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1.
Ultrasonics ; 113: 106367, 2021 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-33550086

RESUMO

The paper presents a study of surface acoustic waves propagation in a damage layer with finite thickness and residual stress on an orthotropic semi-infinite medium to reveal the application of laser ultrasound in the surface inspection of ground silicon wafers. Biot's theory of small deformations influenced by initial stress forms the basis for this study. Considering the case that the displacement and boundary forces are continuous at the interface and the forces vanish on the free surface, the required dispersion relation is obtained. We consider a sample of (100) silicon wafer by grinding with fine abrasive grains, which has a machined face with a micrometer-level thickness of surface damage and residual stress. In order to discuss the impact of propagation directions, degree of surface damage, residual compressive stress on the velocity characteristics of surface waves, the numerical computation of the dispersion equations is performed. It has been found that surface damage has a significant effect on the dispersion curve, while the residual compressive stress can only cause a small decrease Δc in the surface wave velocity. The velocity decrease Δc becomes obvious at high frequencies. For a fixed residual compressive stress and frequency, Δc hardly changes with the degree of surface damage and propagation directions. Based on the above characteristics, we study the inverse problem on detecting both surface damage and residual stress simultaneously by SAW velocities and give a corresponding iterative algorithm. This study may provide theoretical guidance for non-destructive testing of residual stress.

2.
Phytochemistry ; 184: 112675, 2021 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-33548770

RESUMO

Seven undescribed tirucallane-type triterpenoids, kumunorquassins A‒E and kumuquassins K and L, along with nine known analogues, have been isolated from the leaves of Picrasma quassioides (D. Don) Benn. Their structures and absolute configurations were elucidated based on comprehensive spectroscopic analyses, single-crystal X-ray diffraction analysis and electronic circular dichroism (ECD). The absolute configuration of cornusalterin J was unequivocally determined by X-ray diffraction based on its p-bromobenzoate derivative. A brief approach was presented in our study, which could rapidly and conveniently determine the relative and absolute configurations of OCH3-23 of kumuquassin L and cornusalterins J, H and G depending on the chemical shift differences (Δδ) of C-24 and C-25 and the chemical shifts of C-23, H-23 and H-24. In addition, the cytotoxicities of these compounds against two human tumour cell lines (HepG2 and Hep3B) were evaluated.

3.
Skeletal Radiol ; 2021 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-33538864

RESUMO

OBJECTIVE: Characterize the appearance of digital nerve injuries in different ultrasound planes and correlate the presence and size of neuromas with time from injury. MATERIALS AND METHODS: Surgically confirmed nerve injuries were retrospectively evaluated. Appearances of the nerve injury in the available imaging planes were reviewed by two readers. Associations between presence and size of neuroma with time from injury were analyzed. RESULTS: Injuries of 29 digital nerves (3 incomplete lacerations, 17 complete lacerations, 6 with 7 stump neuromas, 3 neuromas-in-continuity) noted on ultrasound were surgically confirmed. Among the 20 lacerations, long-axis images were obtained in 15, of which 10 depicted the injury and 4 did not. Among the 10 depicting the injury in long axis, 2 showed a discrete gap, and 7 showed the nerve obscured by laceration tissue without a gap. In short axis, the nerve injury was visible in all 20, and nerve laceration was seen as a discrete gap in 2, and obscuration by laceration tissue in 14. Neuromas were hypoechoic and well-defined. There was a positive association between time and presence of neuroma (OR = 1.3, p = 0.002). Correlations between time and cross-sectional area (rs = 0.45) and volume (rs = 0.57) of neuromas were moderately positive. CONCLUSION: Ultrasound long axis may be less useful, and those short axis may be more reliable for assessing digital nerve injuries than previously reported. Neuromas are hypoechoic and well-defined, and their size can vary based on time from injury.

4.
Muscle Nerve ; 2021 Jan 26.
Artigo em Inglês | MEDLINE | ID: mdl-33501678

RESUMO

INTRODUCTION: In this study, we aimed to determine whether muscle transverse relaxation time (T2 ) magnetic resonance (MR) mapping results correlate with motor unit loss, as defined by motor unit recruitment patterns on electromyography (EMG). METHODS: EMG and 3-Tesla MRI exams were acquired no more than 31 days apart in subjects referred for peripheral nerve MRI. Two musculoskeletal radiologists qualitatively graded T2 -weighted, fat-suppressed sequences for severity of muscle edema-like patterns and manually placed regions of interest within muscles to obtain T2 values from T2 -mapping sequences. Concordance was calculated between qualitative and quantitative MR grades and EMG recruitment categories (none, discrete, decreased) as well as interobserver agreement for both MR grades. RESULTS: Thirty-four muscles (21 abnormal, 13 control) were assessed in 13 subjects (5 females and 8 males; mean age, 46 years) with 14 EMG-MRI pairs. T2 -relaxation times were significantly (P < .001) increased in all EMG recruitment categories compared with control muscles. T2 differences were not significant between EMG grades of motor unit recruitment (P = .151-.702). T2 and EMG score concordance was acceptable (Harrell's concordance index [c index]: rater A, 0.71; 95% confidence interval [CI], 0.51-0.87; rater B, 0.77; 95% CI, 0.57-0.91). Qualitative MRI and EMG score concordance was poor to acceptable (c index: rater A, 0.60; 95% CI, 0.50-0.79; rater B, 0.72; 95% CI, 0.55-0.89). T2 values had moderate-to-substantial ability to distinguish between absent vs incomplete (ie, decreased or discrete) motor unit recruitment (c index: rater A, 0.78; 95% CI, 0.50-1.00; rater B, 0.86; 95% CI, 0.57-1.00). DISCUSSION: Quantitative T2 MR muscle mapping is a promising tool for noninvasive evaluation of the degree of motor unit recruitment loss.

5.
Bioorg Chem ; 107: 104597, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33450546

RESUMO

Stephania epigaea H. S. Lo is a folk medicine widely distributed in the south of China, especially in Yunnan and Guangxi province. An in vitro anti-neuroinflammatory study showed that total alkaloids of it can potently inhibit LPS-induced NO releasing of BV2 cells with an IC50 value of 10.05 ± 2.03 µg/mL (minocycline as the positive drug, IC50 15.49 ± 2.14 µM). The phytochemical investigation of the total alkaloids afforded three new phenanthrene (1-3), two lactams (4a, 4b), and nine aporphine derivatives (5-13). The final structure of 1 was identified by computer-assisted structure elucidation (ACD/Structure Elucidator software and the 13C NMR calculation with GIAO method) due to many possibilities of the substituent pattern. All isolates were evaluated for their anti-neuroinflammatory effects, and as a result, 5, 8, 10, and 11 exhibited stronger inhibitory activities than the minocycline. The results suggested S. epigaea could provide potential therapeutic agents for neurodegenerative diseases.

6.
Phytochemistry ; 183: 112628, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33412403

RESUMO

Nine undescribed guaiane-type sesquiterpenoids stelleraterpenoids A‒I, along with seven reported congeners, were isolated and identified from the 70% EtOH extract of the roots of Stellera chamaejasme L. Their chemical structures were elucidated on the basis of various spectral data. The relative configurations were determined by their NOESY spectra and comparison between their experimental and calculated NMR data. The absolute configurations were established by the comparison between the experimental and calculated ECD spectra and further by X-ray single-crystal diffraction analysis. The neuroprotective effects of these compounds on the H2O2-induced damage in human neuroblastoma SH-SY5Y cells were evaluated. Stelleraguaianone B exhibited the better activity with 71.62% cell viability compared to the positive control Trolox (65.05%) at 12.5 µM, which might be achieved by inhibiting the apoptosis of SH-SY5Y cells based on an annexin V-FITC/PI staining experiment.


Assuntos
Fármacos Neuroprotetores , Sesquiterpenos , Thymelaeaceae , Peróxido de Hidrogênio , Estrutura Molecular , Fármacos Neuroprotetores/farmacologia , Sesquiterpenos/farmacologia , Sesquiterpenos de Guaiano
7.
Expert Opin Ther Pat ; 31(3): 239-246, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33320034

RESUMO

INTRODUCTION: The ß2 adrenergic receptor (ß2AR) is a member of G protein-coupled receptors (GPCRs) that mediate the majority of cellular responses to external stimuli. The agonists can cause smooth muscle relaxation; therefore, many ß2AR agonists have been developed especially for the treatment of pulmonary disorders such as asthma and chronic obstructive pulmonary disease (COPD). Many new natural and synthetic compounds have been discovered and developed as novel ß2AR agonists over the past 5 years. AREAS COVERED: This review offers an update for the development of ß2AR agonists in the patents published from 2015 to 2020, including new natural and synthetic compounds for the treatment of asthma and COPD. In particular, the latest patents about compounds possessing both muscarinic receptor antagonist and ß2 adrenergic receptor agonist activity are reviewed. EXPERT OPINION: ß2AR agonists have been developed extensively for the treatment of asthma and COPD. In the past 5 years, novel agonists from both natural sources and synthetic methods were intensively developed. Compounds possessing both muscarinic receptor antagonist and ß2AR agonist activity represent a new trend in this area because they are possibly able to act together in a synergistic fashion, therefore, relieve the symptoms of patients through two distinct mechanisms.

8.
Bioorg Chem ; : 104498, 2020 Nov 24.
Artigo em Inglês | MEDLINE | ID: mdl-33272710

RESUMO

Seven new diterpenoids (1-7), including five 7-membered ring vibsane-type diterpenoids, vibsanolide A-E (1-5) and a pair of epimers of 14,15,16,17-tetranorvibsane-type diterpenoids possessing bicyclo[4.2.1]nonane moiety, vibsanolide F-G (6-7), together with twelve known analogues (8-19) were isolated from the crude extracts of the leaves of Viburnum odoratissimum using Small Molecule Accurate Recognition Technology (SMART). These structures including absolute configurations were elucidated by means of comprehensive analyses of spectroscopic data, as well as comparison of the experimental and calculated electronic circular dichroism (ECD) spectra. These compounds were evaluated for their cytotoxic activities against A549 and HepG2 cells by MTT assay. The results showed that compound 2 exhibited potent cytotoxic activity against A549 cells with IC50 value of 1.11 µM. Further staining experiments indicated that 2 could promote apoptosis induction, enhance reactive oxygen species (ROS) level and attenuate mitochondrial membrane potential (MMP) in A549 cells. Taken together, these findings provided new insights into understanding the cytotoxic activity of vibsane-type diterpenoids and it is meaningful to further investigate the application potential of V. odoratissimum.

9.
Neurol Clin Pract ; 10(5): 415-421, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33299669

RESUMO

Objective: We evaluated the performance of ultrasound in the detection of neuropathy of the suprascapular nerve (SSN), long thoracic nerve (LTN), spinal accessory nerve (SAN), and phrenic nerve and compared this performance with MRI. Methods: A retrospective review of 56 patients who had undergone ultrasound imaging of the SSN, LTN, SAN, and phrenic nerve was performed. Diagnoses made by ultrasound, MRI, EMG reports, and clinical and operative notes were recorded. Results: Ultrasound was successful in visualizing nerves in the neck in the overwhelming majority of cases. Sonographic findings were typically in agreement with MRI and clinical findings. Conclusion: Ultrasound is effective in the visualization and diagnostic evaluation of the SSN, LTN, SAN, and phrenic nerve. Classification of evidence: This study provides Class IV evidence that ultrasound can effectively visualize and diagnose neuropathy of the SSN, LTN, SAN, and phrenic nerve in the neck.

10.
Appl Opt ; 59(34): 10645-10650, 2020 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-33361881

RESUMO

The error-diffusion dithering technique is widely used in three-dimensional (3D) measurement. The sinusoid similarity of dithering fringe patterns greatly affects measurement accuracy, while the traditional dithering methods lack this quality. In this paper, we present a kernel-optimized dithering technique based on the Floyd-Steinberg dithering method and establish an optimization strategy considering both intensity and phase aspects to generate high-quality sinusoidal fringes for 3D measurement by utilizing the binary defocusing technique. Both simulations and experiments demonstrate that the proposed method could improve the performance of 3D measurement effectively under different defocusing amounts, especially in narrow strips.

11.
Exp Neurol ; 335: 113528, 2020 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-33189730

RESUMO

Ischemic stroke (IS) is one of the most common cerebrovascular diseases worldwide. The aberrant expression of BCL6 has been previously implicated in the pathogenesis of IS. Meanwhile, miR-31 is known as a target of BCL6, and has also been suggested to diminish cell damage by suppressing the PKD1 expression. Expanding on this relationship, the current study set out to investigate whether BCL6 participates in ischemic stroke by targeting PKD1. Firstly, IS models were established in vitro and in vivo. TUNEL staining and MTT assay were performed to examine the apoptosis and cell survival. In addition, qRT-PCR and Western blot analysis were applied to examine the expression patterns of the BCL6/miR-31/PKD1 axis and its downstream pathway. Bioinformatics analysis was used to predict the target of miR-31. It was found that BCL6 over-expression promoted ODG-induced increase of apoptosis and decreased the cell survival and miR-31 expression levels, whereas the opposite effects were noted in vitro and in vivo models of IS that were treated with shBCL6. Furthermore, miR-31 down-regulation blocked the effect of BCL6 on ODG-induced cell injury. It was also verified that miR-31 directly-targets PKD1. Also, OGD induced the PKD1 expression and activation of the JAK2/STAT3 pathway, while down-regulation of PKD1 inhibited the OGD-induced cell injury and JAK2/STAT3 pathway activation. Lastly, down-regulation of BCL6 in brain brought about a significant reduction in the size of cerebral infarction and oxidative stress levels in IS mice. Collectively, our findings suggest that inhibition of BCL6 may attenuate oxidative stress-induced neuronal damage by targeting the miR-31/PKD1 axis.

12.
Chemosphere ; : 128826, 2020 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-33162155

RESUMO

A quality-assured ecological risk assessment (ERA) requires enormous resources (time and labor) in collection/assessment of hazard data, as well as considerable expertise to interpret the risk. The ERA of chemicals is thereby considered difficult or impossible for those with little assessment experience and cumbersome or complicated for practitioners. To meet the concerns regarding ERA and accelerate the risk assessment and management of chemicals, we developed an all-in-one free tool for multi-purpose ecological risk assessment management (MeRAM) of chemical substances in aquatic environment called the AIST-MeRAM Ver. 2.0.0 (Copyright No: H28PRO-2007). It allows users from beginners to experts to conduct ERA without any preparation because all the necessary ecotoxicity test data and methodologies are available in the system. Approximately 270,000 ecotoxicity test data points for 3900 chemical substances together with the scientific methodologies from traditional simple hazard quotient (HQ) to more ecologically relevant complicated assessments such as species sensitivity distribution (SSD) and population-level assessment are embedded in the AIST-MeRAM. In addition, users can easily understand the Japanese regulatory RA and management of chemical substances due to a special function based on the Japanese Chemical Substance Control Law (CSCL). Here, we demonstrate a tiered ERA using the embedded sample data to evaluate and ensure the functions of AIST-MERAM. We show that the AIST-MeRAM can provide a comprehensive and accurate ERA, suggesting that it is a powerful IT solution for cumbersome ERA.

13.
Bioorg Chem ; 105: 104438, 2020 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-33171406

RESUMO

Six undescribed lanostane triterpenoids (1-6), together with three known compounds (7-9) were isolated from Inonotus obliquus. Compounds 3-5 are the rare natural compounds featuring a 4,5-seco-lanostane core with a 5,7,9-trien-21,24-cyclopentane moiety. The structure elucidation of the compounds was conducted by spectroscopic techniques and the ECD method. The absolute configuration of compound 1 was confirmed by single-crystal X-ray diffraction analysis. All isolated compounds were assayed for their neuroprotective activity against H2O2-induced cell injury using human neuroblastoma SH-SY5Y cells. Compound 9 exhibited the most potent neuroprotective activity and the flow cytometry analysis indicated that 9 could protect SH-SY5Y cells from oxidative damage by inhibiting cell apoptosis.

14.
J Med Chem ; 2020 Nov 19.
Artigo em Inglês | MEDLINE | ID: mdl-33213146

RESUMO

ß2-Adrenoceptor (ß2-AR) agonists are widely used as bronchodilators. The emerge of ultralong acting ß2-agonists is an important breakthrough in pulmonary medicine. In this review, we will provide mechanistic insights into the application of ß2-agonists in asthma, chronic obstructive pulmonary disease (COPD), and heart failure (HF). Recent studies in ß-AR signal transduction have revealed opposing functions of the ß1-AR and the ß2-AR on cardiomyocyte survival. Thus, ß2-agonists and ß-blockers in combination may represent a novel strategy for HF management. Allosteric modulation and biased agonism at the ß2-AR also provide a theoretical basis for developing drugs with novel mechanisms of action and pharmacological profiles. Overlap of COPD and HF presents a substantial clinical challenge but also a unique opportunity for evaluation of the cardiovascular safety of ß2-agonists. Further basic and clinical research along these lines can help us develop better drugs and innovative strategies for the management of these difficult-to-treat diseases.

15.
J Nat Prod ; 2020 Nov 20.
Artigo em Inglês | MEDLINE | ID: mdl-33216556

RESUMO

Eleven metabolites, six echinosporins (1-6), four dibenzoyls (7-10), and an aromatic compound (11), were isolated from the fermentation broth of lichen-associated Amycolatopsis hippodromi. The structures of the new compounds (1-5, 8-11) were elucidated by comprehensive spectroscopic analysis including data from experimental and calculated ECD spectra. Amycolasporins A-C (1-3) demonstrated antibacterial activities against Bacillus subtilis, Staphylococcus aureus, and Escherichia coli with MIC values of 25 or 100 µg/mL. Amycolasporin C (3) and the known dibenzoyl (7) attenuated the production of NO due to the suppression of the expression of nitric oxide synthase (iNOS) in LPS-induced RAW 264.7 cells in a dose-dependent manner.

16.
Drug Des Devel Ther ; 14: 4835-4843, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33204069

RESUMO

Purpose: Precise and timely detection of methotrexate (MTX) concentration played a key role in high-dose MTX individualization therapy in acute lymphoblastic leukemia (ALL) children to avoid serious adverse effects or nonresponse. This report described a sensibility and validation of ultra-high performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) method for therapeutic drug monitoring (TDM) of methotrexate concentration in children's plasma. Methods: One-step protein precipitation of samples was accomplished by adding 200 µL of acetonitrile to 100 µL of plasma sample. The separation of plasma samples was carried out on a ZORBAX Eclipse Plus C18 Rapid Resolution HD column with gradient elution using a mobile phase constituted of acetonitrile and 1% formic acid. The detection was executed by electrospray ionization (ESI) of triple quadrupole tandem mass spectrometer (TQMS) in the multiple reaction monitoring (MRM) mode with the transitions m/z 455.2 → 307.9 for methotrexate and m/z 458.2 → 311.2 for IS, separately. Linear concentration range of the calibration curve was 44-11,000 nmol/L and 44 nmol/L was the lower limit of quantification. Results: The methotrexate elution time was at 1.577 min, and the overall running time was only 3.3 min. The intra- and interday precision for all the analysis results was within 11.24%, and mean recoveries rate of methotrexate exceeded 87.98%. Conclusion: The described and fully validated UHPLC-MS/MS method was successfully applied in clinical TDM after infusion of high-dose methotrexate 1-5 g/m2 to 41 childpatients.

17.
Aging (Albany NY) ; 122020 Nov 18.
Artigo em Inglês | MEDLINE | ID: mdl-33206628

RESUMO

Heart failure (HF) affects over 26 million people worldwide, yet the pathologies of this complex syndrome have not been completely understood. Here, we investigated the involvement of deacetylase Sirtuin 1 (Sirt1) in HF and its downstream signaling pathways. A HF model was induced by the ligation of the left coronary artery in rats, where factors associated with left ventricular echocardiography, heart hemodynamics and ventricular mass indexes were recorded. Collagen volume fraction in heart tissues was determined by Masson's trichrome staining. Cell models of HF were also established (H2O2, 30 min) in cardiomyocytes harvested from suckling rats. HF rats presented with downregulated expressions of Sirt1, brain-derived neurotrophic factor (BDNF) and exhibited upregulated expressions of NF-κB p65 and miR-155. Repressed Sirt1 expression increased acetylation of NF-κB p65, resulting in the elevation of NF-κB p65 expression. NF-κB p65 silencing improved heart functions, decreased ventricular mass and reduced apoptosis in cardiomyocytes. MiR-155 inhibition upregulated its target gene BDNF, thereby reducing cardiomyocyte apoptosis. Sirt1 overexpression upregulated BDNF, improved heart function, and reduced apoptosis in cardiomyocytes. In conclusion, Sirt1 alleviates HF in rats through the NF-κB p65/miR-155/BDNF signaling cascade.

18.
Nat Prod Res ; : 1-7, 2020 Nov 19.
Artigo em Inglês | MEDLINE | ID: mdl-33207963

RESUMO

Five new α-pyrone derivatives, cryptoyunnanes A - E (1 - 5), together with four known analogues, were isolated from the leaves and twigs of Cryptocarya yunnanensis. Their structures including absolute configurations were elucidated by extensive spectroscopic data and electronic circular dichroism (ECD) analyses. Compounds 4 and 6 showed significant cytotoxicity against A549, HCT-116, MDA-MB-231, PC-3 and HeLa with IC50 values from 2.25 to 8.97 µM. Compounds 1, 2 and 7 also displayed good cytotoxicity against HCT-116, MDA-MB-231 and PC-3 with IC50 values from 1.26 to 8.32 µM. This is the first time to report the isolation and bioactivity evaluation of chemical constituents from C. yunnanensis.

19.
Bioorg Chem ; 104: 104338, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33142410

RESUMO

Nine undescribed (1-4, 6-10) sesquiterpene coumarins, together with a new natural one (5) and ten known ones (11-20), were isolated from the low polarity fraction of the 95% ethanol extract of the resin of Ferula sinkiangensis. Their structures were elucidated based on the comprehensive analysis of HRESIMS, 1D and 2D NMR data. The absolute configurations were determined by comparison of experimental and calculated ECD spectra. All the identified SCs were evaluated for their anti-neuroinflammatory activities in LPS-induced BV-2 cells. Ferusingensine G (8) displayed a significant inhibitory effect on nitric oxide (NO) production with an IC50 value of 1.2 µM. The results suggested that natural SCs might be served as potential neuroinflammatory inhibitors.

20.
Bioorg Chem ; 104: 104347, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33142414

RESUMO

A series of artemisinin-sulfonamide hybrids (1-16) have been designed and synthesized by using molecular hybridization approach and investigated for the inhibitory activity of four human (h) carbonic anhydrases (CAs, EC 4.2.1.1), hCA I, II, IX and XII. The results indicated most of the target compounds showed better CA IX and CA XII inhibitory activity than the starting segment sulfanilamide. Among all the compounds, compound 3 (IC50: 5 nM) showed the best CA IX inhibitory efficacy. The p-aminobenzenesulfonamide derivatives showed significant antiproliferative activities against MDA-MB-231 breast cancer cell line and HT-29 colon cancer cell line under hypoxic conditions where CA IX and CA XII are overexpressed and most of them showed no apparent cytotoxic effects toward MCF-10A normal mammary epithelial cell. Among these derivatives, compound 3 displayed the most potent antiproliferative activities (IC50: 0.65 µM) against HT-29 cell line under hypoxia and low cytotoxicity (IC50: 78.0 µM) toward normal cell line. Meanwhile, compound 3 was found to efficiently decrease the hypoxia-induced extracellular acidification in both cancer cells. Molecular docking studies of compounds 3, 4, 5 and 9 revealed the proper interactions between the hybrid molecules and the active site of CA IX. All the results proved the effectiveness of the hybridization approach to develop novel artemisinin-sulfonamide compounds targeting CA IX for cancer treatment.

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