Month: October 2022

Demine, Stephane; Garcia Ribeiro, Rita; Thevenet, Julien; Marselli, Lorella; Marchetti, Piero; Pattou, Francois; Kerr-Conte, Julie; Devoogdt, Nick; Eizirik, Decio L. published the artcile< A nanobody-based nuclear imaging tracer targeting dipeptidyl peptidase 6 to determine the mass of human beta cell grafts in mice>, Related Products of 128-09-6, the main research area is beta cell DPP6 nanobody nuclear imaging; Human islet imaging; PET; Pancreatic beta cell imaging; Pancreatic beta cells; SPECT; Type 1 diabetes.

Type 1 diabetes is characterised by a progressive decline in beta cell mass. This is also observed following implantation of pancreatic islet allografts, but there is no reliable information regarding the time course of beta cell loss. This is due to the limited availability of non-invasive pancreatic islet imaging techniques. We have previously described that dipeptidyl peptidase 6 (DPP6) is an alpha and beta cell-specific biomarker, and developed a camelid antibody (nanobody ‘4hD29’) against it. We demonstrated the possibility to detect DPP6-expressing cells by single-photon emission computed tomog. (SPECT)/ computed tomog. (CT), but the correlation between the number of cells grafted and the SPECT signal was not assessed. Here, we investigate whether the 4hD29 nanobody allows us to detect different amounts of human pancreatic islets implanted into immune-deficient mice. In addition, we also describe the adaptation of the probe for use with positron emission tomog. (PET). DPP6 expression was assessed in human samples using tissue arrays and immunohistochem. The effect of the 4hD29 nanobody on cell death and glucose-stimulated insulin secretion was measured in EndoC-βH1 cells and in human islets using Hoechst/propidium iodide staining and an anti-insulin ELISA, resp. We performed in vivo SPECT imaging on severe combined immunodeficient (SCID) mice transplanted with different amounts of EndoC-βH1 cells (2 x 106, 5 x 106 and 10 x 106 cells), human islets (1000 and 3000) or pancreatic exocrine tissue using 99mTc-labeled 4hD29 nanobody. This DPP6 nanobody was also conjugated to N-chlorosuccinimide (NCS)-1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), radiolabeled with either 67Ga (SPECT) or 68Ga (PET) and used in a proof-of-principle experiment to detect DPP6-expressing cells (Kelly neuroblastoma) grafted in SCID mice. The DPP6 protein is mainly expressed in pancreatic islets. Importantly, the anti-DPP6 nanobody 4hD29 allows non-invasive detection of high amounts of EndoC-βH1 cells or human islets grafted in immunodeficient mice. This suggests that the probe must be further improved to detect lower numbers of islet cells. The 4hD29 nanobody neither affected beta cell viability nor altered insulin secretion in EndoC-βH1 cells and human islets. The conversion of 4hD29 nanobody into a PET probe was successful and did not alter its specificity. These findings suggest that the anti-DPP6 4hD29 nanobody may become a useful tool for the quantification of human islet grafts in mice and, pending future development, islet mass in individuals with diabetes.

Diabetologia published new progress about Allotransplantation. 128-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C4H4ClNO2, Related Products of 128-09-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Washburn, Alex; Abdeen, Sanofar; Ovechkina, Yulia; Ray, Anne-Marie; Stevens, Mckayla; Chitre, Siddhi; Sivinski, Jared; Park, Yangshin; Johnson, James; Hoang, Quyen Q.; Chapman, Eli; Parish, Tanya; Johnson, Steven M. published the artcile< Dual-targeting GroEL/ES chaperonin and protein tyrosine phosphatase B (PtpB) inhibitors: A polypharmacology strategy for treating Mycobacterium tuberculosis infections>, Reference of 22952-32-5, the main research area is benzoxazolylphenyl phenylbenzoxazolyl sulfonamide preparation; inhibition GroEL ES chaperonin PtpB benzoxazolylphenyl phenylbenzoxazolyl sulfonamide; antimycobacterial activity toxicity benzoxazolylphenyl phenylbenzoxazolyl sulfonamide; Antibiotics; Chaperonin; GroEL; GroES; HSP10; HSP60; Molecular chaperone; Mycobacterium tuberculosis; Phosphatases; Polypharmacology; Proteostasis; Small molecule inhibitors.

Benzoxazolylphenyl sulfonamides I (R = Me, Ph, 2-thienyl, 2-FC6H4, 3-FC6H4, 4-FC6H4, 2-ClC6H4, 3-ClC6H4, 4-ClC6H4, 5-chloro-2-thienyl, 2-F3CC6H4, 3-F3CC6H4, 4-F3CC6H4, 3,4-Cl2C6H3, 4-F-3-F3CC6H3, 4-Cl-3-F3CC6H3, 4-Cl-3-O2NC6H3, 5-Cl-2-MeOC6H3, 2-MeC6H4, 3-MeC6H4, 4-MeC6H4, 4-EtC6H4, 4-H2C:CHC6H4, 2-MeOC6H4, 3-MeOC6H4, 4-MeOC6H4, 2-HOC6H4, 3-HOC6H4, 4-HOC6H4) and phenylbenzoxazolyl sulfonamides II (R = Me, Ph, 2-thienyl, 2-FC6H4, 3-FC6H4, 4-FC6H4, 2-ClC6H4, 3-ClC6H4, 4-ClC6H4, 5-chloro-2-thienyl, 2-F3CC6H4, 3-F3CC6H4, 4-F3CC6H4, 3,4-Cl2C6H3, 4-F-3-F3CC6H3, 4-Cl-3-F3CC6H3, 4-Cl-3-O2NC6H3, 5-Cl-2-MeOC6H3, 2-MeC6H4, 3-MeC6H4, 4-MeC6H4, 4-EtC6H4, 4-H2C:CHC6H4, 2-MeOC6H4, 3-MeOC6H4, 4-MeOC6H4, 2-HOC6H4, 3-HOC6H4, 4-HOC6H4) were prepared as dual inhibitors of GroEL/ES and the virulence factor protein tyrosine phosphatase B (PtpB) for the treatment of Mycobacterium tuberculosis infection at all stages of bacterial infection.

Bioorganic & Medicinal Chemistry Letters published new progress about Benzoxazoles Role: ADV (Adverse Effect, Including Toxicity), PAC (Pharmacological Activity), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Reference of 22952-32-5.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Yan, Jingling; Wang, Zhen; Gao, Lianxun; Ding, Mengxian published the artcile< Synthesis and properties of polyimides from isomeric bis(dicarboxylphenylthio)diphenyl sulfone dianhydrides>, Recommanded Product: 5-Chloroisobenzofuran-1,3-dione, the main research area is isomeric tetracarboxylic dianhydride polyimide polysulfone preparation property; permeability permselectivity oxygen nitrogen polyimide polysulfone.

4,4′-Bis(3,4-dicarboxyphenylthio)diphenyl sulfone dianhydride(4,4′-PTPSDA) and 4,4′-bis(2,3-dicarboxyphenylthio)diphenyl sulfone dianhydride(3,3′-PTPSDA) were synthesized from chlorophthalic anhydrides and bis(4-mercaptophenyl)sulfone. Their structures were determined via IR spectra, 1H NMR and elemental anal. A series of polyimides were prepared from isomeric PTPSDAs and aromatic diamines in 1-methyl-2-pyrrolidinone (NMP) via the conventional two-step method. Polyimides based on 4,4′-PTPSDA and 3,3′-PTPSDA have good solubility in polar aprotic solvents and phenols. The 5% weight-loss temperatures of isomeric polyimides were near 500 °C in N2. DMTA and DSC analyses indicated that the glass-transition temperatures of polyimides from 3,3′-PTPSDA are higher than those of polyimides from 4,4′-PTPSDA. The wide-angle X-ray diffraction showed that all polyimides are amorphous. The polyimides from 3,3′-PTPSDA showed higher permeability but lower permselectivity compared with those from 4,4′-PTPSDA.

Polymer published new progress about Elongation at break. 118-45-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H3ClO3, Recommanded Product: 5-Chloroisobenzofuran-1,3-dione.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Li, Yuanheng; Sun, Lilan; Yang, Taoyi; Jiao, Wenxuan; Tang, Jingshu; Huang, Xiaomin; Huang, Zongze; Meng, Ying; Luo, Laichun; Wang, Xintong; Bian, Xiling; Zhang, Fang; Wang, KeWei; Sun, Qi published the artcile< Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice>, Application of C7H8ClN, the main research area is thiazolo pyrimidinone preparation nicotinic acetylcholine receptor allosteric modulator SAR.

A series of novel thiazolo[4,5-d]pyrimidin-7(6H)-ones were designed, synthesized, and evaluated as the type I pos. allosteric modulators of human α7 nAChR expressed in Xenopus oocytes by a two-electrode voltage clamp. The structure-activity relationship anal. identified the compound I as a potent and efficacious PAM with the maximum activation effect of the α7 current of over 1633% in the presence of acetylcholine (100 μM) and an EC50 = 1.26 μM. It is highly specific to α7 nAChR over other subtypes of nAChR, 5-HT3A, NMDA, and GABAA receptors. Compound I showed an elimination half-life of 10.8 ± 1.5 h for 3 mg/kg, i.v., and 7.4 ± 1.1 h for 60 mg/kg, i.g. in rat. It also exhibited sufficient blood-brain barrier penetration with no significant effect on hERG channel. Most importantly, compound I dose-dependently (0.1-1 mg/kg, i.p.) reversed the prepulse inhibition deficit induced by MK-801 in the mouse schizophrenia model.

Journal of Medicinal Chemistry published new progress about 5-HT3A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 29027-20-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H8ClN, Application of C7H8ClN.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Atli Sekeroglu, Zulal; Gediz Erturk, Aliye; Kontas Yedier, Seval; Sekeroglu, Vedat published the artcile< In vitro cytogenetic activity of 3-amino-4-[4-(dimethylamino)phenyl]-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxide>, Reference of 6055-19-2, the main research area is amino dimethylamino phenyl dihydro thiadiazole dioxide cytogenetic activity; 1,2,5-Thiadiazole 1,1-dioxide; chromosome aberrations; cytotoxicity; lymphocytes; micronucleus.

In a previous study, 3-amino-4-[4-(dimethylamino)phenyl]-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxide (DPTD), which is five-membered cyclosulfamide, was synthesized and structurally characterized. The aim of this study was to investigate the cytotoxic and genotoxic effects of DPTD on cultured human lymphocytes in the presence and absence of a metabolic activation system (S9 mix). The cytotoxicity and genotoxicity of DPTD in human peripheral blood lymphocytes were examined in vitro by using chromosomal aberration (CA) and micronucleus (MN) tests. Mitomycin-C (MMC) for cultures without S9 mix and cyclophosphamide monohydrate (CP) for cultures with S9 mix were used as pos. controls. The cultures were treated with DPTD (45, 90, and 180μg/mL) in the absence and presence of S9 mix. The cells were also co-treated with DPTD together with MMC or CP. DPTD showed cytotoxic activity due to decreases in mitotic index (MI) and nuclear division index (NDI) in the absence and presence of S9 mix. DPTD also increased the CAs, aberrant cells with CAs and MN values in cultures with and without S9 mix. When DPTD and MMC or CP were used together, lower MI and NDI values and higher CA and MN values were found than those DPTD treated alone. Both DPTD and its metabolites have cytotoxic, cytostatic and genotoxic potential on human peripheral blood lymphocyte cultures under the exptl. conditions. Furthermore, co-treatment of DPTD and MMC or CP can cause more cytotoxicity and genotoxicity. Our results indicated that the use of DPTD with other chemotherapeutic drugs may display more effective results.

Drug and Chemical Toxicology (1977) published new progress about Genotoxicity. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Reference of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Nakahara, Takako; Sakaeda, Toshiyuki; Nakamura, Tsutomu; Tamura, Takao; Nishioka, Chiharu; Aoyama, Nobuo; Okamura, Noboru; Shirakawa, Toshiro; Gotoh, Akinobu; Kamigaki, Takashi; Ohno, Masakazu; Kuroda, Yoshikazu; Matsuo, Masafumi; Kasuga, Masato; Okumura, Katsuhiko published the artcile< Chemosensitivity Assessed by Collagen Gel Droplet Embedded Culture Drug Sensitivity Test, and MDR1, MRP1, and MRP2 mRNA Expression in Human Colorectal Adenocarcinomas>, Safety of 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate, the main research area is chemosensitivity test multidrug resistance antitumor colorectal adenocarcinomas.

Purpose: To evaluate chemosensitivity and its correlation with expression levels of the multidrug resistant transporter (MDR1) and the multidrug resistance-associated proteins 1 and 2 (MRP1, MRP2) mRNA in human colorectal adenocarcinomas. Methods: Colorectal adenocarcinomas were obtained as surgical samples from 25 patients. The chemosensitivity of 12 anticancer drugs was assessed by the collagen gel droplet embedded culture drug sensitivity test (CD-DST). The expression levels of MDR1, MRP1, and MRP2 mRNA in colorectal adenocarcinomas were also evaluated by real-time quant. reverse transcription-polymerase chain reaction (RT-PCR). Results: The chemosensitivity was successfully evaluated for 16 of 25 patients, and the anticancer drugs were effective against the samples showing a relatively high growth rate. Gemcitabine hydrochloride was found to be more promising than those often prescribed for the treatment of colorectal adenocarcinoma. There was no correlation of the mRNA expression levels of MDR1 and MRP1 with the chemosensitivity of any anticancer drugs tested, but mitomycin C was found to be more effective for the colorectal adenocarcinoma with relatively high expression of MRP2 mRNA.

Pharmaceutical Research published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (MRP1). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Safety of 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Su, Jinling; Zhang, Yan; Chen, Mingren; Li, Weiming; Qin, Xuewei; Xie, Yanping; Qin, Lixiao; Huang, Shihua; Zhang, Min published the artcile< A Copper Halide Promoted Regioselective Halogenation of Coumarins Using N-Halosuccinimides as Halide Source>, Application In Synthesis of 128-09-6, the main research area is chloro bromo coumarin preparation regioselective; coumarin halogenation halosuccinimide copper halide catalyst.

A safe, convenient, and regioselective synthesis of 3-halo coumarins using a metal halide (CuX2 alone or with ZnX2) promoted halogenation with N-halosuccinimides (NXS) as halide source. The synthesis involved the steady in situ generation of highly reactive pos. halogen (X+) by the coordination of copper or zinc with the N-halosuccinimide and subsequent electrophilic aromatic substitution of the electron-deficient coumarins. This procedure works well also for the halogenation of less electron-rich naphthoquinones, flavones, and methoxypsoralen in moderate to quant. yields. This protocol features simple exptl. conditions using readily available inexpensive reagents and provides a convenient approach to the chlorination or bromination of some useful heteroaromatic compounds

Synlett published new progress about Bromination catalysts (regioselective). 128-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C4H4ClNO2, Application In Synthesis of 128-09-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Lu, Tong; Dong, Ling; Pan, Hongmei; Wu, Xuedan; Chen, Xia; Gu, Chengwen; Tao, Naili; Wang, Ao; Zhang, Kehua; Jin, Jie published the artcile< Design and synthesis of C-ring quinoxaline-substituted sinomenine 1,2,3-triazole derivatives via click reactions>, Computed Properties of 611-19-8, the main research area is quinoxalinyl triazolyl sinomenine preparation.

The synthesis of C-ring quinoxaline-substituted sinomenine 1,2,3-triazole derivatives at the 4-OH via click reactions was accomplished, and a total of 16 novel sinomenine double N-heterocyclic derivatives are obtained in 74%-95% yields. The C-ring is first transformed into a 1,2-diketone structure under the action of hydrochloric acid, and then reacted with o-phenylenediamine to obtain a C-ring quinoxaline-substituted structure. The 4-OH of sinomenine reacted with chloropropyne to give an alkynyl sinomenine, and then reacts with sodium azide and various benzyl chlorides to give the target compounds All the synthesized derivatives were characterized by Fourier-transform IR spectrometry, high resolution mass spectrometry, 1H NMR, and 13C NMR spectroscopy.

Journal of Chemical Research published new progress about Aralkyl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Computed Properties of 611-19-8.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zhou, Lu; Zhu, Chuan; Bi, Peijia; Feng, Chao published the artcile< Ni-catalyzed migratory fluoro-alkenylation of unactivated alkyl bromides with gem-difluoroalkenes>, Recommanded Product: 3-Chlorophenethyl Bromide, the main research area is aralkyl bromide aryl difluoroalkene nickel catalyst stereoselective regioselective fluoroalkenylation; diaryl fluoroalkene preparation.

Nickel-catalyzed highly regio- and stereoselective migratory fluoro-alkenylation of unactivated alkyl bromides was reported. Catalytic cycle merged alkyl nickel chain-walking and defluorinative coupling enabled the introduction of a broad array of fluoroalkenyl moieties into carbon chains. Control experiments with other halogenated alkenes demonstrated the essential role of fluorine atoms in this reaction. The reaction proceeded under mild conditions and allowed for the synthesis of a variety of valuable monofluoroalkenes.

Chemical Science published new progress about Alkenylation catalysts, stereoselective. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Recommanded Product: 3-Chlorophenethyl Bromide.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Gummidi, Lalitha; Kerru, Nagaraju; Awolade, Paul; Raza, Asif; Sharma, Arun K.; Singh, Parvesh published the artcile< Synthesis of indole-tethered [1,3,4]thiadiazolo and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids as anti-pancreatic cancer agents>, Synthetic Route of 70057-67-9, the main research area is indole tethered thiadiazolo oxadiazolopyrimidinone hydrid preparation antitumor agent; Indole; Molecular hybridization; Pancreatic cancer; Pyrimidinone; [4+2] Cycloaddition reaction.

New indole-tethered [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one (e.g. I) and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids (e.g. II) were synthesized using [4+2] cycloaddition reactions of functionalized 1,3-diazabuta-1,3-dienes with indole-ketenes. All mol. hybrids were structurally characterized by spectroscopic techniques (IR, NMR, and HRMS) and screened for their anti-pancreatic cancer activity in vitro. The [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids showed stronger anti-pancreatic cancer activity than the [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one hybrids against the PANC-1 cell line. II bearing an ortho-chlorophenyl moiety emerged as the most potent anti-pancreatic cancer agent with an IC50 value of 7.7 ± 0.4μM, much superior to the standard drug Gemcitabine (IC50 > 500μM). The discovery of these [1,3,4]thiadiazolo and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids elicits their potentials as pursuable candidates for pancreatic cancer chemotherapy.

Bioorganic & Medicinal Chemistry Letters published new progress about [4+2] Cycloaddition reaction. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Synthetic Route of 70057-67-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics