Day: November 28, 2022

Localized therapy using anti-PD-L1 anchored and NIR-responsive hollow gold nanoshell (HGNS) loaded with doxorubicin (DOX) for the treatment of locally advanced melanoma was written by Banstola, Asmita;Poudel, Kishwor;Emami, Fakhrossadat;Ku, Sae Kwang;Jeong, Jee-Heon;Kim, Jong Oh;Yook, Simmyung. And the article was included in Nanomedicine (New York, NY, United States) in 2021.Computed Properties of C20H18N2O2S The following contents are mentioned in the article:

Drug resistance and inefficient localization of chemotherapeutic agent limit the current treatment strategy in locally advanced melanoma (MEL), accounting to the 10-yr survival rate from 24% to 68%. In this study we constructed anti-PD-L1 conjugated and doxorubicin loaded hollow gold nanoshell (T-HGNS-DOX) for targeted and localized chemo-photothermal therapy of MEL by the conjugation of LA-PEG-anti-PD-L1 antibody and short PEG chain on the surface of HGNS-DOX. Near IR (NIR) as well as pH dependent drug release profile was observed Significant uptake of DOX following NIR due to high PD-L1 receptors resulted in pronounced anticancer effect of T-HGNS-DOX. Following intratumoral administration, maximum nanoparticles retention with the significant reduction in tumor growth was observed as a result of elevated apoptosis marker (cleaved caspase-3, cleaved PARP) as well as downregulation of proliferative (Ki-67) and angiogenesis marker (CD31). Cumulatively, our system avoids the systemic toxicities of the nanosystem thereby providing maximum chemotherapeutic retention in tumor. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Computed Properties of C20H18N2O2S).

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).Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Computed Properties of C20H18N2O2S

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

Radiosynthesis and preliminary evaluation of 4-[¹⁸F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1 was written by Yamasaki, Tomoteru;Fujinaga, Masayuki;Yoshida, Yuichiro;Kumata, Katsushi;Yui, Joji;Kawamura, Kazunori;Hatori, Akiko;Fukumura, Toshimitsu;Zhang, Ming-Rong. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Category: thiazole The following contents are mentioned in the article:

The purpose of this study was to develop 4-[¹⁸F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([¹⁸F]I) as a new PET ligand for imaging metabotropic glutamate receptor subtype 1 (mGluR1). [¹⁸F]I was synthesized by [¹⁸F]fluorination of a novel nitro precursor with [¹⁸F]KF in the presence of Kryptofix 222. At the end of synthesis, 429-936 MBq (n = 8) of [¹⁸F]I was obtained with >99% radiochem. purity and 204-559 GBq/μmol specific activity starting from 6.7 to 13.0 GBq of [¹⁸F]F^–. The brain distribution of [¹⁸F]I was determined by the in vitro and ex vivo autoradiog. using rat brain sections. The in vitro and in vivo specific binding of [¹⁸F]I to mGluR1 was detected in the cerebellum, thalamus, hippocampus, and striatum. These results suggest that [¹⁸F]I is a promising PET ligand for the in vivo evaluation of mGluR1. This study involved multiple reactions and reactants, such as 4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2Category: thiazole).

4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. 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

Genetic depletion of p53 attenuates cocaine-induced hepatotoxicity in mice was written by Mai, Huynh Nhu;Sharma, Garima;Sharma, Naveen;Shin, Eun-Joo;Kim, Dae-Joong;Pham, Duc Toan;Trinh, Quynh Dieu;Jang, Choon-Gon;Nah, Seung Yeol;Jeong, Ji Hoon;Kim, Hyoung-Chun. And the article was included in Biochimie in 2019.Category: thiazole The following contents are mentioned in the article:

We found that the pharmacol. (i.e. pifithrin-a) and genetic (i.e. p53 knockout) inhibition of p53 significantly attenuates cocaine-induced hepatotoxicity. Cocaine treatment increased alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in the serum of mice, signifying hepatic damage. Consistently, these increases were attenuated by inhibition of p53, implying protection against cocaine-induced hepatic damage. In addition, cocaine treatment significantly increased PKCd, cleaved PKCd and p53 levels in the liver of WT mice. These increases were followed by the interaction between p53 and PKCd, and pro-apoptotic consequences (i.e., cytosolic release of cytochrome c, activation of caspase-3, increase in Bax level and decreases in Bcl-2 and Bcl-xL levels). These changes were attenuated by p53 depletion, reflecting that the critical role of PKCd in p53-mediated apoptotic potentials. Combined, our results suggest that the inhibition of p53 is important for protection against oxidative burdens, pro-apoptotic events, and hepatic degeneration induced by cocaine. 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. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. 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.Category: thiazole

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

Development of N-[4-[6-(Isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methyl-4-[¹¹C]methylbenzamide for Positron Emission Tomography Imaging of Metabotropic Glutamate 1 Receptor in Monkey Brain was written by Fujinaga, Masayuki;Yamasaki, Tomoteru;Maeda, Jun;Yui, Joji;Xie, Lin;Nagai, Yuji;Nengaki, Nobuki;Hatori, Akiko;Kumata, Katsushi;Kawamura, Kazunori;Zhang, Ming-Rong. And the article was included in Journal of Medicinal Chemistry in 2012.COA of Formula: C8H7ClN4S The following contents are mentioned in the article:

Three novel 4-substituted benzamides have been synthesized as potential ligands for the positron emission tomog. (PET) imaging of metabotropic glutamate 1 (mGlu1) receptor in the brain. Of these compounds, N-(4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-N,4-dimethylbenzamide (4) exhibited the highest binding affinity (K_i = 13.6 nM) for mGlu1 and was subsequently labeled with carbon-11. In vitro autoradiog. using rat brain sections showed that [¹¹C]4 binding was consistent with the distribution of mGlu1, with high specific binding in the cerebellum and thalamus. PET studies with [¹¹C]4 in monkey showed a high brain uptake and a kinetic profile suitable for quant. anal. Pretreatment with a mGlu1-selective ligand 16 largely decreased the brain uptake, indicating high in vivo specific binding of [¹¹C]4 to mGlu1. In metabolite anal., only unchanged [¹¹C]4 was found in the brain. [¹¹C]4 is a useful PET ligand for the imaging and quant. anal. of mGlu1 in monkey brain and merits further evaluation in humans. This study involved multiple reactions and reactants, such as 4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2COA of Formula: C8H7ClN4S).

4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2) 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. 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.COA of Formula: C8H7ClN4S

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

Phenyl thiazolyl urea and carbamate derivatives as new inhibitors of bacterial cell-wall biosynthesis was written by Francisco, Gerardo D.;Li, Zhong;Albright, J. Donald;Eudy, Nancy H.;Katz, Alan H.;Petersen, Peter J.;Labthavikul, Pornpen;Singh, Guy;Yang, Youjun;Rasmussen, Beth A.;Lin, Yang-I.;Mansour, Tarek S.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2004.Product Details of 303994-99-2 The following contents are mentioned in the article:

Over 50 Ph thiazolyl urea and carbamate derivatives were synthesized for evaluation as new inhibitors of bacterial cell-wall biosynthesis. Many of them demonstrated good activity against MurA and MurB and gram-pos. bacteria including MRSA, VRE and PRSP. (3,4-Difluorophenyl)(5-cyanothiazolyl)urea with clog P of 2.64 demonstrated antibacterial activity against both gram-pos. and gram-neg. bacteria. The activity of these (phenyl)(thiazolyl)urea and (thiazolyl)carbamate derivatives was also compared to 3-[[[(3,4-dichlorophenyl)amino]carbonyl]amino]-2-thiophenecarboxylic acid Me ester, 5-[[[(3,4-dichlorophenyl)amino]carbonyl]amino]-1-methyl-1H-pyrazole-4-carboxylic acid Me ester, N-(3,4-dichlorophenyl)-N‘-(2-pyridinyl)urea, and some other compounds Antibacterial activity was screened against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococus (VRE), penicillin-resistant Streptococcus pneumoniae (PRSP). Mol. modeling studies were carried out to explore binding preferences within this compound series in the MurB structure. This study involved multiple reactions and reactants, such as 2-Amino-4-(tert-butyl)thiazole-5-carbonitrile (cas: 303994-99-2Product Details of 303994-99-2).

2-Amino-4-(tert-butyl)thiazole-5-carbonitrile (cas: 303994-99-2) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). 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.Product Details of 303994-99-2

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

Fucoxanthin attenuates doxorubicin-induced cardiotoxicity via anti-oxidant and anti-apoptotic mechanisms associated with p38, JNK and p53 pathways was written by Zhao, Yu-Qin;Zhang, Lun;Zhao, Guo-Xu;Chen, Yin;Sun, Kun-Lai;Wang, Bin. And the article was included in Journal of Functional Foods in 2019.Related Products of 63208-82-2 The following contents are mentioned in the article:

Doxorubicin (DOX) is a commonly used anthracycline in treatments of leukemia, lymphoma and breast cancer in humans and has been limited by its cardiotoxicity, which is manifested congestive heart failure in the worst condition. The present study showed that the marine carotenoid of fucoxanthin could exert cardioprotective effect against the DOX-induced injury in ICR mice. And then, the protective effects and mechanisms of fucoxanthin on DOX-induced injury of neonatal rat cardiomyocytes were investigated. The results demonstrated that fucoxanthin significantly reduced mice toxic death triggered by DOX. The protective effects were also showed by the suppression of apoptotic cell death in cardiomyocytes. Further study revealed that fucoxanthin-produced suppression of MAPK activated by DOX was involved in the cardioprotection. The findings confirmed the cardioprotective effect of fucoxanthin against DOX-induced cardiotoxicity by protecting myocardial cells from lipid peroxidation and apoptosis, which would likely result in an increased therapeutic window of DOX in cancer therapy. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Related Products of 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. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. 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.Related Products of 63208-82-2

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

Bioadhesive metal-phenolic nanoparticles for enhanced NIR imaging-guided locoregional photothermal/antiangiogenic therapy was written by Wang, Xiuxia;Li, Hongyu;Meng, Fanling;Luo, Liang. And the article was included in Journal of Materials Chemistry B in 2021.HPLC of Formula: 38215-36-0 The following contents are mentioned in the article:

Locoregional drug delivery has emerged as a promising solution to the problems associated with i.v. administered antitumor agents, such as systemic toxicity and insufficient drug accumulation at tumor sites. Herein, we have developed an adhesive nanoparticle (NP)-based drug delivery system, using natural bioadhesive tannic acid (TA) and metal ions (Fe³⁺), for locoregional photothermal and antiangiogenic synergistic cancer therapy. In this study, a new near-IR (NIR) photothermal agent indocyanine green (IR820) and an antiangiogenic agent sorafenib (SRF) were co-encapsulated in a TA-Fe complex (SIF@TA-Fe). The SIF@TA-Fe NPs exhibited super adhesion, antiangiogenesis, and efficient cellular uptake. Moreover, SIF@TA-Fe NPs showed a synergistic antitumor effect in vivo, including high tumor inhibition rate, excellent survival extension, and low risk of recurrence, resulting from the prolonged retention of the NPs in the tumor. Thus, this adhesive SIF@TA-Fe NP-based therapeutic system provides a promising approach for locoregional drug delivery of combined cancer therapy. 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. 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.HPLC of Formula: 38215-36-0

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

Robust genome editing in adult vascular endothelium by nanoparticle delivery of CRISPR-Cas9 plasmid DNA was written by Zhang, Xianming;Jin, Hua;Huang, Xiaojia;Chaurasiya, Birendra;Dong, Daoyin;Shanley, Thomas P.;Zhao, You-Yang. And the article was included in Cell Reports in 2022.Safety of 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one The following contents are mentioned in the article:

Vascular endothelium plays a crucial role in vascular homeostasis and tissue fluid balance. To target endothelium for robust genome editing, we developed poly(ethylene glycol) Me ether-block-poly(lactide-co-glycolide) (PEG-b-PLGA) copolymer-based nanoparticle formulated with polyethyleneimine. A single i.v. administration of mixture of nanoparticles and plasmid DNA expressing Cas9 controlled by CDH5 promoter and guide RNA (U6 promoter) induced highly efficient genome editing in endothelial cells (ECs) of the vasculatures, including lung, heart, aorta, and peripheral vessels in adult mice. Western blotting and immunofluorescent staining demonstrated an ∼80% decrease of protein expression selectively in ECs, resulting in a phenotype similar to that of genetic knockout mice. Nanoparticle delivery of plasmid DNA could induce genome editing of two genes or genome editing and transgene expression in ECs simultaneously. Thus, nanoparticle delivery of plasmid DNA is a powerful tool to rapidly and efficiently alter expression of gene(s) in ECs for cardiovascular research and potential gene therapy. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Safety of 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. 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.Safety of 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one

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

Synthesis and Evaluation in Monkey of [¹⁸F]4-Fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([¹⁸F]FIMX): A Promising Radioligand for PET Imaging of Brain Metabotropic Glutamate Receptor 1 (mGluR1) was written by Xu, Rong;Zanotti-Fregonara, Paolo;Zoghbi, Sami S.;Gladding, Robert L.;Woock, Alicia E.;Innis, Robert B.;Pike, Victor W.. And the article was included in Journal of Medicinal Chemistry in 2013.Recommanded Product: 932738-80-2 The following contents are mentioned in the article:

We sought to develop a PET radioligand that would be useful for imaging human brain metabotropic subtype 1 receptors (mGluR1) in neuropsychiatric disorders and in drug development. 4-Fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)-thiazol-2-yl)-benzamide (FIMX) was identified as having favorable properties for development as a PET radioligand. We developed a method for preparing [¹⁸F]FIMX in useful radiochem. yield and in high specific activity from [¹⁸F]-fluoride ion and an N-Boc-protected (phenyl)aryliodonium salt precursor. In baseline experiments in the rhesus monkey, [¹⁸F]FIMX gave high brain radioactivity uptake, reflecting the expected distribution of mGluR1 with notably high uptake in cerebellum, which became 47% lower by 120 min after radioligand injection. Pharmacol. challenges demonstrated that a very high proportion of the radioactivity in monkey brain was bound specifically and reversibly to mGluR1. [¹⁸F]FIMX is concluded to be an effective PET radioligand for imaging mGluR1 in monkey brain and therefore merits further evaluation in human subjects. This study involved multiple reactions and reactants, such as 4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2Recommanded Product: 932738-80-2).

4-(6-Chloropyrimidin-4-yl)-N-methylthiazol-2-amine (cas: 932738-80-2) 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. 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.Recommanded Product: 932738-80-2

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

CX-5461 is a potent immunosuppressant which inhibits T cell-mediated alloimmunity via p53-DUSP5 was written by Pan, Guopin;Zhang, Jing;Han, Yu;Chen, Ye;Guo, Xiaosun;Cui, Xiaopei;Cheng, Mei;Gao, Haiqing;Wang, Jianli;Jiang, Fan. And the article was included in Pharmacological Research in 2022.Safety of 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide The following contents are mentioned in the article:

CX-5461 is a first-in-class selective RNA polymerase I inhibitor. Previously we found that CX-5461 had anti-inflammatory activities. In this study we characterized potential immunosuppressive effects of CX-5461 and explored the underlying mechanisms. Allogeneic skin transplantation model (BALB/c to C57BL/6 mice) and heterotopic heart transplantation model (F344 to Lewis rats) were used. We showed that CX-5461 was a potent inhibitor of alloimmunity which prevented acute allograft rejections. CX-5461 treatment was invariably associated with expansion of the regulatory T cell population. In vitro, CX-5461 inhibited agonists-induced T cell activation. CX-5461 consistently inhibited the expression of interferon-γ and interleukin – 2, key mediators of T cell-mediated alloimmunity. Mechanistically, CX-5461-induced immunosuppression was, at least partly, dependent on the p53-DUSP5 (dual-specificity phosphatase 5) axis and subsequent antagonism of the Erk1/2 mitogen-activated protein kinase pathway. In conclusion, our results suggest that CX-5461 is a promising candidate of a novel class of immunosuppressant which may be used as an alternative to the currently approved anti-rejection therapies. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Safety of 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Safety of 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide

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