Month: November 2022

On January 27, 2017, Zhao, Dan; Huang, Shanshan; Qu, Menghua; Wang, Changyuan; Liu, Zhihao; Li, Zhen; Peng, Jinyong; Liu, Kexin; Li, Yanxia; Ma, Xiaodong; Shu, Xiaohong published an article.Category: amides-buliding-blocks The title of the article was Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton’s tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. And the article contained the following:

A new series of diphenylpyrimidine derivatives (DPPYs) bearing various aniline side chains at the C-2 position of pyrimidine core were synthesized as potent BTK inhibitors. Most of these inhibitors displayed improved activity against B leukemia cell lines compared with lead compound spebrutinib. Subsequent studies showed that the peculiar inhibitor I, with IC50 values of 10.5 μM against Ramos cells and 19.1 μM against Raji cells, also displayed slightly higher inhibitory ability than the novel agent ibrutinib. Moreover, compound I is not sensitive to normal cells PBMC, indicating low cell cytotoxicity. In addition, flow cytometry anal. indicated that I significantly induced the apoptosis of Ramos cells, and arrested the cell cycle at the G0/G1 phase. These explorations provided new clues to discover pyrimidine scaffold as more effective BTK inhibitors. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to diphenylpyrimidine preparation bruton tyrosine kinase inhibitory activity, btk, inhibitor, leukemia, pyrimidine, synthesis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On March 24, 2022, Zhao, Hong-Yi; Wang, Hai-Peng; Mao, Yu-Ze; Zhang, Hao; Xin, Minhang; Xi, Xiao-Xiao; Lei, Hao; Mao, Shuai; Li, Dong-Hui; Zhang, San-Qi published an article.SDS of cas: 16230-24-3 The title of the article was Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. And the article contained the following:

To overcome the intractable problem of drug resistance, proteolysis targeting chimeras (PROTACs) targeting EGFR mutants were developed by optimizing covalent EGFR ligands. Covalent or reversible covalent pyrimidine- or purine-containing PROTACs were designed, synthesized, and evaluated. As a consequence, covalent PROTAC I, with a novel purine-containing EGFR ligand, was discovered as a highly potent degrader against EGFRL858R/T790M and EGFRdel19, reaching the lowest DC50 values among all reported EGFR-targeting PROTACs. Furthermore, I exhibited excellent cellular activity against the H1975 and HCC827 cell lines with high selectivity. Mechanism investigation indicated that the lysosome was involved in the degradation process. Importantly, the covalent binding strategy was proven to be an effective approach for the design of PROTACs targeting EGFRL858R/T790M, which laid the practical foundation for further development of potent EGFR-targeting PROTACs. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).SDS of cas: 16230-24-3

The Article related to pyrimidine preparation antitumor egfr inhibition sar mol docking, purine preparation antitumor egfr inhibition sar mol docking, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On December 27, 2018, Cho, Seong Yun; Kim, Pil Ho; Lee, Jeong Ok; Kim, Hyeong Rae; Ha, Jae Du; Jung, Hui Jeong; Yoon, Chang Su; Park, Ji Hun; Hwang, Jong Yeon published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was Fused pyrimidine derivative as Bruton’s tyrosine kinase inhibitor, and method for the preparation thereof. And the patent contained the following:

Disclosed are compound I [n = 0 or 1; A = single bond, -NH- or -O-; D1 = CR4 or N; R4 = H or alkyl; D2 = CH or N; D3 = N or NH; a dotted line accompanied by a solid line represents a single bond or a double bond; R1 = (un)substituted aryl; R2, R3 = independently H, (un)substituted aryl, (un)substituted cycloalkyl, etc.; or its optical isomer or pharmaceutically acceptable salt] and pharmaceutical compositions For example, compound II was prepared from malononitrile via conversion to 4,6-dichloro-3-methyl-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-d]pyrimidine followed by treatment with K2CO3/N-(1s,4s)-(4-aminocyclohexyl)acrylamide and Pd2(dba)3-catalyzed reaction with 4-morpholinoaniline. The invention compound showed high inhibitory activity for Bruton’s tyrosine kinase (BTK), e.g., IC50 value of II was 0.001 μM. Compound I is claimed useful for the treatment of cancer or autoimmune disease. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application In Synthesis of N-(3-Aminophenyl)acrylamide

The Article related to fused pyrimidine preparation bruton tyrosine kinase inhibitor, cancer autoimmune disease treatment fused pyrimidine btk inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of N-(3-Aminophenyl)acrylamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On August 1, 2021, Wang, Zhengjie; Liu, Limin; Dai, Honglin; Si, Xiaojie; Zhang, Luye; Li, Erdong; Yang, Zhang; Chao, Gao; Zheng, Jiaxin; Ke, Yu; Shan, Lihong; Zhang, Qiurong; Liu, Hongmin published an article.Related Products of 16230-24-3 The title of the article was Design, synthesis and biological evaluation of novel 2,4-disubstituted quinazoline derivatives targeting H1975 cells via EGFR-PI3K signaling pathway. And the article contained the following:

In order to find new and highly effective anti-tumor drugs with targeted therapeutic effects, a series of novel 4-aminoquinazoline derivatives containing N-phenylacetamide structure were designed, synthesized and evaluated for antitumor activity against four human cancer cell lines (H1975, PC-3, MDA-MB-231 and MGC-803) using MTT assay. The results showed that the compound I had the most potent antiproliferative activity against H1975, PC-3, MDA-MB-231 and MGC-803 cell lines. At the same time, compound 19e could significantly inhibit the colony formation and migration of H1975 cells. Compound I also arrested the H1975 cell cycle in the G1 phase and mediated cell apoptosis, promoted the accumulation of ROS in H1975 cells. Furthermore, compound I exerted antitumor effect in vitro by reducing the expression of anti-apoptotic protein Bcl-2 and increasing the pro-apoptotic protein Bax and p53. Mechanistically, compound I could significantly decreased the phosphorylation of EGFR and its downstream protein PI3K in H1975 cells. Which indicated that compound I targeted H1975 cell via interfering with EGFR-PI3K signaling pathway. Mol. docking showed that compound I could bind into the active pocket of EGFR. Those work suggested that compound I would have remarkable implications for further design of anti-tumor agents. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Related Products of 16230-24-3

The Article related to quinazoline preparation antiproliferation antitumor mol docking apoptosis egfr, antiproliferation, cell cycle analysis, egfr, quinazoline, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On May 3, 2022, Younis, Osama; Sayed, Mostafa; Mohammed, Ahmed A. K.; Tolba, Mahmoud S.; Hassanien, Reda; Kamal El-Dean, Adel M.; Tsutsumi, Osamu; Ahmed, Mostafa published an article.Recommanded Product: 79-07-2 The title of the article was Solid-State Luminescent Materials Containing Both Indole and Pyrimidine Moieties: Design, Synthesis, and Density Functional Theory Calculations. And the article contained the following:

Heterocyclic compounds with effective solid-state luminescence offer a wide range of uses. It has been observed that combining pyrimidine and indole moieties in a single mol. can enhance material behavior dramatically. Here, different heterocyclic compounds with indole and pyrimidine moieties have been synthesized effectively, and their structures have been validated using NMR, IR, and mass spectroscopy. The photoluminescence behavior of two substances was investigated in powder form and solutions of varying concentrations After aggregation, one mol. displayed a red shifted luminescence spectrum, whereas another homolog showed a blueshift. Thus, d. functional theory calculations were carried out to establish that introducing a terminal group allows modifying of the luminescence behavior by altering the mol. packing. Because of the non-planarity, intermol. interactions, and tiny intermol. distances within the dimers, the materials demonstrated a good emission quantum yield (Φem) in the solid state (ex. 25.6%). At high temperatures, the compounds also demonstrated a stable emission characteristic. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Recommanded Product: 79-07-2

The Article related to design synthesis luminescence dft indole pyrimidine derivative, solid state luminescent material aggregation indole pyrimidine derivative, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 79-07-2

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On June 19, 2014, Ahmed, Mahbub; Ashall-Kelly, Alexander; Bloomfield, Graham Charles; Gueritz, Louisa; McKenna, Jeffrey; McKenna, Joseph; Mutton, Simon; Parmar, Rakesh; Sheperd, Jon; Wright, Paul published a patent.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione The title of the patent was Preparation of tricyclic compounds as CFTR channel inhibitors for treating polycystic kidney disease and diarrhea. And the patent contained the following:

The invention provides tricyclic compounds of general formula I or a pharmaceutical salt thereof, their use for inhibiting the CFTR channel, and methods of treating disease using same, particularly polycystic kidney disease and diarrhea. For I, R1 is Ph, (C4-C7)cycloalkenyl or a 5-6-membered heteroaryl ring, all optionally substituted; R2 is (C1-C6)alkyl, (C3-C7)cycloalkyl, (C4-C7)cycloalkenyl, etc., all optionally substituted; each R3 independently is Me or ethyl; R4 is hydrogen, (C1-C4)alkyl, halo(C1-C4)alkyl, etc.; R4′ is H or methyl; R4a is hydrogen, (C1-C4)alkyl, halo(C1-C4)alkyl, etc.; and X is O, NH, NMe, or -CH2-O- wherein the O atom is attached to the -C(R4)(R4′) atom of the ring. Pharmaceutical compositions containing I, alone or in combination with other active agents, are also disclosed. Synthetic procedures for preparing I are exemplified. Example compound (R)-II was prepared by reacting intermediate III with 5-methylfuran-2-carboxaldehyde and subjecting the racemate formed to chiral separation Using the Ion Works Quatro assay (R)-II had a CFTR IC50 of 1.58 μM. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

The Article related to tricyclic compound preparation cftr channel inhibitor polycystic kidney disease, diarrhea treatment tricyclic compound cftr channel inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On May 1, 2012, Takahashi, Daisuke; Honda, Yutaka; Izawa, Kunisuke published an article.Product Details of 27115-50-0 The title of the article was Syntheses of 5-amino-2-phenyl-4(3H)-pyrimidinone derivatives starting with glycine. And the article contained the following:

N-Cbz-5-amino-2-phenyl-4(3H)-pyrimidinone was prepared from the Na salt of Me (hydroxymethylene)glycinate and benzamidine.HCl in good yield. However, the reaction with N-substituted benzamidine did not proceed to give the desired pyrimidinone. In contrast, the reaction of 4-ethoxymethylene-2-phenyl-5(4H)-oxazolone, readily prepared from hippuric acid and N-substituted benzamidine, proceeded nicely to give 5-(benzoylamino)-6-oxo-2-phenyl-1(6H)-pyrimidineacetate in high yield. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Product Details of 27115-50-0

The Article related to glycine benzamidine cyclocondensation, hippuric acid benzamidine cyclocondensation, aminopyrimidinone preparation, pyrimidinone amino preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 27115-50-0

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On February 1, 2020, Khalil, Nadia A.; Ahmed, Eman M.; Zaher, Ashraf F.; El-Zoghbi, Mona S.; Sobh, Eman A. published an article.Recommanded Product: 2-Chloroacetamide The title of the article was Synthesis of certain benzothieno[3,2-d]pyrimidine derivatives as a selective SIRT2 inhibitors. And the article contained the following:

A series of new benzothieno[3,2-d]pyrimidine derivatives were designed and synthesized. The National Cancer Institute (NCI, USA) evaluated all synthesized compounds against 60 human tumor cell lines. Most of the compounds showed good cytotoxicity against MCF-7 breast cancer cell line and UO-31 renal cancer cell line (growth inhibitory range: 17.88%-68.65%). IC50 of twelve most active compounds was determined against MCF-7 and UO-31 cell lines. IC50 against SIRT2 enzyme was evaluated for the most active compounds to explore the mechanism of antiproliferative activity. The best activity was displayed by compound I (IC50 = 2.10μg/mL), which is 6.6 more potent than cambinol as a reference Moreover, compound I displayed high selectivity against SIRT1 and SIRT2 over SIRT3 in the selectivity studies and displayed twice activity of cambinol in hyperacetylation of α-tubulin protein with IC50 = 32.05μg/mL. Mol. docking study of the synthesized compounds into SIRT2 active site was performed to rationalize the remarkable SIRT2 inhibitory activity. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Recommanded Product: 2-Chloroacetamide

The Article related to benzothienopyrimidine preparation antitumor sirutin inhibition mol docking sar, benzothieno[3,2-d]pyrimidines, cytotoxic activity, sirt2 inhibitors, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 2-Chloroacetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On June 16, 2017, Song, Zhendong; Huang, Shanshan; Yu, Haiqing; Jiang, Yu; Wang, Changyuan; Meng, Qiang; Shu, Xiaohong; Sun, Hunjun; Liu, Kexin; Li, Yanxia; Ma, Xiaodong published an article.Category: amides-buliding-blocks The title of the article was Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC). And the article contained the following:

Potential new EGFRT790M inhibitors comprising of structurally modified diphenylpyrimidine derivatives bearing a morpholine functionality (Mor-DPPYs), e.g., I were synthesized and used to improve the activity and selectivity of gefitinib-resistant non-small cell lung cancer (NSCLC) treatment. This led to the identification of inhibitor I, which displayed high activity against EGFRT790M/L858R kinase (IC50 = 0.71 nM) and repressed H1975 cell replication harboring EGFRT790M mutations at a concentration of 0.037 μM. Inhibitor I demonstrated high selectivity (SI = 631.9) for T790M-containing EGFR mutants over wild type EGFR and suggested that it will cause few side effects. Moreover, this compound also shows promising antitumor efficacy in a murine EGFRT790M/L858R-driven H1975 xenograft model without affecting body weight This study provides new potential lead compounds for further development of anti-NSCLC drugs. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to acrylamide diphenylaminopyrimidinyl morpholino preparation antitumor egfr kinase mol modeling, egfr t790m, inhibitors, nsclc, pyrimidine, resistance, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zaki, Remon M.; El-Ossaily, Yasser A.; Geies, Ahmed A. published an article in 2020, the title of the article was A convenient green synthetic approach to the synthesis of novel bioactive selenolo[2,3-c]pyrazoles as antibacterial and antifungal agents.Application of 79-07-2 And the article contains the following content:

A series of new pyrimidine, triazine, and isoindole heterocycles fused to the selenolopyrazole ring system, e.g., I, was synthesized by various condensation reactions of selenolopyrazole II, which was prepared by a new green methodol. The fused pyrimidinone compound I was used as a versatile precursor for several aromatic nucleophilic substitution reactions to produce sulfanyl- and amino-substituted pyrimidines. Furthermore, some of the compounds were screened against various pathogenic bacterial and fungal strains. Their results demonstrated that some of them revealed remarkable antimicrobial activities. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Application of 79-07-2

The Article related to selenolopyrazole green preparation antibacterial antifungal activity sar, pyrazoloselenolopyrimidine green preparation antibacterial antifungal activity sar, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 79-07-2

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics