors for MM. To discover novel CDK6 inhibitors with better potency and high druggability, structure-based virtual screening was conducted to identify compound I. Further chem. optimization afforded a better derivative, compound II, which exhibited strong inhibition of CDK4/6 and showed high selectivity over 360+ kinases, including homologous CDKs. The in vivo evaluation demonstrated that compound II possessed low toxicity (LD50 > 10,000 mg/kg), favorable bioavailability (F% = 51%), high metabolic stability (t1/2 > 24 h) and strong anti-MM potency. In summary, we discovered a novel CDK4/6 inhibitor bearing favorable drug-like properties and offered a great candidate for MM preclin. studies. The experimental part of the paper was very detailed, including the reaction process of 2,4-Dichloropyrimidine(cas: 3934-20-1Application of 3934-20-1)

2,4-Dichloropyrimidine(cas: 3934-20-1) is a member of organic chlorides. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Application of 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Makova, Barbara; Mik, Vaclav; Liskova, Barbora; Gonzalez, Gabriel; Vitek, Dominik; Medvedikova, Martina; Monfort, Beata; Rucilova, Veronika; Kadlecova, Alena; Khirsariya, Prashant; Gandara Barreiro, Zoila; Havlicek, Libor; Zatloukal, Marek; Soural, Miroslav; Paruch, Kamil; D’Autreaux, Benoit; Hajduch, Marian; Strnad, Miroslav; Voller, Jiri published an article in 2021. The article was titled 《Cytoprotective activities of kinetin purine isosteres》, and you may find the article in Bioorganic & Medicinal Chemistry.Electric Literature of C6H3Cl2N3 The information in the text is summarized as follows:

Kinetin (N6-furfuryladenine), a plant growth substance of the cytokinin family, has been shown to modulate aging and various age-related conditions in animal models. Here, the authors report the synthesis of kinetin isosteres with the purine ring replaced by other bicyclic heterocycles, and the biol. evaluation of their activity in several in vitro models related to neurodegenerative diseases. The findings indicate that kinetin isosteres protect Friedreichs ataxia patient-derived fibroblasts against glutathione depletion, protect neuron-like SH-SY5Y cells from glutamate-induced oxidative damage, and correct aberrant splicing of the ELP1 gene in fibroblasts derived from a familial dysautonomia patient. Although the mechanism of action of kinetin derivatives remains unclear, this data suggest that the cytoprotective activity of some purine isosteres is mediated by their ability to reduce oxidative stress. Further, the studies of permeation across artificial membrane and model gut and blood-brain barriers indicate that the compounds are orally available and can reach the central nervous system. Overall, the data demonstrate that isosteric replacement of the kinetin purine scaffold is a fruitful strategy for improving known biol. activities of kinetin and discovering novel therapeutic opportunities. In the part of experimental materials, we found many familiar compounds, such as 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Electric Literature 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. Electric Literature of C6H3Cl2N3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Yang, Fan; Su, Huilin; Deng, Ji; Mou, Luohe; Wang, Huali; Li, Rong; Dai, Qing-Qing; Yan, Yu-Hang; Qian, Shan; Wang, Zhouyu; Li, Guo-Bo; Yang, Lingling published an article in 2021. The article was titled 《Discovery of new human Sirtuin 5 inhibitors by mimicking glutaryl-lysine substrates》, and you may find the article in European Journal of Medicinal Chemistry.COA of Formula: C4H2Cl2N2 The information in the text is summarized as follows:

Human sirtuin 5 (SIRT5) plays pivotal roles in metabolic pathways and other biol. processes, and is involved in several human diseases including cancer. Development of new potent and selective SIRT5 inhibitors is currently desirable to provide potential therapeutics for related diseases. Herein, we report a series of new 3-thioureidopropanoic acid derivatives, which were designed to mimic the binding features of SIRT5 glutaryl-lysine substrates. Structure-activity relationship studies revealed several compounds with low micromolar inhibitory activities to SIRT5. Computational and biochem. studies indicated that these compounds exhibited competitive SIRT5 inhibition with respect to the glutaryl-lysine substrate rather than NAD cofactor. Moreover, they showed high selectivity for SIRT5 over SIRT1-3 and 6 and could stabilize SIRT5 proteins as revealed by thermal shift analyses. This work provides an effective substrate-mimicking strategy for future inhibitor design, and offers new inhibitors to investigate their therapeutic potentials in SIRT5-associated disease models. After reading the article, we found that the author used 2,4-Dichloropyrimidine(cas: 3934-20-1COA of Formula: C4H2Cl2N2)

