Luo, Guoli et al. published their research in RSC Advances in 2018 |CAS: 5301-96-2

The Article related to alkyltriazole preparation, triazole vinyl ether gold catalyst regioselective alkylation, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.Computed Properties of 5301-96-2

Luo, Guoli; Sun, Chenyang; Li, Yan; Li, Xiaoxiao; Zhao, Zhigang published an article in 2018, the title of the article was N2-selective alkylation of NH-1,2,3-triazoles with vinyl ethers via gold catalysis.Computed Properties of 5301-96-2 And the article contains the following content:

A new method was developed to synthesize N2-alkyl-substituted 1,2,3-triazoles via gold catalyzed alkylation of vinyl ethers with mono- and unsubstituted NH-1,2,3-triazoles and benzotriazole. A hydrogen bond between the oxygen atom of the vinyl ethers, activated via the gold catalyst, and the NH-1,2,3-triazoles was supposed to be generated, which selectively gave the N2-alkylation products. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).Computed Properties of 5301-96-2

The Article related to alkyltriazole preparation, triazole vinyl ether gold catalyst regioselective alkylation, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.Computed Properties of 5301-96-2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Boev, V. I. et al. published their research in Khimiya Geterotsiklicheskikh Soedinenii in 1980 |CAS: 5301-96-2

The Article related to ferrocenyl triazole, triazole ferrocenylsulfonyl, Organometallic and Organometalloidal Compounds: Iron Compounds and other aspects.Recommanded Product: 5301-96-2

On May 31, 1980, Boev, V. I.; Kushnir, V. N.; Shevchuk, M. I.; Dombrovskii, A. V. published an article.Recommanded Product: 5301-96-2 The title of the article was Synthesis and properties of 1,2,3-triazoles containing a ferrocenyl nucleus. And the article contained the following:

The title compounds I (R1 = H, Me, MeO, Cl, Br, NO2, R2 = H; R1 = H, R2 = Me; Fc = ferrocenyl) were prepared in 57-77% yields by cyclizing Ph3P:CR2COR1 with FcSO2N3. Treating I with EtOH gave 96-99% II. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).Recommanded Product: 5301-96-2

The Article related to ferrocenyl triazole, triazole ferrocenylsulfonyl, Organometallic and Organometalloidal Compounds: Iron Compounds and other aspects.Recommanded Product: 5301-96-2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Oh, Sangtae et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2010 |CAS: 5301-96-2

The Article related to triazole artemisinin preparation anticancer, Terpenes and Terpenoids: Sesquiterpenes (C15), Including Ionones and other aspects.HPLC of Formula: 5301-96-2

On July 15, 2010, Oh, Sangtae; Shin, Woon-Seob; Ham, Jungyeob; Lee, Seokjoon published an article.HPLC of Formula: 5301-96-2 The title of the article was Acid-catalyzed synthesis of 10-substituted triazolyl artemisinins and their growth inhibitory activity against various cancer cells. And the article contained the following:

A diastereomeric and regioisomeric library of 10-triazolylartemisinins with potent growth-inhibitory activities against various cancer cell lines was established. These compounds were synthesized by the reaction with dihydroartemisinin and various triazoles in CH2Cl2 using BF3.OEt2 catalyst. Most of the compounds exhibited a strong potency in the submicromolar range, and, in particular, 3 compounds, having a (pentylphenyl)triazole moiety, proved to be promising candidates for preclin. trials. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).HPLC of Formula: 5301-96-2

The Article related to triazole artemisinin preparation anticancer, Terpenes and Terpenoids: Sesquiterpenes (C15), Including Ionones and other aspects.HPLC of Formula: 5301-96-2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Lee, Seokjoon et al. published their research in Bulletin of the Korean Chemical Society in 2011 |CAS: 5301-96-2

The Article related to triazolylartemisinin preparation anticancer, artemisinin triazole preparation anticancer, Terpenes and Terpenoids: Sesquiterpenes (C15), Including Ionones and other aspects.Synthetic Route of 5301-96-2

On February 20, 2011, Lee, Seokjoon published an article.Synthetic Route of 5301-96-2 The title of the article was Synthesis of 10β-substituted triazolyl artemisinins and their growth inhibitory activity against various cancer cells. And the article contained the following:

A library of 10-triazolylartemisinins was established comprising compounds that strongly inhibit the growth of cancer cell lines, such as DLD-1, U-87, Hela, SiHa, A172, and Bi1. These compounds were synthesized by an acid-catalyzed reaction of dihydroartemisinin (I) with various triazoles in CH2Cl2 at room temperature In particular, when 3 equivalent of triazole were reacted with I, 10β-(4-substituted triazolyl)artemisinins were obtained, which means that the type of product obtained differs according to the quantity of triazole reactant employed in the synthesis. From the viewpoint of antiproliferative activity against the various cancer cells, compounds, which have a (pentylphenyl)triazole moiety, exhibited potent activity. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).Synthetic Route of 5301-96-2

The Article related to triazolylartemisinin preparation anticancer, artemisinin triazole preparation anticancer, Terpenes and Terpenoids: Sesquiterpenes (C15), Including Ionones and other aspects.Synthetic Route of 5301-96-2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Mitsiades, Constantine S. et al. published their patent in 2021 |CAS: 1949837-12-0

The Article related to e3 ubiquitin ligase degrader cancer therapy, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Formula: C49H60ClN9O7S2

On March 18, 2021, Mitsiades, Constantine S.; Shirasaki, Ryosuke; Matthews, Geoffrey M.; Gandolfi, Sara; De Matos Simoes, Ricardo published a patent.Formula: C49H60ClN9O7S2 The title of the patent was Methods for treating cancer using serial administration of E3 ubiquitin ligase degraders. And the patent contained the following:

The present invention relates, in part, to methods for treating cancer using serial administration of E3 ubiquitin ligase degraders. The experimental process involved the reaction of (2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide(cas: 1949837-12-0).Formula: C49H60ClN9O7S2

The Article related to e3 ubiquitin ligase degrader cancer therapy, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Formula: C49H60ClN9O7S2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Liu, Jing et al. published their research in Journal of the American Chemical Society in 2021 |CAS: 1949837-12-0

The Article related to preparation folate caged protac cancer toxicity, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 1949837-12-0

On May 19, 2021, Liu, Jing; Chen, He; Liu, Yi; Shen, Yudao; Meng, Fanye; Kaniskan, H. Umit; Jin, Jian; Wei, Wenyi published an article.Synthetic Route of 1949837-12-0 The title of the article was Cancer Selective Target Degradation by Folate-Caged PROTACs. And the article contained the following:

PROTACs (proteolysis targeting chimeras) are an emerging class of promising therapeutic modalities that degrade intracellular protein targets by hijacking the cellular ubiquitin-proteasome system. However, potential toxicity of PROTACs in normal cells due to the off-tissue on-target degradation effect limits their clin. applications. Precise control of a PROTAC’s on-target degradation activity in a tissue-selective manner could minimize potential toxicity/side-effects. To this end, we developed a cancer cell selective delivery strategy for PROTACs by conjugating a folate group to a ligand of the VHL E3 ubiquitin ligase, to achieve targeted degradation of proteins of interest (POIs) in cancer cells vs. noncancerous normal cells. We show that our folate-PROTACs, including BRD PROTAC (folate-ARV-771), MEK PROTAC (folate-MS432), and ALK PROTAC (folate-MS99), are capable of degrading BRDs, MEKs, and ALK, resp., in a folate receptor-dependent manner in cancer cells. This design provides a generalizable platform for PROTACs to achieve selective degradation of POIs in cancer cells. The experimental process involved the reaction of (2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide(cas: 1949837-12-0).Synthetic Route of 1949837-12-0

The Article related to preparation folate caged protac cancer toxicity, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 1949837-12-0

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Sun, B. et al. published their research in Leukemia in 2018 |CAS: 1949837-12-0

The Article related to mantle cell lymphoma antitumor bet protein proteolysis, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 1949837-12-0

On February 28, 2018, Sun, B.; Fiskus, W.; Qian, Y.; Rajapakshe, K.; Raina, K.; Coleman, K. G.; Crew, A. P.; Shen, A.; Saenz, D. T.; Mill, C. P.; Nowak, A. J.; Jain, N.; Zhang, L.; Wang, M.; Khoury, J. D.; Coarfa, C.; Crews, C. M.; Bhalla, K. N. published an article.Synthetic Route of 1949837-12-0 The title of the article was Bet protein proteolysis targeting chimera (protac) exerts potent lethal activity against mantle cell lymphoma cells. And the article contained the following:

Bromodomain extraterminal protein (BETP) inhibitors transcriptionally repress oncoproteins and nuclear factor-κB (NF-κB) target genes that undermines the growth and survival of mantle cell lymphoma (MCL) cells. However, BET bromodomain inhibitor (BETi) treatment causes accumulation of BETPs, associated with reversible binding and incomplete inhibition of BRD4 that potentially compromises the activity of BETi in MCL cells. Unlike BETi, BET-PROTACs (proteolysis-targeting chimera) ARV-825 and ARV-771 (Arvinas, Inc.) recruit and utilize an E3-ubiquitin ligase to effectively degrade BETPs in MCL cells. BET-PROTACs induce more apoptosis than BETi of MCL cells, including those resistant to ibrutinib. BET-PROTAC treatment induced more perturbations in the mRNA and protein expressions than BETi, with depletion of c-Myc, CDK4, cyclin D1 and the NF-κB transcriptional targets Bcl-xL, XIAP and BTK, while inducing the levels of HEXIM1, NOXA and CDKN1A/p21. Treatment with ARV-771, which possesses superior pharmacol. properties compared with ARV-825, inhibited the in vivo growth and induced greater survival improvement than the BETi OTX015 of immune-depleted mice engrafted with MCL cells. Cotreatment of ARV-771 with ibrutinib or the BCL2 antagonist venetoclax or CDK4/6 inhibitor palbociclib synergistically induced apoptosis of MCL cells. These studies highlight promising and superior preclin. activity of BET-PROTAC than BETi, requiring further in vivo evaluation of BET-PROTAC as a therapy for ibrutinib-sensitive or -resistant MCL. The experimental process involved the reaction of (2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide(cas: 1949837-12-0).Synthetic Route of 1949837-12-0

The Article related to mantle cell lymphoma antitumor bet protein proteolysis, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 1949837-12-0

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Bernstein, Bradley E. et al. published their patent in 2020 |CAS: 1949837-12-0

The Article related to antitumor screening therapeutic drug target cancer treatment, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.SDS of cas: 1949837-12-0

On February 13, 2020, Bernstein, Bradley E.; Doench, John G.; Najm, Fadi J. published a patent.SDS of cas: 1949837-12-0 The title of the patent was Methods of combinatorial drug screening and use of therapeutic targets thereof in cancer treatment. And the patent contained the following:

CRISPR-Cas9 has enabled a new generation of screening strategies to interrogate gene function. However, redundant genes and the complexity of functional gene networks can confound single gene knockout approaches. Furthermore, simple addition of two or more sgRNAs has shown only modest targeting efficacy in screening approaches. The present invention relates to combined orthogonal CRISPR-derived components to maximize gene targeting activity with minimal cross-talk and interference. The present invention also relates to efficient S. aureus Cas9 sgRNA design rules, which were paired with S. pyogenes Cas9 sgRNA design rules to achieve dual target gene inactivation in a high fraction of cells. Applicants developed a lentiviral vector and cloning strategy to generate high complexity pooled dual-knockout libraries and show that screening these libraries can identify combinatorial phenotypes, including synthetic lethal gene pairs across multiple cell types. The gene pairs can be targeted therapeutically and applicants disclose therapeutically effective combination therapies using agents such as AZD5153, CPI-203, OTX015, JQ1. The experimental process involved the reaction of (2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide(cas: 1949837-12-0).SDS of cas: 1949837-12-0

The Article related to antitumor screening therapeutic drug target cancer treatment, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.SDS of cas: 1949837-12-0

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Wang, Shihui et al. published their research in Chemical Research in Chinese Universities in 2018 |CAS: 1949837-12-0

The Article related to leukemia cell brd4 protein degradation proteolysis targeting chimera, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Recommanded Product: 1949837-12-0

On April 30, 2018, Wang, Shihui; Li, Haiyan; Wang, Yue; Gao, Yang; Yu, Shanshan; Zhao, Qianqian; Jin, Xiangqun; Lu, Haibin published an article.Recommanded Product: 1949837-12-0 The title of the article was Design and synthesis of proteolysis targeting chimeras for inducing brd4 protein degradation. And the article contained the following:

In this paper, we synthesized a series of proteolysis targeting chimeras(PROTACs) using VHL E3 ligase ligands for BRD4 protein degradation One of the most promising compound 19g exhibited robust potency of BRD4 inhibition with IC50 value of (18.6±1.3) nmol/L, resp. Furthermore, compound 19g potently inhibited cell proliferation in BRD4-sensitive cell lines RS4;11 with IC50 value of (34.2±4.3) nmol/L and capable of inducing de-gradation of BRD4 protein at 0.4-0.6μmol/L in the RS4;11 leukemia cells. These data show that compound 19g is a highly potent and efficacious BRD4 degrader. The experimental process involved the reaction of (2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide(cas: 1949837-12-0).Recommanded Product: 1949837-12-0

The Article related to leukemia cell brd4 protein degradation proteolysis targeting chimera, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Recommanded Product: 1949837-12-0

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Raina, Kanak et al. published their research in Proceedings of the National Academy of Sciences of the United States of America in 2016 |CAS: 1949837-12-0

The Article related to bromodomain extra terminal protein, bet, brd4, protac, prostate, protein degradation, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application of 1949837-12-0

On June 28, 2016, Raina, Kanak; Lu, Jing; Qian, Yimin; Altieri, Martha; Gordon, Deborah; Rossi, Ann Marie K.; Wang, Jing; Chen, Xin; Dong, Hanqing; Siu, Kam; Winkler, James D.; Crew, Andrew P.; Crews, Craig M.; Coleman, Kevin G. published an article.Application of 1949837-12-0 The title of the article was PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. And the article contained the following:

Prostate cancer has the second highest incidence among cancers in men worldwide and is the second leading cause of cancer deaths of men in the United States. Although androgen deprivation can initially lead to remission, the disease often progresses to castration-resistant prostate cancer (CRPC), which is still reliant on androgen receptor (AR) signaling and is associated with a poor prognosis. Some success against CRPC has been achieved by drugs that target AR signaling, but secondary resistance invariably emerges, and new therapies are urgently needed. Recently, inhibitors of bromodomain and extra-terminal (BET) family proteins have shown growth-inhibitory activity in preclin. models of CRPC. Here, we demonstrate that ARV-771, a small-mol. pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technol., demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. Unlike BET inhibitors, ARV-771 results in suppression of both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model. This study is, to our knowledge, the first to demonstrate efficacy with a small-mol. BET degrader in a solid-tumor malignancy and potentially represents an important therapeutic advance in the treatment of CRPC. The experimental process involved the reaction of (2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide(cas: 1949837-12-0).Application of 1949837-12-0

The Article related to bromodomain extra terminal protein, bet, brd4, protac, prostate, protein degradation, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application of 1949837-12-0

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics