Month: November 2022

Sunagar, Manjunath G. published the artcileSynthesis of novel N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine derivatives as inducers of apoptosis in MCF-7 breast cancer cells, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is RSC Advances (2016), 6(19), 15286-15297, database is CAplus.

A series of N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine derivatives (PP05-PP21) were prepared and evaluated for their anticancer activity against a panel of human cancer cell lines. Evaluation of results revealed that some of the synthesized compounds exhibited promising anticancer activity against the examined cancer cell lines. The structure-activity relationship (SAR) studies in the present work revealed that simple N-9 alkyl substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purines are potent anticancer agents. Among all the compounds, PP17 (9-sec-butyl-6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine) showed good inhibitory activity against MCF-7 cells. Cell cycle anal. of the compound suggested that induces G2/M phase arrest. Biochem. experiments showed that PP17 significantly induced MCF-7 cell apoptosis. Therefore, compound PP17 with a potent in vitro anticancer activity can serve as a promising lead compound for further study.

RSC Advances published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C14H10O4, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Blass, Benjamin E. published the artcileDesign, synthesis, and evaluation of novel, selective γ-butyrolactones sigma-2 ligands, Recommanded Product: 1-(3-Cyanophenyl)piperazine, the publication is Medicinal Chemistry Research (2021), 30(9), 1713-1727, database is CAplus.

Nearly 40 years after the first disclosure of sigma receptors, the sigma-2 (σ2) receptor was recently identified as the Transmembrane Protein 97 (TMEM97, also known as MAC30 (Meningioma-associated protein)). This macromol. has been associated with a number of disease states such as schizophrenia, Alzheimer’s disease, neuropathic pain, traumatic brain injury, and cancer. We have recently identified a series of novel, functionalized γ-butyrolactones that are potent σ2 receptor ligands that are drug-like and identified a potential candidate (I) for future in vivo study.

Medicinal Chemistry Research published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Recommanded Product: 1-(3-Cyanophenyl)piperazine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Zhang, Huairong published the artcileIdentification of differentially expressed kinase and screening potential anticancer drugs in papillary thyroid carcinoma, HPLC of Formula: 863127-77-9, the publication is Disease Markers (2016), 2832980/1-2832980/9, database is CAplus and MEDLINE.

We aim to identify protein kinases involved in the pathophysiol. of papillary thyroid carcinoma (PTC) in order to provide potential therapeutic targets for kinase inhibitors and unfold possible mol. mechanisms. The gene expression profile of GSE27155 was analyzed to identify differentially expressed genes and mapped onto human protein kinases database. Correlation of kinases with PTC was addressed by systematic literature search, GO and KEGG pathway anal. The functional enrichment anal. indicated that “mitogen-activated protein kinases pathway” expression was extremely enriched, followed by “neurotrophin signaling pathway,” “focal adhesion,” and “GnRH signaling pathway.”. MAPK, SRC, PDGFRa, ErbB, and EGFR were significantly regulated to correct these pathways. Kinases investigated by the literature on carcinoma were considered to be potential novel mol. therapeutic target in PTC and application of corresponding kinase inhibitors could be possible therapeutic tool. SRC,MAPK, and EGFR were the most important differentially expressed kinases in PTC. Combined inhibitors may have high efficacy in PTC treatment by targeting these kinases.

Disease Markers published new progress about 863127-77-9. 863127-77-9 belongs to piperazines, auxiliary class TGF-beta/Smad,Bcr-Abl,Natural product, name is N-(2-Chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide hydrate, and the molecular formula is C6H4KNO6S, HPLC of Formula: 863127-77-9.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Power, Eoin C. published the artcilePartial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK_Ca), Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Bioorganic & Medicinal Chemistry Letters (2006), 16(4), 887-890, database is CAplus and MEDLINE.

A series of partial structures of ketoconazole has been synthesized and tested for activity on the large conductance calcium-activated potassium channel (BK) in bovine smooth muscle cells. This has provided openers and blockers of the channel. The results suggest that the Ph and phenoxy moieties are important for interaction with BK, whereas the imidazole group is unimportant. The properties of the phenoxy moiety seem to determine whether the compounds act to open or block the channel.

Bioorganic & Medicinal Chemistry Letters published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Mehta, Naimee published the artcileOptimization of Physicochemical Properties for 4-Anilinoquinoline Inhibitors of Plasmodium falciparum Proliferation, Category: piperazines, the publication is ACS Infectious Diseases (2018), 4(4), 577-591, database is CAplus and MEDLINE.

The authors recently reported the medicinal chem. reoptimization of a known human tyrosine kinase inhibitor, lapatinib, against a variety of parasites responsible for numerous tropical diseases, including human African trypanosomiasis (Trypanosoma brucei), Chagas disease (T. cruzi), Leishmaniasis (Leishmania spp.), and malaria (Plasmodium falciparum). Herein, the authors report the authors’ continuing efforts to optimize this series against P. falciparum. Through the design of a library of compounds focused on reducing the lipophilicity and mol. weight, followed by an SAR exploration, the authors have identified NEU-1953 (40). This compound is a potent inhibitor of P. falciparum with an improved ADME profile over the previously reported compound, NEU-961.

ACS Infectious Diseases published new progress about 914610-39-2. 914610-39-2 belongs to piperazines, auxiliary class Piperazine,Boronic acid and ester,Sulfamide,Benzene,Piperazine,Boronate Esters,Boronic acid and ester,, name is 1-Methyl-4-((4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)sulfonyl)piperazine, and the molecular formula is C17H27BN2O4S, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Camps, Pelayo published the artcileStereoselective syntheses of both enantiomers of ketoconazole from (R)- and (S)-epichlorohydrin, HPLC of Formula: 67914-60-7, the publication is Tetrahedron: Asymmetry (1995), 6(6), 1283-94, database is CAplus.

Stereoselective syntheses of both enantiomers of ketoconazole (I) from com. available (R)- or (S)-epichlorohydrin has been developed. The key step of these syntheses involves the selective substitution of the methylene chlorine atom by benzoate on a mixture of (2S,4R)-II and (2R,4R)-II or of their enantiomers, followed by crystallization of the corresponding cis-benzoates, from which (+)- or (-)-I were obtained as described for (±)-I. The ee’s of (+)- and (-)-ketoconazole were determined by HPLC on the CSP Chiralcel OD-H.

Tetrahedron: Asymmetry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, HPLC of Formula: 67914-60-7.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Cummings, David F. published the artcileThree amino acids in the D₂ dopamine receptor regulate selective ligand function and affinity, Related Products of piperazines, the publication is Journal of Neurochemistry (2009), 110(1), 45-57, database is CAplus and MEDLINE.

The D₂ dopamine receptor is an important therapeutic target for the treatment of psychotic, agitated, and abnormal behavioral states. To better understand the specific interactions of subtype-selective ligands with dopamine receptor subtypes, seven ligands with high selectivity (>120-fold) for the D₄ subtype of dopamine receptor were tested on wild-type and mutant D₂ receptors. Five of the selective ligands were observed to have 21-fold to 293-fold increases in D₂ receptor affinity when three non-conserved amino acids in TM2 and TM3 were mutated to the corresponding D₄ amino acids. The two ligands with the greatest improvement in affinity for the D₂ mutant receptor [i.e., 3-([4-(4-iodophenyl) piperazin-1-yl]methyl)-1H-pyrrolo[2,3-b]pyridine (L-750,667) and 1-[4-iodobenzyl]-4-[N-(3-isopropoxy-2-pyridinyl)-N-methyl]- aminopiperidine (RBI-257)] were investigated in functional assays. Consistent with their higher affinity for the mutant than for the wild-type receptor, concentrations of L-750,667 or RBI-257 that produced large reductions in the potency of quinpirole’s functional response in the mutant did not significantly reduce quinpirole’s functional response in the wild-type D₂ receptor. In contrast to RBI-257 which is an antagonist at all receptors, L-750,667 is a partial agonist at the wild-type D₂ but an antagonist at both the mutant D₂ and wild-type D₄ receptors. Our study demonstrates for the first time that the TM2/3 microdomain of the D₂ dopamine receptor not only regulates the selective affinity of ligands, but in selected cases can also regulate their function. Utilizing a new docking technique that incorporates receptor backbone flexibility, the three non-conserved amino acids that encompass the TM2/3 microdomain were found to account in large part for the differences in intermol. steric contacts between the ligand and receptors. Consistent with the exptl. data, this model illustrates the interactions between a variety of subtype-selective ligands and the wild-type D₂, mutant D₂, or wild-type D₄ receptors.

Journal of Neurochemistry published new progress about 337972-47-1. 337972-47-1 belongs to piperazines, auxiliary class Inhibitor, name is 2-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine, and the molecular formula is C18H19ClN4, Related Products of piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Oshima, Shinji published the artcileStudy on the increased probability of detecting adverse drug reactions based on Bayes’ theorem: evaluation of the usefulness of information on the onset timing of adverse drug reactions, Recommanded Product: N-(2-Chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide hydrate, the publication is Biological & Pharmaceutical Bulletin (2017), 40(9), 1389-1398, database is CAplus and MEDLINE.

In order to avoid adverse drug reactions (ADRs), pharmacists are reconstructing ADR-related information based on various types of data gathered from patients, and then providing this information to patients. Among the data provided to patients is the time-to-onset of ADRs after starting the medication (i.e., ADR onset timing information). However, a quant. evaluation of the effect of onset timing information offered by pharmacists on the probability of ADRs occurring in patients receiving this information has not been reported to date. In this study, we extracted 40 ADR-drug combinations from the data in the Japanese Adverse Drug Event Report database. By applying Bayes’ theorem to these combinations, we quant. evaluated the usefulness of onset timing information as an ADR detection predictor. As a result, when information on days after taking medication was added, 54 ADR-drug combinations showed a likelihood ratio (LR) in excess of 2. In particular, when considering the ADR-drug combination of anaphylactic shock with levofloxacin or loxoprofen, the number of days elapsed between start of medication and the onset of the ADR was 0, which corresponded to increased likelihood ratios (LRs) of 138.7301 or 58.4516, resp. When information from 1-7d after starting medication was added to the combination of liver disorder and acetaminophen, the LR was 11.1775. The results of this study indicate the clin. usefulness of offering information on ADR onset timing.

Biological & Pharmaceutical Bulletin published new progress about 863127-77-9. 863127-77-9 belongs to piperazines, auxiliary class TGF-beta/Smad,Bcr-Abl,Natural product, name is N-(2-Chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide hydrate, and the molecular formula is C22H28ClN7O3S, Recommanded Product: N-(2-Chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide hydrate.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Brossard, Dominique published the artcileSynthesis of bile acid derivatives and in vitro cytotoxic activity with pro-apoptotic process on multiple myeloma (KMS-11), glioblastoma multiforme (GBM), and colonic carcinoma (HCT-116) human cell lines, HPLC of Formula: 87179-40-6, the publication is European Journal of Medicinal Chemistry (2010), 45(7), 2912-2918, database is CAplus and MEDLINE.

The use of nitrogenous heterocycles as building blocks in the synthesis of conjugate bile acid derivatives was described. New piperazinyl bile acid derivatives I [R^7a = OH, R^7b = H, R¹² = OH, R²⁴ = 4-methyl-1-piperazinylamino, 4-(trans-cinnamyl)-1-piperazinyl; R^7a = H, R^7b = OH, R¹² = H, R²⁴ = 4-methyl-1-piperazinylamino, 4-(trans-cinnamyl)-1-piperazinyl; R^7a = OH, R^7b = H, R¹² = H, R²⁴ = 4-methyl-1-piperazinylamino, 4-(trans-cinnamyl)-1-piperazinyl] were synthesized and tested in vitro against various human cancer cells (GBM, KMS-11, HCT-116). The best pro-apoptotic activity was obtained with N-(4N-cinnamylpiperazin-1-yl)-3α,7β-dihydroxy-5β-cholan-24-amide I [R^7a = H, R^7b = OH, R¹² = H, R²⁴ = 4-(trans-cinnamyl)-1-piperazinyl] and N-(4N-cinnamyllpiperazin-1-yl)-3α,7α-dihydroxy-5β-cholan-24-amide I [R^7a = OH, R^7b = H, R¹² = H, R²⁴ = 4-(trans-cinnamyl)-1-piperazinyl] on these human cancer cell lines (IC₅₀: 8.5-31.4 μM). This activity was associated with nuclear and DNA fragmentation, demonstrating that I [R^7a = H, R^7b = OH, R¹² = H, R²⁴ = 4-(trans-cinnamyl)-1-piperazinyl] induces cell death by an apoptotic process as does I [R^7a = OH, R^7b = H, R¹² = H, R²⁴ = 4-(trans-cinnamyl)-1-piperazinyl]. This study shows the possibility of heterocycle-steroids as new anticancer agents with improved bioactivity and easy to synthesize.

European Journal of Medicinal Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, HPLC of Formula: 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Irie, Osamu published the artcileDiscovery of selective and nonpeptidic cathepsin S inhibitors, Formula: C12H16N2O2, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(14), 3959-3962, database is CAplus and MEDLINE.

Nonpeptidic, selective, and potent cathepsin S inhibitors were derived from an inhouse pyrrolopyrimidine cathepsin K inhibitor by modification of the P2 and P3 moieties. The pyrrolopyrimidine-based inhibitors show nanomolar inhibition of cathepsin S with over 100-fold selectivity against other cysteine proteases, including cathepsin K and L. Some of the inhibitors showed cellular activities in mouse splenocytes as well as oral bioavailabilities in rats.

Bioorganic & Medicinal Chemistry Letters published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Formula: C12H16N2O2.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics