Month: November 2022

On July 31, 2019, Liu, Renshuai; Liu, Lulu; Yang, Xinying; Fang, Hao published an article.Recommanded Product: 97-09-6 The title of the article was Discovery and development of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as Bcl-2/Mcl-1 inhibitors. And the article contained the following:

Bcl-2 family proteins play a vital role for cancer cell in escaping apoptosis, and small-mol. anti-apoptotic Bcl-2 protein inhibitors have been developed as new anticancer therapies. In current study, a series of substituted 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were developed based on the lead compound 1 (Ki = 5.2 μM against Bcl-2 protein). The fluorescence polarization assays suggested that active compounds possessed potent binding affinities to both Bcl-2 and Mcl-1 protein, but had minor or no binding affinities to Bcl-XL protein. MTT assays showed that these compounds had certain anti-proliferative activities against cancer cells. Furthermore, it was found that active compound 11t(I) could induce cell apoptosis and caspase-3 activation in a dose-dependent manner in Jurkat cells. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Recommanded Product: 97-09-6

The Article related to neoplasm antitumor bcl2 mcl1, 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, anti-tumor, apoptosis, bcl-2, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 97-09-6

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

On January 1, 2017, Wan, Yichao; Liu, Tingting; Li, Xiaoxian; Chen, Chen; Fang, Hao published an article.Category: amides-buliding-blocks The title of the article was Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains. And the article contained the following:

As an important member of anti-apoptotic Bcl-2 protein, myeloid cell leukemia sequence 1 (Mcl-1) protein is an attractive target for cancer therapy. In this study, a new series of pyrrolidine derivatives as Mcl-1 inhibitors were developed by mainly modifying the amino acid side chain of compound 1. Among them, compound 18 (Ki = 0.077 μM) exhibited better potent inhibitory activities towards Mcl-1 protein compared to pos. control Gossypol (Ki = 0.18 μM). In addition, compound 40 possessed good antiproliferative activities against PC-3 cells (Ki = 8.45 μM), which was the same as pos. control Gossypol (Ki = 7.54 μM). The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Category: amides-buliding-blocks

The Article related to pyrrolidine derivative preparation sar mcl1 inhibitor bcl2 apoptosis cancer, bcl-2, cancer, mcl-1, pyrrolidine, target, Pharmacology: Structure-Activity and other aspects.Category: amides-buliding-blocks

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

On October 15, 2017, Xu, Guangsen; Liu, Tingting; Zhou, Yi; Yang, Xinying; Fang, Hao published an article.Product Details of 97-09-6 The title of the article was 1-Phenyl-1H-indole derivatives as a new class of Bcl-2/Mcl-1 dual inhibitors: Design, synthesis, and preliminary biological evaluation. And the article contained the following:

Bcl-2 proteins, such as B-cell lymphoma (Bcl-2) protein, myeloid cell leukemia sequence 1 (Mcl-1) protein, has been implicated in the progression and survival of multiple tumor types and become a validated and attractive target for cancer therapy. In this work, a series of 1-phenyl-1H-indole derivatives has been designed and synthesized. The preliminary biol. studies (binding assay for Bcl-2 proteins and MTT assay) suggested that some active compounds showed potent inhibitory activities on Bcl-2/Mcl-1 without binding on Bcl-XL. Furthermore, Compound I and II showed better anti-proliferative activity than WL-276. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Product Details of 97-09-6

The Article related to phenylindole synthesis antitumor bcl2 mcl1, 1-phenyl-1h-indole derivatives, anti-tumor, apoptosis, bcl-2/mcl-1 dual inhibition, Pharmacology: Structure-Activity and other aspects.Product Details of 97-09-6

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

On December 1, 2015, Wang, Gang; Wang, Yutao; Wang, Lei; Han, Leiqiang; Hou, Xuben; Fu, Huansheng; Fang, Hao published an article.Product Details of 97-09-6 The title of the article was Design, synthesis and preliminary bioactivity studies of imidazolidine-2,4-dione derivatives as Bcl-2 inhibitors. And the article contained the following:

Anti-apoptotic B-cell lymphoma-2 (Bcl-2) proteins are promising targets for cancer therapy. In the present study, a series of imidazolidine-2,4-dione derivatives were designed and synthesized to test their inhibitory activities against anti-apoptotic Bcl-2 proteins. Among them, compound 8k had better growth inhibitory effects on K562 and PC-3 cell lines compared to lead compound WL-276. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Product Details of 97-09-6

The Article related to imidazolidine dione derivative preparation bcl2 inhibitor antitumor leukemia, antitumor, bcl-2, imidazolidine-2,4-dione, inhibitors, Pharmacology: Structure-Activity and other aspects.Product Details of 97-09-6

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

Ma, Min; Jiang, Xingjun; Wang, Xueding; Zou, Hao; Yang, Weiqing; Zhang, Yuanyuan; Peng, Changrong; Li, Zicheng; Yang, Jing; Du, Quan; Ma, Menglin published an article in 2016, the title of the article was Synthesis and Quantitative Structure-activity Relationships Study for Arylpropenamide Derivatives as Inhibitors of Hepatitis B Virus Replication.Name: 2-(4-Methylbenzamido)acetic acid And the article contains the following content:

A series of new arylpropenamide derivatives containing different aryl groups were synthesized, characterized, and evaluated for their anti-hepatitis B virus (HBV) activities. A new high accuracy QSAR model of arylpropenamide was constructed based on a more completely activities data and calculation parameter. The 2D-QSAR equations, by using DFT and multiple linear regression anal. methods, revealed that higher value of thermal energy (TE) and lower entropy Sn.1257 increase the anti-HBV activities of the arylpropenamide mols. Predictive 3D-QSAR models were established by SYBYL multifit mol. alignment rule. The optimum models were all statistically significant with cross-validated and conventional coefficients, indicating that they were reliable enough for activity prediction. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Name: 2-(4-Methylbenzamido)acetic acid

The Article related to aryl propenamide derivative preparation structure antiviral hepatitis b, 2d-qsar, 3d-qsar, sybyl, arylpropenamide, hepatitis b virus, Pharmacology: Structure-Activity and other aspects.Name: 2-(4-Methylbenzamido)acetic acid

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

Pawar, Rahul S.; Grundel, Erich published an article in 2017, the title of the article was Overview of regulation of dietary supplements in the USA and issues of adulteration with phenethylamines (PEAs).Related Products of 456-12-2 And the article contains the following content:

A review. The multi-billion dollar dietary supplement industry is global in reach. The industry has been criticized for problems related to poor quality control, safety, misbranding, and adulteration. In this review, we describe how the US Food and Drug Administration (FDA) regulates dietary supplements within the framework of the Federal Food, Drug, and Cosmetic Act (FD&C Act). The Dietary Supplement Health and Education Act of 1994 (DSHEA), which amended the FD&C Act, gave the FDA the authority to promulgate Good Manufacturing Practices for dietary supplements and required that manufacturers provide the FDA information supporting a conclusion that the ingredients are reasonably expected to be safe if the dietary ingredients were not marketed in the USA before 15 Oct. 1994. Recent amendments to the FD&C Act require that serious dietary-supplement-related adverse events be reported to the FDA and provide the agency with mandatory recall authority. We discuss the presence of naturally occurring (e.g. Ephedra, Citrus aurantium, Acacia) and synthetic (e.g. β-methylphenethylamines, methylsynephrine, α-ethyl-phenethylamine) biol. active phenethylamines (PEAs) in dietary supplements and of PEA drugs (e.g. clenbuterol, fenfluramine, sibutramine, lorcaserin) in weight-loss products. Regulatory actions against manufacturers of products labeled as dietary supplements that contain the aliphatic amines 1,3-dimethylamine and 1,3-dimethylbutylamine, and PEAs such as β-methylphenethylamine, aegeline, and Dendrobium illustrate the FDA’s use of its authority under the FD&C Act to promote dietary supplement safety. Published 2016. This article is a U. S. Government work and is in the public domain in the USA. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Related Products of 456-12-2

The Article related to phenethylamine dietary supplement regulation review, dshea, adulteration, dietary supplements, new dietary ingredient, phenethylamine, Food and Feed Chemistry: Reviews and other aspects.Related Products of 456-12-2

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

On March 31, 1985, De Benedetti, Pier G.; Menziani, M. Cristina; Frassineti, Chiara published an article.Reference of 3-Nitro-4-chlorobenzenesulfonamide The title of the article was A quantum chemical QSAR study of carbonic anhydrase inhibition by sulfonamides. Sulfonamide carbonic anhydrase inhibitors: quantum chemical QSAR. And the article contained the following:

MO indexes were computed (CNDO/2) for 3 series of sulfonamide inhibitors, (in their neutral and anionic forms) of carbonic anhydrase  [9001-03-0]. Linear regression analyses between the calculated indexes and both physico-chem. and enzyme inhibition data gave good correlations which allowed the testing of predictive and diagnostic aspects of the quant. structure-activity relationships employing quantum chem. indexes. Results indicated that the mol. size affects the inhibitory power among the different sulfonamide derivatives (aliphatic, arylic and bridged diarylic) but not significantly within each mol. series. Results indicated further that the MO indexes are good predictors of the various exptl. mol. properties and suggest that the less electron-rich the sulfamoyl group is, the more favored are both the hydrophobic and hydrophilic steps leading to enzyme inhibition. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Reference of 3-Nitro-4-chlorobenzenesulfonamide

The Article related to carbonic anhydrase inhibition sulfonamide qsar, qsar sulfonamide derivative, structure activity sulfonamide derivative, mo sulfonamide, Pharmacology: Structure-Activity and other aspects.Reference of 3-Nitro-4-chlorobenzenesulfonamide

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

On March 15, 2017, Liu, Tingting; Wan, Yichao; Liu, Renshuai; Ma, Lin; Li, Minyong; Fang, Hao published an article.COA of Formula: C6H5ClN2O4S The title of the article was Design, synthesis and preliminary biological evaluation of indole-3-carboxylic acid-based skeleton of Bcl-2/Mcl-1 dual inhibitors. And the article contained the following:

The B-cell lymphoma-2 (Bcl-2) family proteins are attractive targets for cancer therapy. In the previous work, the structure-activity relationship of WL-276 was studied. According to the results, rhodanine derivatives show potent binding affinity for Bcl-2 and Mcl-1 protein and show weaker activity against Bcl-XL protein. Based on the previous results, a new class of indole-3-carboxylic acid-based derivatives were designed and synthesized as Bcl-2/Mcl-1 dual inhibitors. Among them, compound I has a Ki value of 0.26 μM for Bcl-2 protein and is better than WL-276. Furthermore, it inhibits the myeloid cell leukemia sequence 1 (Mcl-1) protein with a Ki value of 72 nM. Especially, compound II can selectively acting on Bcl-2 and Mcl-1 protein but not Bcl-XL protein, which has great significance for developing dual inhibitors targeting Bcl-2 and Mcl-1 protein, as well as specific antitumor abilities in cells. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).COA of Formula: C6H5ClN2O4S

The Article related to indolecarboxylate bcl2 mcl1 inhibitor antitumor neoplasm, anti-tumor, bcl-2/mcl-1, indole-3-carboxylic acid-based derivatives, inhibitors, Pharmacology: Structure-Activity and other aspects.COA of Formula: C6H5ClN2O4S

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 January 31, 2020, Alkahtani, Hamad M.; Abdalla, Ashraf N.; Obaidullah, Ahmad J.; Alanazi, Mohammed M.; Almehizia, Abdulrahman A.; Alanazi, Mashael G.; Ahmed, Ahmed Y.; Alwassil, Osama I.; Darwish, Hany W.; Abdel-Aziz, Alaa A.-M.; El-Azab, Adel S. published an article.COA of Formula: C2H4ClNO The title of the article was Synthesis, cytotoxic evaluation, and molecular docking studies of novel quinazoline derivatives with benzenesulfonamide and anilide tails: Dual inhibitors of EGFR/HER2. And the article contained the following:

We synthesized a new series of 2-[(3-(4-sulfamoylphenethyl)-4(3H)-quinazolinon-2-yl)thio]anilide derivatives (2-16) and evaluated their cytotoxic activity against breast adenocarcinoma (MCF-7), colorectal adenocarcinoma (HT-29), and acute myeloid leukemia (HL-60 and K562) cells. To reveal their selectivity toward cancer cells, the compounds were also tested against the human fibroblast cell line, MRC-5. Compounds 1-5 exhibited potent cytotoxic activity against the tested cell lines with IC50 values of 0.65-3.86, 0.68-4.60, 0.41-1.45, 0.42-4.07, and 3.77-25.55μM, resp. compared to sorafenib, the standard drug (IC50 2.50, 2.50, and 3.14μM against MCF-7, HT-29, and HL60 cells, resp.). Interestingly, compounds 1-5 displayed selectivity toward the cancer cell lines over MRC-5 (IC50 3.77-25.55μM). These compounds also displayed potent inhibitory activity against EGFR and HER2 kinases (IC50 0.09-0.43 and 0.15-0.33μM, resp.) compared to the standard drug, sorafenib (IC50 0.11 and 0.13μM, resp.). Likewise, compounds 1, 4, and 5 showed strong inhibitory activity against VEGFR2 (IC50 0.34, 0.28 and 0.39μM, resp.) compared to sorafenib (IC50 0.17μM). We also employed mol. docking to identify the structural features required for the EGFR/HER2 inhibitory activity of the new series. Ultimately, compounds 1, 4, and 5 were demonstrated to be candidates for further preclin. investigations. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).COA of Formula: C2H4ClNO

The Article related to preparation quinazoline benzenesulfonamide anilide derivative egfr her2 inhibitor cancer, anticancer, egfr, her2, molecular docking, quinazolin-4-ones, Pharmacology: Structure-Activity and other aspects.COA of Formula: C2H4ClNO

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