2,4-Dichloropyrimidine(cas: 3934-20-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.COA of Formula: C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Introducing rigid pyrimidine ring to improve the mechanical properties and thermal-oxidative stabilities of phthalonitrile resin》 was written by Yang, Kaixiong; Chen, Xinggang; Zhang, Zhenjiang; Yu, Xiaoyan; Naito, Kimiyoshi; Zhang, Qingxin. Formula: C4H2Cl2N2 And the article was included in Polymers for Advanced Technologies in 2020. The article conveys some information:

In this study, a novel phthalonitrile monomer containing pyrimidine ring, 4,6-bis[3-(3,4-dicyanophenoxy)phenoxy]pyrimidine (BCPM), was successfully synthesized by nucleophilic substitution reaction with resorcinol, 4,6-dichloropyrimidine and 4-nitrophthalonitrile. The BCPM monomer was cured by different temperature programs with 4-(aminophenoxy)phthalonitrile (APPH) as catalyst to give the polymers. The mol. structures of the BCPM monomer and the polymers were investigated by Fourier transform IR (FTIR) spectroscopy and NMR (NMR) spectroscopy. Differential scanning calorimetric (DSC) anal. was performed to study the processability of the BCPM monomer, which showed a wide processing window of about 117°. The mech. properties and thermal-oxidative stability of the polymer were characterized by dynamic mech. anal. (DMA) and thermogravimetric anal. (TGA), resp., which indicated that the polymers exhibited excellent storage modulus, high glass transition temperature over 400°, and outstanding thermal stability. The polymers also have low water absorption capacity and are suitable for humid environments. In the experiment, the researchers used 4,6-Dichloropyrimidine(cas: 1193-21-1Formula: C4H2Cl2N2)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Formula: C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《An efficient synthesis of designed 4-thiazolidinone fused pyrimidine derivatives as potent antimicrobial agents》 was written by Patel, Janki J.; Morja, Mayur I.; Chikhalia, Kishor H.. Name: 2,4,6-Trichloropyrimidine And the article was included in Journal of Heterocyclic Chemistry in 2020. The article conveys some information:

A novel series of hybrid 2-substituted [(pyrimidin-2-yl)hydrazinyl]thiazolidin-4-one derivatives I [R = H, 3-Cl, 4-NO2, etc.] was synthesized via aromatic nucleophilic displacement of chlorine atoms/intermol. cyclization of 2-chloro-N’-[6-morpholino-4-[(substituted-phenyl)amino]pyrimidin-2-yl]acetohydrazides II with ammonium thiocyanate. I were evaluated for their antibacterial and antifungal activities against various strains of bacteria and fungi. Structure-activity relationship and HOMO-LUMO studies were also carried out for confirming structure-biol. activity. Thus, these studies suggested that hydrazinyl pyrimidine derivatives I bearing a thiazolidinone moiety are interesting scaffolds for the development of novel antimicrobial agents. After reading the article, we found that the author used 2,4,6-Trichloropyrimidine(cas: 3764-01-0Name: 2,4,6-Trichloropyrimidine)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Name: 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Design, synthesis, and anticancer evaluation of acetamide and hydrazine analogues of pyrimidine》 was published in Journal of Heterocyclic Chemistry in 2020. These research results belong to Khazir, Jabeena; Mir, Bilal Ahmad; Chashoo, Gousia; Maqbool, Tariq; Riley, Darren; Pilcher, Lynne. Product Details of 1193-21-1 The article mentions the following:

A library of acetamide I [R = 2-hydroxyethylamino, 1-pyrrolidinyl, N-morpholinyl, etc.] and hydrazine II [R1 = 1-pyrrolidinyl, 1-piperidinyl, N-morpholinyl, 4-propanoyl-1-piperidyl; R2 = H, 2-Br, 3,4-di-MeO, etc.] analogs were generated on the pyrimidine ring through a multistep reaction starting from 5-nitro-pyrimidine-4,6-diol and pyrimidine-4,6-diol, resp. The synthesized analogs I and II were screened for in-vitro cytotoxic activity against various human cancer cell lines like HCT-1 and HT-15 (colon), MCF-7(breast), PC-3 (prostrate), SF268 (CNS) using MTT method. From the bioassay results, it was observed that even though many of the synthesized derivatives I and II exhibited a good potency against various screened cancer cell lines, compound I [R = 1-piperidinyl] showed potent anticancer activity on all the tested cancer cell lines with IC50 value of 0.36μM on CNS cell line and 1.6μM on HT-21 cell line, and compound II [R1 = N-morpholinyl, R2 = 2-OH] showed potent activity against three tested cancer cell lines with IC50 value of 0.76μM on HT-29 cell line, 2.6μM on HCT-15 and 3.2μM on MCF-7 cell line. After reading the article, we found that the author used 4,6-Dichloropyrimidine(cas: 1193-21-1Product Details of 1193-21-1)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Product Details of 1193-21-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia