Category: thiazole

Establishment of an oligoasthenospermia mouse model based on TAp73 gene suppression was written by Liu, Hong-Juan;Deng, Meng-Yun;Zhu, Yan-Yan;Wu, De-Ling;Tong, Xiao-Hui;Li, Li;Wang, Lei;Xu, Fei;Wang, Tong-Sheng. And the article was included in Animal Models and Experimental Medicine in 2021.Category: thiazole The following contents are mentioned in the article:

Oligoasthenospermia is one of the main causes of male infertility. Researchers usually use chem. drugs to directly damage germ cells to prep oligoasthenospermia models, which disregards the adhesion and migration between spermatogenic cells and Sertoli cells. TAp73 is a critical regulator of the adhesin of germ cell; thus, we sought to explore a novel oligoasthenospermia model based on TAp73 gene suppression. Mice in the Pifithrin-α group were injected i.p. with 2.5 mg/kg Pifithrin-α (TAp73 inhibitor) daily for 30 consecutive days. Reproductive hormone levels and epididymal sperm quality, as well as the network morphologyof Sertoli cells were tested. Sperm d, motility, and the relative protein and mRNA expression of TAp73 and Nectin 2 were obviously decreased in the Pifithrin-α group compared with the normal control group. No significant distinction was observed in the relative mRNA and protein expression of ZO-1. Furthermore, the tight junctions (TJs) and apical ectoplasmic specialization (ES) were destroyed in the Pifithrin-α group. The above indicate that we successfully established a new oligoasthenospermia mouse model. This study provides a foundation for further exploration of the roles of TAp73 genes during spermatogenesis and provides new research objects for further oligospermia research and future drug discovery. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Category: thiazole).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Synthesis, Properties, and Solar Cell Performance of Poly(4-(p-alkoxystyryl)thiazole)s was written by Jaeger, Jakob;Schraff, Sandra;Pammer, Frank. And the article was included in Macromolecular Chemistry and Physics in 2018.Safety of 5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide The following contents are mentioned in the article:

Polythiazoles (PvTzs) featuring conjugated styryl sidechains equipped with different solubilizing p-alkoxy-groups (-OR, R = n-octyl, n-dodecyl, 2-ethylhexyl, 2-hexyldecyl) is prepared by Negishi-coupling polycondensation. Soluble material with number-average mol. weights of up to M_n = 8.5 kDa (polydispersity (PDI) = 1.3, d.p. (DPn) ≈ 20) is obtained, with a head-to-tail content of the PvTzs of ≈77%, as estimated from comparison with reference polymers. The polymers exhibit optical absorption properties similar to their polythiophene analogs, while their electrochem. characterization shows a significant stabilization of their frontier orbital levels. Fluorescence measurements indicate that upon excitation of the electron rich alkoxystyryl side-chains charge transfer onto the more electron deficient polythiazole backbone occurs. This finding is corroborated by d. functional theory (DFT) calculations on oligomeric model systems, which also consistently reproduce the optical properties observed for the polymers. The potential of these materials for applications in organic electronics can be demonstrated by their use as donor materials in organic photovoltaic cells, which exhibit higher open circuit voltages (V_OC, up to 0.86 V) than P3HT- or analogous polythiophene-based cells (V_OC = 0.5-0.6 V). This study involved multiple reactions and reactants, such as 5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide (cas: 79247-77-1Safety of 5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide).

5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide (cas: 79247-77-1) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Safety of 5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

TP53 upregulates α-smooth muscle actin expression in tamoxifen-resistant breast cancer cells was written by Kim, Sangmin;You, Daeun;Jeong, Yisun;Yu, Jonghan;Kim, Seok Won;Nam, Seok Jin;Lee, Jeong Eon. And the article was included in Oncology Reports in 2019.Category: thiazole The following contents are mentioned in the article:

In a previous study, we reported that α-smooth muscle actin (α-SMA), one of the mesenchymal marker proteins, is highly expressed in tamoxifen-resistant breast cancer (TamR) cells. However, the exact mechanism of α-SMA expression in TamR cells is not fully understood. Here, we investigated the effect of TP53 on α-SMA expression in breast cancer cells. The levels of α-SMA mRNA and protein expression were analyzed by real-time PCR and western blotting, resp. In estrogen receptor-pos. [ER(+)] breast cancer patients, aberrant α-SMA expression was found to be associated with a poor prognosis. The level of α-SMA expression was significantly increased in established TamR cells compared to tamoxifen-sensitive (TamS) cells. To verify the regulatory mechanism of α-SMA expression, we analyzed diverse kinase activities between TamS and TamR cells. The activity of TP53 was markedly increased in the TamR cells. When TamS cells were treated with TP53 activator, Nutlin3 (Nut3), α-SMA expression was increased in the TamS cells. In addition, α-SMA expression was significantly increased by TP53 overexpression in breast cancer cells. On the contrary, the basal level of α-SMA expression was decreased by the TP53 inhibitor, pifithrin-α (PFT-α). Taken together, we demonstrated that α-SMA expression is regulated by TP53 activity in TamR cells. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Category: thiazole).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Dopamine-loaded lipid based nanocarriers for intranasal administration of the neurotransmitter: A comparative study was written by Trapani, Adriana;De Giglio, Elvira;Cometa, Stefania;Bonifacio, Maria Addolorata;Dazzi, Laura;Di Gioia, Sante;Hossain, Niamat Md;Pellitteri, Rosalia;Antimisiaris, Sophia G.;Conese, Massimo. And the article was included in European Journal of Pharmaceutics and Biopharmaceutics in 2021.Name: 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one The following contents are mentioned in the article:

Both dopamine (DA) loaded Solid Lipid Nanoparticles (SLN) and liposomes (Lip), designed for intranasal administration of the neurotransmitter as an innovative Parkinson disease treatment, were already characterized in vitro in some extent by us (Trapani et al., 2018a and Cometa et al., 2020, resp.). Herein, to gain insight into the structure of SLN, XPS Anal. was carried out and DA-SLN (SLN 1) were found to exhibit high amounts of the neurotransmitter on the surface, whereas the external side of Glycol Chitosan (GCS) containing SLN (SLN 2) possessed only few amounts However, SLN 2 were characterized by the highest encapsulation DA efficiency (i.e., 81%). Furthermore, in view of intranasal administration, mucoadhesion tests in vitro were also conducted for SLN and Lip formulations, evidencing high muchoadesive effect exerted by SLN 2. Concerning ex-vivo studies, SLN and Lip were found to be safe for Olfactory Ensheathing Cells and fluorescent SLN 2 were taken up in a dose-dependent manner reaching the 100% of pos. cells, while Lip 2 (chitosan-glutathione-coated) were internalised by 70% OECs with six-times more lipid concentration Hence, SLN 2 formulation containing DA and GCS may constitute interesting formulations for further studies and promising dosage form for non-invasive nose-to-brain neurotransmitter delivery. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Name: 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Name: 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Bromination-induced spirocyclization of rhodamine dyes affording a FRET-based ratiometric fluorescent probe for visualization of hypobromous acid (HOBr) in live cells and zebrafish was written by Wu, Lei;Shi, Yongqin;Yu, Hanjie;Zhang, Jianjian;Li, Zheng;Yang, Xiao-Feng. And the article was included in Sensors and Actuators, B: Chemical in 2021.HPLC of Formula: 38215-36-0 The following contents are mentioned in the article:

Hypobromous acid (HOBr) has been implicated in many physiol. and pathol. conditions. Therefore, real-time monitoring of HOBr fluctuations in biosystem plays a key role for understanding pathophysiol. processes. To date, it remains a challenge to design fluorescent probes specific toward HOBr, because HOBr and HOCl have similar chem. properties and the former has a relatively lower concentration in comparison with the former in living system. Herein, a Forster resonance energy transfer (FRET)-based ratiometric fluorescent HOBr probe (Cou-RhB) was developed. The probe consists of a coumarin donor and a rhodamine acceptor. Upon treatment of Cou-RhB with HOBr, the electrophilic bromination of xanthene ring occurs, which shifts the equilibrium of rhodamine from the highly absorbing and fluorescent zwitterion form to the colorless and non-fluorescent spirolactone form, thus decreasing the FRET efficiency within the probe. The above reaction affords a large emission wavelength shift (ca. 89 nm), and ratiometric sensing of HOBr can be realized by measuring the ratio of coumarin- to rhodamine-type intensities (I₄₉₁/I₅₈₀). Cou-RhB responds to HOBr with a fast kinetics (∼ 10 s), high sensitivity and excellent specificity and has been applied for ratiometric imaging of HOBr inside live cells and zebrafish. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0HPLC of Formula: 38215-36-0).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.HPLC of Formula: 38215-36-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Ionic liquid-mediated delivery of a BCL-2 inhibitor for topical treatment of skin melanoma was written by Huda, Nurul Md;Deaguro, Isaac G.;Borrego, Edgar A.;Kumar, Raj;Islam, Tamanna;Afrin, Humayra;Varela-Ramirez, Armando;Aguilera, Renato J.;Tanner, Eden E. L.;Nurunnabi, Md. And the article was included in Journal of Controlled Release in 2022.Recommanded Product: 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one The following contents are mentioned in the article:

Skin melanoma is one of the most common cancer types in the United States and worldwide, and its incidence continues to grow. Primary skin melanoma can be removed surgically when feasible and if detected at an early stage. Anti-cancer drugs can be applied topically to treat skin cancer lesions and used as an adjunct to surgery to prevent the recurrence of tumor growth. We developed a topical formulation composed of Navitoclax (NAVI), a BCL-2 inhibitor that results in apoptosis, and an ionic liquid of choline octanoate (COA) to treat early-stage melanoma. NAVI is a small hydrophobic mol. that solubilizes at 20% (w/v) when dissolved in 50% COA. Although NAVI is a highly effective chemotherapeutic, it is equally thrombocytopenic. We found that COA-mediated topical delivery of NAVI enhanced its penetration into the skin and held the drug in the deeper skin layers for an extended period. Topical delivery of NAVI produced a higher cancer-cell killing efficacy than orally administrated NAVI. In vivo experiments in a mouse model of human melanoma-induced skin cancer confirmed the formulation′s effectiveness via an apoptotic mechanism without any significant skin irritation or systemic absorption of NAVI. Overall, this topical approach may provide a safe and effective option for better managing skin cancer in the clinic. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Recommanded Product: 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Recommanded Product: 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Rapid visualizing and pathological grading of bladder tumor tissues by simple nanodiagnostics was written by Liu, Hongxing;Mei, Chaoming;Deng, Xuanru;Lin, Weiqiang;He, Lizhen;Chen, Tianfeng. And the article was included in Biomaterials in 2021.Related Products of 38215-36-0 The following contents are mentioned in the article:

Developing a tissue diagnosis technol. to avoid the complicated processes and the usage of expensive reagents while achieving rapid pathol. grading diagnosis to provide a better strategy for clin. treatment is an important strategy of tumor diagnose. Herein, we selected the integrin αvβ3 as target based on the anal. of clin. data, and then designed a stable and cancer-targeted selenium nanosystem (RGD@SeNPs) by using RGD polypeptide as the targeting modifier. In vitro experiments showed that RGD@SeNPs could specifically recognized tumor cells, especially in co-culture cells model. The RGD@SeNPs can be used for clin. samples staining without the use of primary and secondary antibody. Fluorescence difference of the tissue specimens staining with RGD@SeNPs could be used to distinguish normal tissues and tumor tissues or estimate different pathol. grades of cancer at tissue level. 132 clin. tumor specimens with three types of tumor and 76 non-tumor specimens were examined which verified that the nanoparticles could specific and sensitive distinguish tumor tissue from normal tissue with a specificity of 92% and sensitivity of 96%. These results demonstrate the potential of cancer-targeted RGD@SeNPs as translational nanodiagnostics for rapid visualizing and pathol. grading of bladder tumor tissues in clin. specimens. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Related Products of 38215-36-0).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Related Products of 38215-36-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

12,13-Aziridinyl Epothilones. Stereoselective Synthesis of Trisubstituted Olefinic Bonds from Methyl Ketones and Heteroaromatic Phosphonates and Design, Synthesis, and Biological Evaluation of Potent Antitumor Agents was written by Nicolaou, K. C.;Rhoades, Derek;Wang, Yanping;Bai, Ruoli;Hamel, Ernest;Aujay, Monette;Sandoval, Joseph;Gavrilyuk, Julia. And the article was included in Journal of the American Chemical Society in 2017.Name: 4-(Bromomethyl)-2-methylthiazole The following contents are mentioned in the article:

The synthesis and biol. evaluation of a series of 12,13-aziridinyl epothilone B analogs is described. These compounds were accessed by a practical, general process that involved a 12,13-olefinic Me ketone as a starting material obtained by ozonolytic cleavage of epothilone B followed by tungsten-induced deoxygenation of the epoxide moiety. The attachment of the aziridine structural motif was achieved by application of the Ess-Kurti-Falck aziridination, while the heterocyclic side chains were introduced via stereoselective phosphonate-based olefinations. In order to ensure high (E) selectivities for the latter reaction for electron-rich heterocycles, it became necessary to develop and apply an unprecedented modification of the venerable Horner-Wadsworth-Emmons reaction, employing 2-fluoroethoxyphosphonates that may prove to be of general value in organic synthesis. These studies resulted in the discovery of some of the most potent epothilones reported to date. Equipped with functional groups to accommodate modern drug delivery technologies, some of these compounds exhibited picomolar potencies that qualify them as payloads for antibody drug conjugates (ADCs), while a number of them revealed impressive activities against drug resistant human cancer cells, making them desirable for potential medical applications. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Name: 4-(Bromomethyl)-2-methylthiazole).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Name: 4-(Bromomethyl)-2-methylthiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Farnesoid X receptor functions in cervical cancer via the p14^ARF-mouse double minute 2-p53 pathway was written by Huang, Xiaohua;Wang, Bin;Shen, Huimin;Huang, Danmei;Shi, Ganggang. And the article was included in Molecular Biology Reports in 2022.Computed Properties of C16H19BrN2OS The following contents are mentioned in the article:

Cervical cancer is the second most common cancer among women living in developing countries. Farnesoid X receptor (FXR) is a member of the nuclear receptor family, which regulates the development and proliferation of cancer. However, the role of and mol. mechanism by which FXR acts in cervical cancer are still unknown. The relationship between FXR and the proliferation of cervical cancer cell lines was detected by MTT and colony formation assays. Immunohistochem. was used to detect the expression of FXR in cervical cancer tissue slides. Western blotting was used to detect the expression of p14ARF, mouse double minute 2 (MDM2) and p53 when FXR was overexpressed or siRNA was applied. Western blotting was used to detect the expression of MDM2 and p53 when pifithrin-α (PFT-α) was applied. FXR activation inhibited the proliferation of cervical cancer cell lines. FXR was significantly decreased in cervical squamous cell carcinoma, which was correlated with TNM stage, but not with metastasis. Overexpression of FXR activated the p14ARF-MDM2-p53 pathway. As a p53 inhibitor, PFT-α increased MDM2 in Lenti-vector cells, but had no effect on MDM2 in Lenti-FXR cells. FXR inhibits cervical cancer by upregulating the p14ARF-MDM2-p53 pathway. Activation of FXR may be a potential strategy for the treatment of cervical cancer. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Computed Properties of C16H19BrN2OS).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Computed Properties of C16H19BrN2OS

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

PFT-α inhibits gallid alpha herpesvirus 1 replication by repressing host nucleotide metabolism and ATP synthesis was written by Xu, Li;Wang, Zhitao;Chen, Zhijie;Cui, Lu;Liu, Zheyi;Liang, Yumeng;Li, Xuefeng;Zhang, Yanhui;Liu, Shengwang;Li, Hai. And the article was included in Veterinary Microbiology in 2022.Recommanded Product: 63208-82-2 The following contents are mentioned in the article:

Therapeutics targeting virus-host interactions have been considered promising strategies for treating herpesvirus infection. Our previous study on avian infectious laryngotracheitis virus (ILTV), an avian herpesvirus economically important to the poultry industry worldwide, identified the small mol. Pifithrin-α (PFT-α) as a potential therapeutic agent. However, the underlying mechanisms of its antiviral function remain largely unknown. Using the ILTV-permissive chicken cell line LMH as the model, we found that PFT-α effectively suppressed the transcription and genome replication of ILTV and greatly reduced the level of infectious virions. Genome-wide transcriptome anal. revealed extensive repression of the metabolic processes of infected cells by PFT-α administration. Further metabolome assays of ILTV-infected cells using liquid chromatog. coupled with mass spectrometry suggest host nucleotide metabolism and ATP synthesis as the key targets of PFT-α treatment during its repression of ILTV replication, which was exptl. supported by the reduced transcription of many key enzymes essential to nucleotide metabolism and ATP synthesis. The present study provides insights into the mechanisms by which PFT-α inhibits ILTV infection, which may increase the probability of successful clin. application of this mol. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Recommanded Product: 63208-82-2).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Recommanded Product: 63208-82-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica