Tag: 100-200

On March 29, 2012, Bartolozzi, Alessandra; Bosanac, Todd; Chen, Zhidong; De Lombaert, Stephane; Huber, John D.; Liu, Weimin; Lo, Ho Yin; Loke, Pui Leng; Riether, Doris; Tye, Heather; Wu, Lifen; Zindell, Renee M. published a patent.Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of oxadiazole inhibitors of leukotriene production. And the patent contained the following:

The title compounds I [R1, R2 = H, alkyl, carboxyxlice (with the proviso that both R1 and R2 are not hydrogen); R3 = (un)substituted 5-11 membered heteroaryl ring containing 1-3 heteroatoms selected from N, O and S; R4 = H, halo, alkyl, nitrile; R5 = (un)substituted alkyl, C3-10 carbocycle, 5-11 membered heterocycle, etc.], useful in treating a leukotriene-mediated disorders, were prepared Thus, reacting compound II (preparation given) with the pyrimidine derivative III afforded the title compound IV. Biol. testing showed that compounds I are effective inhibitors of 5-lipoxygenase activating protein (FLAP) and thus inhibit leukotriene production (IC50 values were given). The invention also relates to pharmaceutical compositions comprising compounds I, methods of I in the treatment of various diseases and disorders, processes for preparing I and intermediates useful in these processes. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

The Article related to oxadiazole preparation leukotriene production ltb4 inhibitor, lipoxygenase activating protein flap inhibitor oxadiazole preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On September 30, 2021, Ameriks, Michael K.; Laforteza, Brian Ngo; Ravula, Suchitra; Schiffer, Jamie M.; Stenne, Brice M. published a patent.Electric Literature of 143803-93-4 The title of the patent was Preparation of fused and bridged compounds as monoacylglycerol lipase modulators. And the patent contained the following:

This invention relates to the title compounds I [R1a = alkyl; R1b = H; or R1a and R1b taken together form (CH2)2-3; R2 = (un)substituted Ph, pyridyl, bicyclic heteroaryl; R3 = 1H-alkyl-pyrazolyl, 1H-haloalkyl-pyrazolyl, 1H-pyridyl-pyrazolyl, etc.; with the proviso], and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, to pharmaceutical compositions containing them, to methods of making them, and to methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurol. disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions. E.g., a multi-step synthesis of (S)-II, starting from Et L-alaninate hydrochloride and Et 4-bromobutanoate, was described. Exemplified compounds I were tested for their in vitro activity of MGL (data given for representative compounds I). The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).Electric Literature of 143803-93-4

The Article related to analgesics, antidepressants, antitumor agents, anxiety disorders (anxious depression), anxiolytics, asperger syndrome, bipolar disorder, depression (treatment-resistant), eye disease and other aspects.Electric Literature of 143803-93-4

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On July 30, 2020, Tang, Guozhi; Li, Dongbo; Li, Liugen; Zha, Xianchan; Chen, Wenming; Wang, Shaomeng; Yang, Chao-Yie published a patent.Formula: C9H12N2O3 The title of the patent was Preparation of macrocyclic fused pyrazoles as Mcl-1 inhibitors. And the patent contained the following:

The title compounds represented by formula I [R = H or C1-6 alkyl; X = O, S, S(O), S(O)2, or (un)substituted NH; ring A = each (un)substituted 1,3-phenylene or 1,3-naphthalenylene; ring B = arylenyl and heteroarylenyl; ring C = each (un)substituted 1H-pyrazol-3,4-diyl or 1H-pyrazol-4,5-diyl; L1 = [C(R14a)(R14b)]s; L2 = [C(R14c)(R14d)]t; L3 = [C(R14c)(R14f)]v; R14a, R14b, R14d, R14f = each independently H or C1-4 alkyl; s = 2,3,4,5, or 6; t, v = each independently 1,2,3, or 4] or pharmaceutically acceptable salts or solvates thereof are prepared The compounds I are useful for treating a condition or disorder responsive to Mcl-1 inhibition such as cancer, a chronic autoimmune disorder, an inflammatory condition, a proliferative disorder, sepsis, or a viral infection. Thus, Et 7-[2-(bromomethyl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-chloro-3-[3-[[3-[(4-methoxybenzyl)thio]naphthalen-1-yl]oxy]propyl]-1-methyl-1H-indole-2-carboxylate underwent thioetherification with S-[[5-[[(tert-butyldimethylsilyl)oxy]methyl]-1-methyl-1H-pyrazol-3-yl]methyl] ethanethioate in the presence of K2CO3 in methanol/THF at room for 1 h to give 27% Et 7-[2-[[[[5-[[(tert-butyldimethylsilyl)oxy]methyl]-1-methyl-1H-pyrazol-3-yl]methyl]thio]methyl]-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-chloro-3-[3-[[3-[(4-methoxybenzyl)thio]naphthalen-1-yl]oxy]propyl]-1-methyl-1H-indole-2-carboxylate (II; Ra = 4-methoxybenzyl, Rb = tert-butyldimethylsilyloxy) which was treated with Bu4NF·3H2O in dry THF at room temperature for 2 h to give II (Ra = 4-methoxybenzyl, Rb = HO). Bromination of II (Ra = 4-methoxybenzyl, Rb = HO) with CBr4 and PPh3 in CH2Cl2 at room temperature for 3 h gave II (Ra = 4-methoxybenzyl, Rb = Br) as a brown oil which underwent debenzylation by treatment with triethylsilane and CF3CO2H in CH2Cl2 at room temperature overnight to give II (Ra = H, Rb = Br). Cyclization of II (Ra = H, Rb = Br) by treatment with K2CO3 in acetonitrile at room temperature for 3 h gave macrocyclic 7-(pyrrolo[1,2-b]pyrazol-3-yl)indole-2-carboxylic acid Et ester (III; Rc = Et) which was saponified with a mixture of 2 N aqueous NaOH solution, THF, and MeOH at room temperature for 5 h followed by acidification with 1 N aqueous HCl solution to give III (Rc = H) in 3% over 6 steps. III (Rc = H) showed IC50 of 15 nM against the competitive binding of a fluorescein labeled 21-residue Bid BH3 peptide (residues 79-99) [Swiss-Prot: P55957] to Mcl-1 protein. It showed IC50 of 437 and 123 nM against OPM2 and H929 cell, resp., in a cell viability assay. The experimental process involved the reaction of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate(cas: 153597-59-2).Formula: C9H12N2O3

The Article related to indolyl fused pyrazole macrocyclic compound preparation mcl 1 inhibitor, macrocyclic fused pyrazole preparation mcl 1 inhibitor, cancer chronic autoimmune disorder treatment macrocyclic fused pyrazole preparation, inflammatory condition proliferative disorder macrocyclic fused pyrazole preparation, sepsis viral infection macrocyclic fused pyrazole preparation and other aspects.Formula: C9H12N2O3

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On October 4, 2012, Vankayalapati, Hariprasad; Appalaneni, Rajendra P.; Reddy, Y. Venkata Krishna published a patent.COA of Formula: C7H8N4 The title of the patent was Preparation of substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine and pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors. And the patent contained the following:

This invention relates to the title compounds I-III [X = N, CH; L1 = a bond, (un)substituted 6-membered aryl, heteroaryl, etc.; R1-R3 = H, halo, CN, etc.; Q = NH, O, S, etc.; L2 = IV (wherein X1 = N, CH; X2 = N, CH; X3 = N, CH; R10 = H, halo, CN, etc.)] which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson’s disease, Alzheimer’s disease, Down’s syndrome, Huntington’s disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases, and to methods for making them. Seventy title compounds were prepared and formulated. For example, a multi-step synthesis of V, starting from mucobromic acid, was described. Exemplified title compounds were tested in the LRRK2 kinase assay (data given). Also disclosed are pharmaceutical compositions including the title compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using title compounds and pharmaceutical compositions including the title compounds The experimental process involved the reaction of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine(cas: 1186608-73-0).COA of Formula: C7H8N4

The Article related to pyrazinylpyrazolopyridine pyrazolopyridine preparation protein kinase inhibitor antitumor antiinflammatory antiparkinsonian, parkinson’s alzheimer’s disease down’s syndrome treatment pyrazinylpyrazolopyridine pyrazolopyridine preparation, huntington’s disease neurodegenerative cns disorder treatment pyrazinylpyrazolopyridine pyrazolopyridine preparation and other aspects.COA of Formula: C7H8N4

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On July 1, 2021, Pinkerton, Anthony; Sergienko, Eduard; Kiyotsuka, Yohei; Kagechika, Katsuji; Kurosaki, Yasunobu; Arai, Yoshikazu; Nagamochi, Masatoshi; Ishibashi, Koutaro published a patent.Safety of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol The title of the patent was Preparation of bicyclic heteroaryls, especially thienopyrimidines, as ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) modulators. And the patent contained the following:

The invention is related to the preparation of bicyclic heteroaryl-based small mol. modulators of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), e.g., of formula I [B = aryl or a 5 or 6-membered heteroaryl; n = 0-3; X = (CH2)1-2; p = 0-3; Y1 = NR4, O; L1 = Y2L2, Y2L2L3; Y2 = a bond, CO; L2 = a bond, (un)substituted alk(en/yn)ylene, heteroalkylene, C2-C6 cycloalkylene; R1 = H, halo, CN, OH, etc.; R2 = H, COOH and derivatives, fluoroalkoxy, etc.; R3 = H, halo, SH and derivatives, NH2 and derivatives, etc.; R5 = independently at each occurrence H, NO2, CN, SO2NH2 and derivatives, etc.; R6 = independently at each occurrence halo, alk(en/yn)yl, etc.; ], their pharmaceutically acceptable salts and solvates , compositions containing them, and methods of using the compounds and compositions comprising the compounds for treating disorders associated with ENPP1, such as pseudogout. Thus, II was prepared by cyclization of Me 3-amino-4-methylthiophene-2-carboxylate with formamide, chlorination of 7-methylthieno[3,2-d]pyrimidin-4-ol with POCl3, amination of 4-chloro-7-methylthieno[3,2-d]pyrimidine with tert-Bu (piperidin-4-yl)carbamate, cleavage of tert-butoxycarbonyl group and benzylation of 1-(7-methylthieno[3,2-d]pyrimidin-4-yl)piperidin-4-amine with benzyl chloride. II inhibited ENPP1 in a TR-FRET assay (IC50 in the range of 0.1μM – 1.0μM). The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Safety of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol

The Article related to bicyclic heteroaryl preparation ectonucleotide pyrophosphatase phosphodiesterase 1 enpp1 inhibitor, thienopyrimidine pyrazolopyrimidine pyrazolopyridine thienopyridine preparation enpp1 inhibitor pseudogout antiarthritic, triazolopyrimidine isoxazolopyrimidine pyrazolopyridazine isothiazolopyrimidine preparation enpp1 inhibitor and other aspects.Safety of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On December 7, 2006, Mansour, Tarek Suhayl; Venkatesan, Aranapakam Mudumbai published a patent.HPLC of Formula: 153597-59-2 The title of the patent was Bicyclic 6-alkylidene-penems as class-D β-lactamase inhibitors. And the patent contained the following:

Penems, such as I [R = H, alkali metal, C1-6 alkyl, C5-6 cycloalkyl, or substituted ester; A, B = H, heteroaryl, fused bicycles, fused tricycles, etc.], were prepared for use in pharmaceutical compositions as inhibitors of β-lactamases which are class-D enzymes that hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections. Thus, (5R,6Z)-6-(7-methyl-5,6,7,8-tetrahydroimidazo[1,2-a]pyrazin-2-ylmethylene)-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid sodium salt (II) was prepared via a coupling reaction of 7-methyl-5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine-2-carboxaldehyde with (5R,6S)-6-bromo-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid 4-nitrobenzyl ester. The prepared penems were assayed for microbial susceptibility against E. coli GC 2883, a class-D producing organism. The experimental process involved the reaction of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate(cas: 153597-59-2).HPLC of Formula: 153597-59-2

The Article related to alkylidene penem derivative preparation beta lactamase inhibitor, beta lactam antibiotic alkylidene penem derivative preparation, antibacterial agent alkylidene penem derivative preparation beta lactamase inhibitor, bacterial infection treatment alkylidene penem preparation beta lactamase inhibitor and other aspects.HPLC of Formula: 153597-59-2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On September 18, 2014, Nazare, Marc; Halland, Nis; Schmidt, Friedemann; Kleemann, Heinz-Werner; Weiss, Tilo; Saas, Joachim; Struebing, Carsten published a patent.Synthetic Route of 98138-75-1 The title of the patent was Preparation of N-[4-(azaindazol-6-yl)-phenyl]-sulfonamides as SGK1 inhibitors. And the patent contained the following:

The title compounds I [Ar = (un)substituted Ph, 5-6 membered monocyclic, aromatic, heterocyclic group which comprises 1-3 identical or different ring heteroatoms selected from the series consisting of N, O and S, and is bonded via a ring C atom; n = 0-2; X = N, CH; Z = a bond, O, S, (un)substituted NH; R1 = H, (un)substituted NH2, NHC(O)NH2, etc.; R2 = halo, alkyl, alkoxy, CN; R3 = H, alkyl, -alkyl-R (R = (un)substituted 3-12 membered, monocyclic or bicyclic, saturated, partially unsaturated or aromatic, cyclic group which comprises 0-3 identical or different ring heteroatoms selected from N, O and S)] which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism, were prepared E.g., a multi-step synthesis of II, starting from 2,5-dichlorobenzenesulfonyl chloride and 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenylamine, was described. Exemplified compounds I were tested for serum and glucocorticoid-regulated kinase 1 (SGK-1) inhibitory activity (data given). The invention furthermore relates to processes for the preparation of compounds I, their use as pharmaceuticals, and pharmaceutical compositions comprising them. The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Synthetic Route of 98138-75-1

The Article related to azaindazolylphenyl sulfonamide preparation sgk1 inhibitor antiinflammatory antirheumatic antiarthritic, degenerative joint disorder osteoarthritis treatment azaindazolylphenyl sulfonamide preparation, serum glucocorticoid regulated kinase sgk inhibitor azaindazolylphenyl sulfonamide preparation and other aspects.Synthetic Route of 98138-75-1

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On April 13, 2017, Aiguade Bosch, Jose; Connolly, Stephen; Eastwood, Paul Robert; Gomez Castillo, Elena; Moreno Mollo, Immaculada Montserrat; Roberts, Richard Spurring; Sevilla Gomez, Sara published a patent.Application of 314021-93-7 The title of the patent was Preparation of bicyclic fused pyrimidinone and triazinone derivatives as new TRPA1 antagonists. And the patent contained the following:

The present invention relates to compounds of Formula I [G1 = C or N atom; G2, G3, G4, G5 = each independently C(Ra), N(Rb), or N; G6 = N, G7 = C atom, G8 = N atom, G9 = O atom; Ra = H, linear or branched C1-4 alkyl, halogen atom, linear or branched C1-4 alkoxy, linear or branched C1-4 haloalkyl, linear or branched C1-4 haloalkoxy, oxo, C3-7 cycloalkyl, cyano, amino, mono – or di(C1-4 alkyl)amino, or hydroxy; Rb = H or linear or branched C1-4 alkyl; L = (un)substituted linear or branched C2-4 alkylene, C(Rb):C(Rb), C3-7 cycloalkylene, (CH2)2-3-O, (CH2)1-2-C(O), (CH2)1-2-S, (CH2)1-2-S(O), CONH, CF2O, or 4- to 6-membered N-containing heterocyclylene, wherein at least one nitrogen atom is linked the G7 group; Q = each (un)substituted monocyclic or bicyclic C6-14 aryl or monocyclic or bicyclic 5- to 14-membered heteroaryl containing at least one heteroatom selected from N, O and S; or when Q = Ph, L together with Q form a 5- to 7-membered N-containing heterocyclyl fused to the Ph group; n = 0-1; the solid/dashed line = single or a double bond], pharmaceutically acceptable salts, solvates, N-oxides, tautomers, stereoisomers, or isotopically-labeled derivatives thereof:. These compounds are used in the treatment of a pathol. condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism. The pathol. condition or disease is selected from acute and/or chronic pruritus, acute and/or chronic pain, inflammatory dermatol. diseases, respiratory disorders, gastrointestinal inflammatory disorders, and urinary tract disorders. Thus, a suspension of 0.040 g 5-methylquinazolin-4(3H)-one and 0.069 g potassium carbonate in 1.0 mL DMF was stirred at room temperature for 10 min, followed by adding a solution of 0.071 g 5-(chloromethyl)-3-[2-(4-chlorophenyl)ethyl]-1,2,4-oxadiazole in 0. 5 mL DMF, and the resulting mixture of was stirred for 3 h to give, after workup and flash chromatog., 72% 3-[[3-[2-(4-chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-5-methylquinazolin-4(3H)-one (II). II and 3-[[3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-5-methylimidazo[5,1-f]-[1,2,4]triazin-4(3H)-one (III) inhibited the tetracycline-inducible human TRPA1 expression in CHO cells in a calcium flux assay with IC50 of 100-1,000 and <100 nM, resp. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Application of 314021-93-7

The Article related to fused pyrimidinone preparation trpa1 antagonist, bicyclic fused triazinone preparation trpa1 antagonist, transient receptor potential cation channel trpa trpa1 antagonist, acute chronic pruritus treatment bicyclic heterocycle, chronic acute pain treatment bicyclic heterocycle and other aspects.Application of 314021-93-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On May 31, 2011, Wenglowsky, Steve; Ren, Li; Ahrendt, Kateri A.; Laird, Ellen R.; Aliagas, Ignacio; Alicke, Bruno; Buckmelter, Alex J.; Choo, Edna F.; Dinkel, Victoria; Feng, Bainian; Gloor, Susan L.; Gould, Stephen E.; Gross, Stefan; Gunzner-Toste, Janet; Hansen, Joshua D.; Hatzivassiliou, Georgia; Liu, Bonnie; Malesky, Kim; Mathieu, Simon; Newhouse, Brad; Raddatz, Nicholas J.; Ran, Yingqing; Rana, Sumeet; Randolph, Nikole; Risom, Tyler; Rudolph, Joachim; Savage, Scott; Selby, LeAnn T.; Shrag, Michael; Song, Kyung; Sturgis, Hillary L.; Voegtli, Walter C.; Wen, Zhaoyang; Willis, Brandon S.; Woessner, Richard D.; Wu, Wen-I.; Young, Wendy B.; Grina, Jonas published an article.Computed Properties of 1186608-73-0 The title of the article was Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors. And the article contained the following:

The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approx. 7% of all cancers. Using structure-based design, a novel series of pyrazolopyridine inhibitors of B-RafV600E was developed. Optimization led to the identification of 3-methoxy pyrazolopyridines 17 and 19, potent, selective, and orally bioavailable agents that inhibited tumor growth in a mouse xenograft model driven by B-RafV600E with no effect on body weight On the basis of their in vivo efficacy and preliminary safety profiles, 17 and 19 were selected for further preclin. evaluation. The experimental process involved the reaction of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine(cas: 1186608-73-0).Computed Properties of 1186608-73-0

The Article related to pyrazolopyridine derivative braf kinase inhibitor preparation antitumor pharmacokinetics toxicity, b-rafv600e, mapk pathway, amorphous spray-dried dispersion, pyrazolopyridine, targeted therapy and other aspects.Computed Properties of 1186608-73-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2015,Nicolaou, K. C.; Rhoades, Derek; Wang, Yanping; Totokotsopoulos, Sotirios; Bai, Ruoli; Hamel, Ernest published 《Synthesis and Biological Evaluation of Novel Epothilone B Side Chain Analogues》.ChemMedChem published the findings.Name: 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

The design, synthesis, and biol. evaluation of a series of epothilone analogs with novel side chains equipped with an amino group are described. Their design facilitates potential conjugation to selective drug delivery systems such as antibodies. Their synthesis proceeded efficiently via Stille coupling of a readily available vinyl iodide and heterocyclic stannanes. Cytotoxicity studies and tubulin binding assays revealed two of these analogs, I (R = CF3, F), to be more potent than epothilones A-D and the anticancer agent ixabepilone, currently in clin. use. The experimental process involved the reaction of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Name: 3-(Trifluoromethyl)-1H-pyrazole)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Name: 3-(Trifluoromethyl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics