Category: 16230-24-3

On August 5, 2022, Li, Qinlan; Guo, Qian; Wang, Shuyi; Wan, Shanhe; Li, Zhonghuang; Zhang, Jiajie; Wu, Xiaoyun published an article.Application of 16230-24-3 The title of the article was Design and synthesis of proteolysis targeting chimeras (PROTACs) as an EGFR degrader based on CO-1686. And the article contained the following:

Epidermal growth factor receptor (EGFR) inhibitors represent the first-line treatment of non-small-cell lung cancer (NSCLC). However, the emergence of acquired drug resistance and side effects largely encumbered their application in clinic. The emerging technol. proteolysis targeting chimera (PROTAC) could be an alternative strategy to overcome these problems. Herein, we reported the discovery of EGFRL858R/T790M degraders based on CO-1686. Promising PROTAC 1q could effectively and selectively inhibit the growth of PC-9 (EGFRDel 19) and H1975 (EGFRL858R/T790M) cells, but not that of A549 (EGFRWT) cells. In addition, 1q could time- and dose-dependently induce degradation of EGFRL858R/T790M in H1975 cells with a DC50 value of 355.9 nM, while did not show obvious effect on the EGFRDel 19 and EGFRWT protein. Preliminary mechanism study demonstrated that the protein degradation was mediated through ubiquitin-proteasome system (UPS). Furthermore, 1q could significantly induce the apoptosis of H1975 cells and arrest the cells in G0/G1 phase. These findings demonstrated that compound 1q could be used as initial lead compound for the development of new EGFRL858R/T790M degraders based therapy. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to human lung adenocarcinoma nsclc apoptosis protac egfr degrader co1686, co-1686, degrader, egfr, protac, Placeholder for records without volume info and other aspects.Application of 16230-24-3

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

On April 30, 2018, Liu, Zhuo; Wang, Luhong; Feng, Min; Yi, Yuanyuan; Zhang, Wenhan; Liu, Wenjuan; Li, Lei; Liu, Zhihao; Li, Yanxia; Ma, Xiaodong published an article.HPLC of Formula: 16230-24-3 The title of the article was New acrylamide-substituted quinazoline derivatives with enhanced potency for the treatment of EGFR T790M-mutant non-small-cell lung cancers. And the article contained the following:

A new class of acrylamide-substituted quinazoline derivatives with enhanced inhibitory activity against mutant EGFR T790M enzyme were synthesized. Among them, compound 10b displayed the strongest inhibitory potency to block the phosphorylation of the EGFR T790M enzyme, with an IC50 value of 4.3 nM. Compared with the lead compound gefitinib, compound 10b significantly strengthened the activity against EGFR T790M (194 times higher). Furthermore, compound 10b only exhibited moderate activity against wild type EGFR, with an IC50 of 105.0 nM, suggesting its improved selectivity over the T790M-mutated EGFR. In addition, compound 10b also showed stronger activity against H1975 cells harboring the EGFR T790M mutation than gefitinib. Moreover, compound 10b has low inhibitory activity toward the normal HBE cells (IC50 > 34.04 μM), indicating its low cell cytotoxicity. Overall, this modification provided a new insight to design covalent binding EGFRT790M inhibitors to prevent 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 acrylamide quinazoline synthesis anticancer egfr lung breast cancer, Pharmacology: Structure-Activity and other aspects.HPLC of Formula: 16230-24-3

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

On January 1, 2018, Ge, Yang; Wang, Changyuan; Song, Shijie; Huang, Jiaxin; Liu, Zhihao; Li, Yongming; Meng, Qiang; Zhang, Jianbin; Yao, Jihong; Liu, Kexin; Ma, Xiaodong; Sun, Xiuli published an article.Application of 16230-24-3 The title of the article was Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. And the article contained the following:

The BTK and JAK3 receptor tyrosine kinases are two validated and therapeutically amenable targets in the treatment of B-cell lymphomas. Here the authors report the identification of several classes of pyrimidine derivatives as potent BTK and JAK3 dual inhibitors. Among these mols., approx. two thirds displayed strong inhibitory capacity at less than 10 nM concentration, and four compounds could significantly inhibit the phosphorylation of BTK and JAK3 enzymes at concentrations lower than 1 nM. Addnl., these pyrimidine derivatives also exhibited enhanced activity to block the proliferation of B-cell lymphoma cells compared with the representative BTK inhibitor ibrutinib. In particular, two structure-specific compounds I and II displayed stronger activity than reference agents in cell-based evaluation, with IC50 values lower than 10 μM. Further biol. studies, including flow cytometric anal., and a xenograft model for in vivo evaluation, also indicated their efficacy and low toxicity in the treatment of B-cell lymphoma. These findings provide a new insight for the development of novel anti-B-cell lymphoma drugs with multitarget actions. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to btk jak3 inhibitor antitumor neoplasm, btk, inhibitor, jak3, lymphoma, pyrimidine, Pharmacology: Structure-Activity and other aspects.Application of 16230-24-3

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

On November 1, 2016, Song, Zhendong; Jin, Yue; Ge, Yang; Wang, Changyuan; Zhang, Jianbin; Tang, Zeyao; Peng, Jinyong; Liu, Kexin; Li, Yanxia; Ma, Xiaodong published an article.Safety of N-(3-Aminophenyl)acrylamide The title of the article was Synthesis and biological evaluation of azole-diphenylpyrimidine derivatives (AzDPPYs) as potent T790M mutant form of epidermal growth factor receptor inhibitors. And the article contained the following:

A series of novel azole-diphenylpyrimidine derivatives (AzDPPYs) were synthesized and biol. evaluated as potent EGFRT790M inhibitors. Among these analogs, the most active inhibitor 6e not only displayed high activity against EGFRT790M/L858R kinase (IC50 = 3.3 nM), but also was able to repress the replication of H1975 cells harboring EGFRT790M mutation at a concentration of 0.118 μmol/L. In contrast to the lead compound rociletinib, 6e slightly reduces the key EGFRT790M-induced drug resistance. Significantly, inhibitor 6e demonstrates high selectivity (SI = 299.3) for T790M-containing EGFR mutants over wild type EGFR, hinting that it will cause less side effects. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Safety of N-(3-Aminophenyl)acrylamide

The Article related to azole diphenyl pyrimidine derivative preparation egfr inhibitor cancer, azole-diphenylpyrimidine, egfr t790m, inhibitors, nsclc, synthesis, Pharmacology: Structure-Activity and other aspects.Safety of N-(3-Aminophenyl)acrylamide

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

On November 1, 2021, Liu, Limin; Wang, Zhengjie; Gao, Chao; Dai, Honglin; Si, Xiaojie; Zhang, Yang; Meng, Yaqi; Zheng, Jiaxin; Ke, Yu; Liu, Hongmin; Zhang, Qiurong published an article.Reference of N-(3-Aminophenyl)acrylamide The title of the article was Design, synthesis and antitumor activity evaluation of trifluoromethyl-substituted pyrimidine derivatives. And the article contained the following:

In order to find efficient new antitumor drugs, a series of novel trifluoromethyl-substituted pyrimidine derivatives were designed and synthesized and the bioactivity against four human tumor cells (PC-3, MGC-803, MCF-7 and H1975) was evaluated by MTT assay. Compound I displayed potent anti-proliferative activity on H1975 (IC50 = 2.27 渭M), which was better than the pos. control 5-FU (IC50 = 9.37 渭M). Further biol. evaluation studies showed that compound I apoptosis of H1975 cells and arrested the cell cycle at G2/M phase. Furthermore, compound I induced H1975 cells apoptosis through increasing the expression of pro-apoptotic proteins Bax and p53 and down-regulating the anti-apoptotic protein Bcl-2. In addition, compound I was able to be tightly embedded in the active pocket of EGFR. These results demonstrated that compound I has a potential as a lead compound for further investigation. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Reference of N-(3-Aminophenyl)acrylamide

The Article related to trifluoromethyl benzyl thio pyrimidin preparation sar antitumor mol docking, antitumor activity, pyrimidine derivatives, synthesis, trifluoromethyl moiety, Placeholder for records without volume info and other aspects.Reference of N-(3-Aminophenyl)acrylamide

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

On January 31, 2013, Sano, Satoshi; Ishino, Tomonori; Nagata, Ichiro; Shiratsuchi, Kentaro; Itou, Shigehide; Ishizuka, Kenichi; Umehara, Takeshi published a patent.Safety of N-(3-Aminophenyl)acrylamide The title of the patent was Composite membranes for separating gases, gas separation module using same, gas separation devices and gas separation method. And the patent contained the following:

Provided is a composite membrane for separating gases having a gas separation layer, which contains a crosslinked polyimide resin, on a gas permeable support layer side, wherein the crosslinked polyimide resin has a structure in which a polyimide compound is crosslinked via a specific crosslinking chain, and the specific crosslinking chain has at least one type of linking group selected from a group comprising -NRaC(:O)-, -NRbC(:O)O-, -CH2OCH2-, -CH2SCH2-, -OC(:O)O-, -C(:O)O-N+(Rc)3-, -SO3-N+(Rd)3-, and -PO3-N+(Re)3-, wherein Ra, Rb, Rc, Rd and Re = hydrogen atom or a substituent. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Safety of N-(3-Aminophenyl)acrylamide

The Article related to composite membrane gas separator crosslinked polyimide, Plastics Fabrication and Uses: Plastic Product Uses and other aspects.Safety of N-(3-Aminophenyl)acrylamide

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

On January 31, 2013, Sano, Satoshi; Ishino, Tomonori; Nagata, Ichiro; Shiratsuchi, Kentaro; Itou, Shigehide; Ishizuka, Kenichi; Umehara, Takeshi published a patent.Safety of N-(3-Aminophenyl)acrylamide The title of the patent was Composite membranes for separating gases, gas separation module using same, gas separation devices and gas separation method. And the patent contained the following:

Provided is a composite membrane for separating gases having a gas separation layer, which contains a crosslinked polyimide resin, on a gas permeable support layer side, wherein the crosslinked polyimide resin has a structure in which a polyimide compound is crosslinked via a specific crosslinking chain, and the specific crosslinking chain has at least one type of linking group selected from a group comprising -NRaC(:O)-, -NRbC(:O)O-, -CH2OCH2-, -CH2SCH2-, -OC(:O)O-, -C(:O)O-N+(Rc)3-, -SO3-N+(Rd)3-, and -PO3-N+(Re)3-, wherein Ra, Rb, Rc, Rd and Re = hydrogen atom or a substituent. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Safety of N-(3-Aminophenyl)acrylamide

The Article related to composite membrane gas separator crosslinked polyimide, Plastics Fabrication and Uses: Plastic Product Uses and other aspects.Safety of N-(3-Aminophenyl)acrylamide

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

On July 31, 2018, Zhang, Yinsheng; Gao, Yong; Ren, Jing; Wang, Qinglin; Zhao, Damin; Zhou, Yu; Wu, Zheyang published a patent.Synthetic Route of 16230-24-3 The title of the patent was Preparation of boron-containing compounds as tyrosine kinase inhibitors. And the patent contained the following:

The title compounds I [wherein R1 is H, F, Cl, Br, alkyl, etc.; X is NH or O; R4 and R6 are independently H, alkyl, alkoxy, etc.; R3 and R7 are independently H and alkoxy; R5 is H, alkylamino, alkyl, cycloalkyl, etc.; Cy is (un)substituted Ph] were claimed and prepared The inventive compound has good inhibitory action on tyrosine kinase, and can be applied in treating the proliferative diseases caused by tyrosine kinase. 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 preparation boron tyrosine kinase inhibitor treatment proliferative disease, Organometallic and Organometalloidal Compounds: Boron Compounds and other aspects.Synthetic Route of 16230-24-3

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

On July 25, 2013, Popovici-Muller, Janeta; Saunders, Jeffrey O.; Salituro, Francesco G.; Cai, Zhenwei; Yan, Shunqi; Zhou, Ding published a patent.HPLC of Formula: 16230-24-3 The title of the patent was Preparation of heterocycles as isocitrate dehydrogenase 1 inhibitors, therapeutically active compositions and their methods of use. And the patent contained the following:

Provided are compounds of formula I as IDH1 inhibitors; their preparation and use of those compounds for treating cancer. Compounds of formula I wherein R1 is (un)substituted C4-6 carbocyclyl; R2 and R3 are independently (un)substituted aryl and (un)substituted heteroaryl; R4 is (un)substituted saturated heterocyclyl, heteroaralkyl, CH2-heterocyclyl, etc.; and pharmaceutically acceptable salts and hydrates thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their IDH1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of ≤ 0.1 μM. 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 heterocycle preparation idh1 inhibitor treatment cancer, Heterocyclic Compounds (One Hetero Atom): Other 5-Membered Rings and other aspects.HPLC of Formula: 16230-24-3

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

On August 7, 2018, Wang, Changyuan; Li, Si; Meng, Qiang; Sun, Xiuli; Li, Hua; Shu, Xiaohong; Sun, Huijun; Liu, Kexin; Liu, Zhihao; Ma, Xiaodong published an article.Electric Literature of 16230-24-3 The title of the article was Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. And the article contained the following:

A new family of diphenylpyrimidine derivatives bearing an amino acid substituent were identified as potent BTK inhibitors. Among them, compound 7b (N-[3-[[5-chloro-2-[4-[2-[2-(methoxycarbonyl)-1-pyrrolidinyl]-2-oxoethoxy]phenylamino]-4-pyrimidinyl]amino]phenyl]-2-acrylamide), which features an L-proline substituent, was identified as the strongest BTK inhibitor, with an IC50 of 8.7 nM. Compound 7b also displayed similar activity against B-cell lymphoma cell lines as ibrutinib. Moreover, 7b exhibited low cytotoxic activity against normal PBMC cells. In addition, the acridine orange/ethidium bromide (AO/EB) staining assay, Western blot anal. and flow cytometry anal. also showed its effectiveness in interfering with B-cell lymphoma cell growth. The mol. simulation performance showed that 7b forms addnl. strong hydrogen bonds with the BTK protein. All these findings provided new clues about the pyrimidine scaffold as an effective BTK inhibitor for the treatment of B-cell lymphoma. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Electric Literature of 16230-24-3

The Article related to diphenylpyrimidine derivative preparation antitumor btk inhibitor b cell lymphoma, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Electric Literature of 16230-24-3

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