Category: 16230-24-3

On January 31, 2021, Li, Si; Wu, Bin; Zheng, Xu; Wang, Changyuan; Zhao, Jingyuan; Sun, Huijun; Sun, Xiuli; Tang, Zeyao; Yuan, Hong; Chen, Lixue; Ma, Xiaodong published an article.Synthetic Route of 16230-24-3 The title of the article was Synthesis and biological activity of imidazole group-substituted arylaminopyrimidines (IAAPs) as potent BTK inhibitors against B-cell lymphoma and AML. And the article contained the following:

Bruton’s tyrosine kinase (BTK) is a member of the Tec kinase family and plays a key role in the modulation of the B-cell receptor (BCR)-mediated signaling pathway. Inhibition of BTK has been proven to be an effective therapeutic approach for various hematol. malignancies, such as chronic lymphocytic leukemia (CLL), mantle cell leukemia (MCL), diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML). Here, a new series of imidazole group-substituted arylaminopyrimidines (IAAPs) were designed and synthesized as potent inhibitors of the enzymic activity of BTK with a half maximal inhibitory concentration (IC50) ranging from 13.10 to 42.40 nM. In particular, 11a and 11b exhibited stronger antiproliferative activity against AML and B lymphomas cell lines compared with BTK inhibitor ibrutinib and showed low cytotoxicity against normal peripheral blood mononuclear cells (PBMCs). In addition, anal. of the mechanism of action of these compounds revealed that 11a and 11b induced significant apoptosis in AML and B lymphoma cells by arresting the cell cycle at the G1/G0 or G2/M stage and blocked BTK autophosphorylation as well as the ensuing abrogation of pro-survival AKT and ERK signaling. Taken together, these results suggest that 11a and 11b might serve as valuable preclin. candidates for the treatment of AML and B-cell lymphoma. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Synthetic Route of 16230-24-3

The Article related to aml iaap btk inhibitor bcell lymphoma cell cycle akt, aml, b-cell lymphoma, btk inhibitors, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 16230-24-3

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

On January 15, 2017, Ge, Yang; Yang, Haijun; Wang, Changyuan; Meng, Qiang; Li, Lei; Sun, Huijun; Zhen, Yuhong; Liu, Kexin; Li, Yanxia; Ma, Xiaodong published an article.Application of 16230-24-3 The title of the article was Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton’s tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines. And the article contained the following:

A family of phosphoryl-substituted diphenylpyrimidine derivatives (Pho-DPPYs) were synthesized and biol. evaluated as potent BTK inhibitors in this study. Compound 7b was found to markedly inhibit BTK activity at concentrations of 0.82 nmol/L, as well as to suppress the proliferations of B-cell leukemia cell lines (Ramos and Raji) expressing high levels of BTK at concentrations of 3.17 μM and 6.69 μM. Moreover, flow cytometry anal. results further indicated that 7b promoted cell apoptosis to a substantial degree. In a word, compound 7b is a promising BTK inhibitor for the treatment of B-cell lymphoblastic leukemia. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to preparation phosphoryl derivative diphenylpyrimidine bruton’s kinase inhibitor leukemia, btk, dppy, inhibitor, leukemia, phosphoryl, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application of 16230-24-3

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

Yi, Yuanyuan; Wang, Luhong; Zhao, Dan; Huang, Shanshan; Wang, Changyuan; Liu, Zhihao; Sun, Huijun; Liu, Kexin; Ma, Xiaodong; Li, Yanxia published an article in 2018, the title of the article was Structural optimization of diphenylpyrimidine scaffold as potent and selective epidermal growth factor receptor inhibitors against L858R/T790M resistance mutation in non-small cell lung cancer.HPLC of Formula: 16230-24-3 And the article contains the following content:

A new class of thiodiphenylpyrimidine analogs (Thio-DPPY) were synthesized as potent and selective EGFR T790M inhibitors to overcome gefitinib resistance in non-small cell lung cancer (NSCLC). This structural optimization led to the identification of two potent EGFRT790M/L858R inhibitors, 14a (N-[3-[[5-chloro-2-[4-((1-morpholino)propylthio)phenylamino]-4-pyrimidinyl]amino]phenyl]-2-propenamide) and 14e (N-[3-[[5-chloro-2-[4-((1-morpholino)ethanethioate)phenylamino]-4-pyrimidinyl]oxygen]phenyl]-2-propenamide), which possess IC50 values of 27.5 and 9.1 nM, resp. Moreover, compounds 14a (SI > 36.4) and 14e (SI > 109.9) exhibited high selectivity and low activity against the wild-type EGFR (IC50 > 1000 nM). In particular, compound 14a also displayed strong potency against EGFRT790M-mutated H1975 cells (IC50 = 0.074 μM), but weak activity toward normal cells HBE (IC50 > 40 μM) and LO-2 (IC50 = 9.891 μM). It is important that compound 14a (SI = 52.6) significantly improved the selectivity against mutant H1975 cells over wild-type A431 cells than rociletinib (SI = 6.0), thus revealing its slight cell cytotoxicity. This study provides a promising Thio-DPPY derivative as enhanced EGFR T790M inhibitor, and also revealed valuable clues for further optimization of DPPY scaffold to overcome NSCLC resistance. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).HPLC of Formula: 16230-24-3

The Article related to diphenylpyrimidine preparation egf receptor inhibitor mutation antitumor lung nsclc, egfr t790m, nsclc, inhibitors, pyrimidine, resistance, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.HPLC of Formula: 16230-24-3

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

Sun, Bo; Liu, Xiaowen; Zheng, Xu; Wang, Changyuan; Meng, Qiang; Sun, Huijun; Shu, Xiaohong; Liu, Kexin; Sun, Xiuli; Li, Yanxia; Ma, Xiaodong published an article in 2020, the title of the article was Novel Pyrimidines as Multitarget Protein Tyrosine Kinase Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis (IPF).Recommanded Product: 16230-24-3 And the article contains the following content:

A new class of pyrimidine derivatives were identified as potent protein tyrosine kinase (PTK) inhibitors for the treatment of idiopathic pulmonary fibrosis (IPF). Most of these small-mol. inhibitors displayed strong enzymic activity against BTK and JAK3 kinases at concentrations lower than 10 nM. The representative compound N-(3-((5-chloro-2-(4-((1-morpholino)acetylamino)phenylamino)-4-pyrimidinyl)amino)phenyl)acrylamide (6 a) also exhibited high inhibitory potency toward both BTK and JAK kinase families, as well as ErbB4, at a concentration of 10 nM, achieving rates of inhibition higher than 57%. Addnl., in vivo biol. evaluations showed that 6 a can remarkably decrease the severity of IPF disease. All these investigations suggested that the multi-PTK inhibitor 6 a may serve as a promising agent for the treatment of IPF. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Recommanded Product: 16230-24-3

The Article related to pyrimidine derivative preparation tyrosine kinase inhibitor idiopathic pulmonary fibrosis, ipf, ptk, inhibitors, multitarget, pyrimidine, Pharmacology: Effects Of Inflammation Inhibitors and Immune Agents and other aspects.Recommanded Product: 16230-24-3

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

On January 15, 2020, Zhu, Yanming; Zheng, Xu; Wang, Changyuan; Sun, Xiuli; Sun, Huijun; Ma, Tengyue; Li, Yanxia; Liu, Kexin; Chen, Lixue; Ma, Xiaodong published an article.Product Details of 16230-24-3 The title of the article was Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. And the article contained the following:

Idiopathic pulmonary fibrosis (IPF) is a serious and fatal lung disease, with a median survival of only 3-5 years from diagnosis. Janus kinase 3 (JAK3) has a well-established role in the pathogenesis of various autoimmune diseases, including rheumatoid arthritis (RA) and autoimmune-related pulmonary fibrosis. In this study, through the use of a conformationally-constrained design strategy, a series of thieno[3,2-d]pyrimidines were synthesized as potent JAK3 inhibitors for the treatment of IPF. Among them, the most potent JAK3 inhibitor, namely 8e (IC50 = 1.38 nM), significantly reduced the degree of airsacculitis and fibrosis according to hematoxylin-eosin (HE) staining assay for the lung tissue in the bleomycin (BLM)-induced pulmonary fibrosis mouse model. The clear reduction of the lung collagen deposition by the determination of Masson and hydroxyproline (HYP) content also demonstrated its efficacy in the treatment of fibrosis. In addition, 8e also reduced the expression of the inflammatory markers IL-6, IL-17A, TNF-α and malondialdehyde (MDA) in lung tissue, which indicated its higher anti-inflammatory activity compared with that of the reference agents (nintedanib and gefitinib). Furthermore, it possessed low cytotoxicity against normal human bronchial epithelia (HBE) cells (IC50 > 39.0μM) and C57BL mice. All these evaluated biol. properties suggest that 8e may be a potential JAK3 inhibitor for the treatment of IPF. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Product Details of 16230-24-3

The Article related to thieno pyrimidine derivative preparation jak3 inhibitors idiopathic pulmonary fibrosis, idiopathic pulmonary fibrosis, jak inhibitors, thieno[3,2-d]pyrimidines, Pharmacology: Effects Of Inflammation Inhibitors and Immune Agents and other aspects.Product Details of 16230-24-3

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

On April 19, 2017, Ma, Xiaodong; Ge, Yang; Song, Zhendong; Huang, Shanshan; Wang, Changyuan; Zhang, Jianbin; Tang, Zeyao; Liu, Kexin published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was Phosphoryl pyrimidine compound, and its composition and application. And the patent contained the following:

The title phosphoryl pyrimidine compound is shown in formula I, wherein, X is Cl or F; L is -CH2- or -O(CH2)2CH2-; R1 is selected from H, Me, methoxy, and Cl; R2 is selected from methoxy, ethoxy, etc.; R3 is methoxy, ethoxy, etc. The phosphoryl pyrimidine compound is capable of inhibiting Brutons tyrosine kinase, so as to treat tumor diseases, such as Burkitts lymphoma, diffuse large B cell lymphoma, follicular lymphoma, and chronic lymphocytic leukemia. 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 phosphoryl pyrimidine compound preparation antitumor activity, Organometallic and Organometalloidal Compounds: Phosphorus Compounds and other aspects.Application In Synthesis of N-(3-Aminophenyl)acrylamide

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

On March 2, 2018, Vallejos Calzada, Saul; Garcia Garcia, Felix Clemente; Serna Arenas, Felipe; Camara Nebreda, Jose Maria; Represa Perez, Cesar; Bertolin Burillo, Juan Carlos; Garcia Perez, Jose Miguel; Pascual Portal, Blanca Sol; Trigo Lopez, Miriam published a patent.Recommanded Product: N-(3-Aminophenyl)acrylamide The title of the patent was Conductive polymers based on polyaniline sequences and procedure for obtaining them. And the patent contained the following:

The invention relates to solid elec. conductive polymeric materials prepared by growing polyaniline side chains from non-conducting polymers with aminophenyl side groups in their structure, preferably in form of films or coatings, as well as the procedure for obtaining them and their use in the elaboration of sensors with resistive or conductive substances for substances of interest, both in the gas phase and in the dissolution, or for use in elec. and electronic systems. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Recommanded Product: N-(3-Aminophenyl)acrylamide

The Article related to conductive polymer polyaniline, Chemistry of Synthetic High Polymers: Chemical Transformation Of Polymers and other aspects.Recommanded Product: N-(3-Aminophenyl)acrylamide

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

On August 14, 2014, Haq, Nadia; Niu, Deqiang; Petter, Russell C.; Qiao, Lixin; Singh, Juswinder; Zhu, Zhendong published a patent.Quality Control of N-(3-Aminophenyl)acrylamide The title of the patent was Pyrimidine derivatives as ERK inhibitors and their preparation. And the patent contained the following:

The invention provides compounds of formula I, compositions thereof, and methods of using the same. Compounds of formula I wherein A is (un)substituted Ph, 3- to 8-membered (un)saturated monocyclic ring, 4- to 7-membered monocyclic heterocyclic ring, etc.; B is (un)substituted Ph, (un)substituted (un)saturated 3- to 7-membered carbocyclic ring, 5- to 6-membered monocyclic heteroaryl, absent, etc.; m and p are independently 0 – 4; R1 is a warhead group, wherein R1 is attached to an atom adjacent to where W is attached; each R2 is H, (un)substituted C1-6 aliphatic, halo and OH and derivatives; each R3 is H, halo, OH and derivatives, SH and derivatives, CN, etc.; R4 is H, (un)substituted C1-6 aliphatic, halo, haloalkyl, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their ERK inhibitor activity (some data given). The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Quality Control of N-(3-Aminophenyl)acrylamide

The Article related to pyrimidine preparation erk inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of N-(3-Aminophenyl)acrylamide

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

On May 17, 2018, Na, Yun Soo; Bang, Keuk Chan; Park, Joon Seok published a patent.Product Details of 16230-24-3 The title of the patent was Preparation of novel pyrrolopyrimidine derivatives as BTK inhibitors and pharmaceutical composition comprising the same. And the patent contained the following:

The invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, and the compound according to the invention can be usefully used for the prevention or treatment of diseases in which the BTK inhibitory action is beneficial. Compounds of formula I wherein X is NH and O; L is a bod and CO; R is H, (un)substituted C6-10 aryl and (un)substituted C3-10 heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their BTK inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 20.9 n< and 100 % inhibition at 1 μM. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Product Details of 16230-24-3

The Article related to pyrrolopyrimidine preparation btk inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 16230-24-3

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

On May 16, 2018, Na, Yun Su; Bang, Geuk Chan; Park, Jun Seok published a patent.Related Products of 16230-24-3 The title of the patent was Preparation of novel pyrrolopyrimidine derivatives as BTK inhibitors and pharmaceutical composition comprising the same. And the patent contained the following:

The invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, and the compound according to the invention can be usefully used for the prevention or treatment of diseases in which the BTK inhibitory action is beneficial. Compounds of formula I wherein X is NH and O; L is a bod and CO; R is H, (un)substituted C6-10 aryl and (un)substituted C3-10 heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their BTK inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 20.9 n< and 100 % inhibition at 1 μM. 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 pyrrolopyrimidine preparation btk inhibitor, 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