Category: Uncategorized

High efficacy of BGD (bendamustine, gemcitabine, and dexamethasone) in relapsed/refractory Hodgkin Lymphoma was written by Swoboda, Ryszard;Giebel, Sebastian;Knopinska-Posluszny, Wanda;Chmielowska, Ewa;Drozd-Sokolowska, Joanna;Paszkiewicz-Kozik, Ewa;Kulikowski, Waldemar;Taszner, Michal;Mendrek, Wlodzimierz;Najda, Jacek;Czerw, Tomasz;Olszewska-Szopa, Magdalena;Czyz, Anna;Giza, Agnieszka;Spychalowicz, Wojciech;Subocz, Edyta;Szwedyk, Pawel;Krzywon, Aleksandra;Wilk, Agata;Zaucha, Jan Maciej. And the article was included in Annals of Hematology in 2021.COA of Formula: C16H21Cl2N3O2 The following contents are mentioned in the article:

The optimal salvage therapy in relapsed/refractory Hodgkin lymphoma (R/R HL) has not been defined so far. The goal of this multicenter retrospective study was to evaluate efficacy and safety of BGD (bendamustine, gemcitabine, dexamethasone) as a second or subsequent line of therapy in classical R/R HL. We have evaluated 92 consecutive R/R HL patients treated with BGD. Median age was 34.5 (19-82) years. Fifty-eight patients (63%) had received 2 or more lines of chemotherapy, 32 patients (34.8%) radiotherapy, and 21 patients (22.8%) an autologous hematopoietic stem cell transplantation (autoHCT). Forty-four patients (47.8%) were resistant to first line of chemotherapy. BGD therapy consisted of bendamustine 90 mg/m2 on days 1 and 2, gemcitabine 800 mg/m2 on days 1 and 4, dexamethasone 40 mg on days 1-4. Median number of BGD cycles was 4 (2-7). The following adverse events �3 grade were noted: neutropenia (22.8%), thrombocytopenia (20.7%), anemia (15.2%), infections (10.9%), AST/ALT increase (2.2%), and skin rush (1.1%). After BGD therapy, 51 (55.4%) patients achieved complete remission, 23 (25%)-partial response, 7 (7.6%)-stable disease, and 11 (12%) patients experienced progression disease. AutoHCT was conducted in 42 (45.7%) patients after BGD therapy, and allogeneic HCT (alloHCT) in 16 (17.4%) patients. Median progression-free survival was 21 mo. BGD is a highly effective, well-tolerated salvage regimen for patients with R/R HL, providing an excellent bridge to auto- or alloHCT. This study involved multiple reactions and reactants, such as 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7COA of Formula: C16H21Cl2N3O2).

4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).COA of Formula: C16H21Cl2N3O2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The protective effect of rabeprazole on cisplatin-induced apoptosis and necroptosis of renal proximal tubular cells was written by Chen, Shi-qing;Hu, Bing-feng;Yang, Ya-ru;He, Yuan;Yue, Lin;Guo, Dong;Wu, Ting-ni;Feng, Xiao-wen;Li, Qing;Zhang, Wei;Wen, Jia-gen. And the article was included in Biochemical and Biophysical Research Communications in 2022.Recommanded Product: 117976-90-6 The following contents are mentioned in the article:

Nephrotoxicity is a major adverse reaction of cisplatin-based chemotherapy. Organic cation transporter 2 (OCT2) which is located on the basement membrane of human proximal renal tubules is responsible for the renal accumulation of cisplatin and its nephrotoxicity. This study aimed to investigate the protective effect of PPIs to CP-induced nephrotoxicity. Three kinds of PPIs including lansoprazole, omeprazole and rabeprazole (Rab) were co-administrated with CP to mice. In addition, OCT2-overexpressed HEK293, HK-2 and A549 cells were co-incubated with CP and PPIs. The results showed that PPIs can attenuate CP-induced increase of CRE, BUN and histol. damage of kidney. Among the three PPIs, Rab was found with a superior protective effect. It significantly reduced the accumulation of CP in OCT2-overexpressed HEK293 cells and in the renal cortex tissues of mice, but not in HK-2 cells. Moreover, Rab reduced the expression levels of cleaved-caspase-3, RIPK1, RIPK3, MLKL and p-MLKL and the apoptosis rate of renal tubular cells induced by CP in vivo, but not in HK-2 cells. However, Rab increased the viability of CP-treated cells in a concentration-dependent manner and attenuated CP-induced apoptosis and necroptosis in OCT2 over-expressed HEK293 cells. Finally, we demonstrated that Rab have no influence on the antitumor effect of CP. In conclusion, Rab attenuate CP-induced nephrotoxicity mainly through inhibiting OCT2-mediated CP uptake, without interfering with its anti-tumor property of inducing apoptosis and necroptosis. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Recommanded Product: 117976-90-6).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. Imidazole has been usedin the lysis, wash and elution buffer for the purification of histidine tagged Sonic Hedgehog(shh-N) protein, in elution buffer in stepwise gradient for the purification of histidine tagged aldo keto reductases using nickel affinity chromatography, as a component of homogenization buffer for the purification of phagosomal compartments from dendritic cells.Recommanded Product: 117976-90-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Petryayeva, Eleonora published the artcileA job for quantum dots: use of a smartphone and 3D-printed accessory for all-in-one excitation and imaging of photoluminescence, Synthetic Route of 359860-27-8, the publication is Analytical and Bioanalytical Chemistry (2016), 408(11), 2913-2925, database is CAplus and MEDLINE.

Point-of-care (POC) diagnostic technologies are needed to improve global health and smartphones are a prospective platform for these technologies. While many fluorescence or photoluminescence-based smartphone assays have been reported in the literature, common shortcomings are the requirement of an excitation light source external to the smartphone and complicated integration of that excitation source with the smartphone. Here, the photog. flash associated with the smartphone camera can be used to enable all-in-one excitation and imaging of photoluminescence (PL), thus eliminating the need for an excitation light source external to the smartphone. A simple and low-cost 3D-printed accessory was designed to create a dark environment and direct excitation light from the smartphone flash onto a sample. Multiple colors and compositions of semiconductor quantum dot (QD) were evaluated as photoluminescent materials for all-in-one smartphone excitation and imaging of PL, and these were compared with fluorescein and R-phycoerythrin (R-PE), which are widely used mol. and protein materials for fluorescence-based bioanal. The QDs exhibit much better brightness and have the best potential for two-color detection. A model protein binding assay with a sub-microgram per mL detection limit and a Forster resonance energy transfer (FRET) assay for proteolytic activity were demonstrated, including imaging with serum as a sample matrix. In addition, FRET within tandem conjugates of a QD donor and fluorescent dye acceptor enabled smartphone detection of dye fluorescence that was otherwise unobservable without the QD to enhance its brightness. The ideal properties of photoluminescent materials for all-in-one smartphone excitation and imaging are discussed in the context of several different materials, where QDs appear to be the best overall material for this application.

Analytical and Bioanalytical Chemistry published new progress about 359860-27-8. 359860-27-8 belongs to imidazoles-derivatives, auxiliary class Other Aliphatic Heterocyclic,Chiral,Amine,Amide,Ether,Inhibitor, name is N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, and the molecular formula is C18H34N4O5S, Synthetic Route of 359860-27-8.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Elkamhawy, Ahmed published the artcileOptimization study towards more potent thiazolidine-2,4-dione IKK-β modulator: Synthesis, biological evaluation and in silico docking simulation, Safety of 3-Chloro-4-(1H-imidazol-1-yl)benzaldehyde, the main research area is arylidene methylpiperazinylbutoxyphenyl thiazolidinedione diastereoselective preparation IKK inhibition SAR docking; IKK-β modulator; Molecular docking; NF-κB signaling pathway; Thiazolidine-2,4-dione.

A novel class of thiazolidine-2,4-diones I [R1 = 3-imidazol-1-ylphenyl, 5-phenylthiophen-2-yl, 4-chlorophenoxyphenyl, etc.] as structurally novel modulators for IKK-β was identified. A hit optimization study via analog synthesis strategy aiming to acquire more potent derivatives, probe the structure activity relationship (SAR) and get reasonable explanations for the elicited IKK-β inhibitory activities though an in-silico docking simulation study was reported. Accordingly, a new series of eighteen thiazolidine-2,4-dione derivatives was rationally synthesized, identified with different spectroscopic techniques and biol. evaluated as noteworthy IKK-β potential modulators. Successfully, new IKK-β potent modulators were obtained, including the most potent analog up-to-date I [R1 = 4-chlorophenoxyphenyl] with IC50 value of 260 nM. A detailed structure activity relationship (SAR) was discussed and a mechanistic study for I [R1 = 4-chlorophenoxyphenyl] was carried out indicating its irreversible inhibition mode with IKK-β (Kinact value = 0.01 (min-1)). Furthermore, the conducted in-silico simulation study provided new insights for the binding modes of this novel class of modulators with IKK-β.

Bioorganic Chemistry published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 870837-48-2 belongs to class imidazoles-derivatives, name is 3-Chloro-4-(1H-imidazol-1-yl)benzaldehyde, and the molecular formula is C10H7ClN2O, Safety of 3-Chloro-4-(1H-imidazol-1-yl)benzaldehyde.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Zhang, Ying Ping published the artcileStructural basis of the mutagenicity of heterocyclic amines formed during the cooking processes, HPLC of Formula: 116599-55-4, the main research area is amine structure mutagenicity; MSBAR heterocyclic amine mutagen.

A database consisting of 61 heterocyclic amines formed during food preparation and their desamino analogs was subjected to structure-activity anal. using the CASE method, a structural activity relational expert system. The program identified the major structural determinants associated with mutagenic activity or lack thereof. The structures identified as contributing to the probability of activity as well as those associated with mutagenic potency were highly predictive of mols. not in the learning set. The major structural determinant, the aromatic amino moiety, and quantum mech. calculations revealed that the mutagenic potency associated with this functionality derived from their contribution to the energy of the LUMO.

Environmental and Molecular Mutagenesis published new progress about Mutagens. 116599-55-4 belongs to class imidazoles-derivatives, name is 5,7-Dimethyl-1H-imidazo[4,5-b]pyridine, and the molecular formula is C8H9N3, HPLC of Formula: 116599-55-4.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On September 10, 1991, Simha, Devendranath; Palejwala, Vaseem A.; Humayun, M. Zafri published an article.Related Products of 55662-66-3 The title of the article was Mechanisms of mutagenesis by exocyclic DNA adducts. Construction and in vitro template characteristics of an oligonucleotide bearing a single site-specific ethenocytosine. And the article contained the following:

It is widely accepted that mutagenic DNA lesions fall into two categories: mispairing lesions hydrogen bond with an incorrect incoming base, generally do not stop replication, and possess high mutagenic efficiency without any requirement for induced functions; noninstructional lesions lack accessible template information, act as strong blocks to DNA replication (and are therefore toxic), and their mutagenic effects are SOS-dependent. The recent results show that a noninstructional exocyclic DNA lesion induced by vinyl chloride, may have unusual mutagenic properties. To obtain more definitive exptl. evidence for the observed effects, a single ethenocytosine (εC) residue was introduced at a specific site of coliphage M13AB28 replicative form DNA by a single-stranded linker-ligation technique. The resulting DNA was purified and transfected into appropriate recA+ or recA- Escherichia coli host cells. The effect of εC on survival was determined from transfection efficiency. Both the frequency and specificity of mutations induced by εC were determined by direct sequence anal. of randomly picked progeny phage plaques. The results indicated that εC has little effect on the survival of M13 DNA. Approx. 30% of the progeny phage obtained by transfecting εC DNA had a base substitution mutation precisely at the lesion site. No such mutations were observed in progeny plaques obtained by transfecting the control DNA construct. All εC-induced mutations were either C-to-T transitions or C-to-A transversions. Neither survival nor mutagenic efficiency was significantly affected in recA- host cells. The findings reported here and in the preceding paper suggest that ethenocytosine may represent a novel type of RecA-independent, highly mutagenic noninstructional DNA lesion. These and other results argue that a requirement for SOS functions is neither a defining attribute nor an exclusive attribute of noninstructional lesions. These data also support the possibility that mutation recovery (i.e., lesion bypass) rather than misincorporation may be the major role of SOS functions in mutagenesis. Finally, the high mutagenic efficiency observed makes εC a reasonable candidate for mediating the genotoxic properties of vinyl chloride, a suspected human carcinogen, and a major industrial chem. that is produced in large quantities around the world. The experimental process involved the reaction of Imidazo[1,2-c]pyrimidin-5(6H)-one(cas: 55662-66-3).Related Products of 55662-66-3

The Article related to ethenocytosine lesion dna mutagenicity, Toxicology: Carcinogens, Mutagens, and Teratogens and other aspects.Related Products of 55662-66-3

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On April 30, 1999, Chitale, Dipalee; Pratap, K.; Amarpal; Singh, G. R.; Gupta, O. P. published an article.Category: imidazoles-derivatives The title of the article was Biochemical effects of ketamine with premedication of alpha-2 agonists and diazepam in goats. And the article contained the following:

The authors studied the biochem. changes in goats premedicated with diazepam along with xylazine, medetomidine or romifidine hydrochloride and anesthetized with ketamine. None of the combinations caused alarming changes in different biochem. parameters and therefore, may be considered safe for the goats. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Category: imidazoles-derivatives

The Article related to anesthetic ketamine alpha2 adrenoceptor agonist diazepam goat, medetomidine diazepam romifidine xylazine ketamine anesthetic, cholesterol glucose bilirubin albumin general anesthesia and other aspects.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Boulton, B. E.; Coller, B. A. W. published the artcile< Kinetics, stoichiometry, and mechanism in the bromination of aromatic heterocycles. II. Aqueous bromination of imidazole, 1-methylimidazole, and 2-methylimidazole>, Name: 5-Bromo-1-methyl-1H-imidazole, the main research area is imidazole bromination kinetics.

The coulo-chrono-potentiometric method was used to obtain rate constants for reaction of Br with neutral imidazoles (aqueous, 298°K). Positional reactivities of imidazole and 1-methylimidazole decreased in the order 5 > 4 > 2. The 5-position of 2-methylimidazole was the most reactive site.

Australian Journal of Chemistry published new progress about Bromination kinetics. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Name: 5-Bromo-1-methyl-1H-imidazole.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

In 2019,Journal of Applied Laboratory Medicine included an article by Bevins, Nicholas J.; Hubbard, Jacqueline A.; Fitzgerald, Robert L.; Kelner, Michael J.. HPLC of Formula: 58-85-5. The article was titled 《A dilution method to mitigate biotin interference in cardiac troponin T testing》. The information in the text is summarized as follows:

Background: Oral biotin supplementation is known to interfere with biotin-streptavidin-based immunoassays, including Roche’s fifth-generation cardiac troponin T (cTnT) assay, which plays a critical role in the diagnosis of myocardial infarction (MI). The utility of dilution, a quick and easy method to detect and remove interferences, has not been published for biotin interference. Methods: Concentrations of cTnT were measured in pooled serum from clin. samples. Serum samples were supplemented with biotin to known concentrations, then cTnT concentrations were remeasured to assess for biotin interference. Samples were then diluted to assess for effective removal of biotin interference. Results: At cTnT values near the critical reporting range for our institution (100 ng/L) we observed significant interference in measured values with added biotin concentrations above 50 ng/mL. In specimens without added biotin, autodilution at a 1:10 ratio yielded a mean 157% capture of measured cTnT, precluding the use of autodilution for detecting and mitigating biotin interference. A 1:10 dilution with serum containing 20-30 ng/L cTnT yielded a mean capture of 107%, which was suitable for detecting underlying biotin interference in supplemented samples. Conclusions: Biotin interference, at supraphysiol. concentrations, may create an artifactual reduction in measured cTnT to levels that could lead to delayed detection of an MI. Dilution with serum of known cTnT concentration of 20-30 ng/L is a fast and effective method to mitigate the anal. consequences of biotin interference. In addition to this study using 5-((3aS,4S,6aR)-2-Oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanoic acid, there are many other studies that have used 5-((3aS,4S,6aR)-2-Oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanoic acid(cas: 58-85-5HPLC of Formula: 58-85-5) was used in this study.

5-((3aS,4S,6aR)-2-Oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanoic acid(cas: 58-85-5) may be used to elute proteins from avidin/streptavidin resins. It has been used for culturing of oligodendrocytes.HPLC of Formula: 58-85-5 And it has been used for blocking endogenous biotin during immunohistology procedures.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Reference of 17325-26-7, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 17325-26-7 as follows.

Synthesis of (1S,2R) and (1R,2S)-methyl-1-(2-(2-(4-chlorophenyl)-2′-oxospiro [cyclopropane-1,3′-indoline]-1′-yl)ethyl)-1H-imidazole-4-carboxylate To a solution of methyl-imidazole-4-carboxylate (100 mg, 0.2 mmol) in 1 mL of anhydrous DMF was added NaH (60% disp.) (8.8 mg, 0.22 mmol) at room temperature. The reaction mixture was stirred for 1 hour at that temperature. To the mixture was added a solution of racemic (1R,2S) and (1S,2R)-1′-(2-bromoethyl)-2-(4-chlorophenyl)spiro[cyclopropane-1,3′-indolin]-2′-one (75.2 mg, 0.2 mmol) in 1 mL of DMF. The reaction was stirred at room temperature for 14 hours and then concentrated under reduced pressure. The residue was dissolved in EtOAc and washed with saturated aqueous NaHCO3. The layers were separated and the aqueous layer was extracted with EtOAc. The organic layers were combined and washed with brine, dried over anhydrous Na2SO4, filtered and concentrated in vacuo to give the title compound as white solid (30 mg, 35%). LC/MS m/e calcd. for C23H20ClN3O3: 421, observed (M+H)+: 422.3.

According to the analysis of related databases, 17325-26-7, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Chen, Li; Feng, Lichun; He, Yun; Huang, Mengwei; Yun, Hongying; US2011/144106; (2011); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem