(3R,3'R,3a'R,4'S,7'S,7a'R)-3'-Acetoxy-7',7a'-dimethyl-4-methylene-2-oxodecahydrospiro[furan-3,2'-inden]-4'-yl (2Z)-2-methyl-2-butenoate/2-Butenoic acid, 2-methyl-, (3R,3'R,3a'R,4'S,7'S,7a'R)-3'-(acetyloxy)decahydro-7',7'a-dimethyl-4-methylene-2-oxospiro[furan-3(2H),2'-[2H]inden]-4'-yl ester, (2Z)-
Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
503.0±50.0 °C at 760 mmHg
HS Code Reference
Personal Projective Equipment
For Reference Standard and R&D, Not for Human Use Directly.
provides coniferyl ferulate(CAS#:18455-98-6) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
The improvement of body’s own immune system is considered one of the safest approaches to fight against cancer and several other diseases. Excessive catabolism of the essential amino acid, L-tryptophan (L-Trp) assists the cancer cells to escape normal immune obliteration. The formation of disproportionate kynurenine and other downstream metabolites suppress the T cell functions. Blocking of this immunosuppressive mechanism is considered as a promising approach against cancer, neurological disorders, autoimmunity, and other immune-mediated diseases. Overexpression of indoleamine 2,3-dioxygenase 1 (IDO1) enzyme is directly related to the induction of immunosuppressive mechanisms and represents an important therapeutic target. Several classes of small molecule-based IDO1 inhibitors have been already reported, but only few compounds are currently being evaluated in various stages of clinical trials as adjuvants or in combination with chemo- and radiotherapies. In the quest for novel structural class(s) of IDO1 inhibitors, we developed a series of 4,5-disubstituted 1,2,3-triazole derivatives. The optimization of 4,5-disubstituted 1,2,3-triazole scaffold and comprehensive biochemical and biophysical studies led to the identification of compounds, 3i, 4i, and 4k as potent and selective inhibitors of IDO1 enzyme with IC50 values at a low nanomolar level. These potent compounds also showed strong IDO1 inhibitory activities in MDA-MB-231 cells with no/negligible level of cytotoxicity. The T cell activity studies revealed that controlled regulation of IDO1 enzyme activity in the presence of these potent compounds could induce immune response against breast cancer cells. The compounds also showed excellent in vivo antitumor efficacy (of tumor growth inhibition = 79-96%) in the female Swiss albino mice. As a consequence, this study describes the first example of 4,5-disubstituted 1,2,3-triazole based IDO1 inhibitors with potential applications for immunotherapeutic studies.
Subject terms: Drug discovery and development, Oxidoreductases
4,5-Disubstituted 1,2,3-triazoles: Effective Inhibition of Indoleamine 2,3-Dioxygenase 1 Enzyme Regulates T cell Activity and Mitigates Tumor Growth
Subhankar Panda,#1 Nirmalya Pradhan,#1 Soumya Chatterjee,2 Sudhir Morla,3 Abhishek Saha,1 Ashalata Roy,1 Sachin Kumar,3 Arindam Bhattacharyya,corresponding author2 and Debasis Mannacorresponding author1
Background: Quantification of the association between the consumption of vegetables and risk of age-related cataract is still conflicting. We therefore conducted a meta-analysis to summarize the evidence from epidemiological studies of vegetables consumption with the risk of age-related cataract. Methods: Pertinent studies were identified by searching of PubMed and Web of Science. The random effect model was used to combine the results. Meta-regression and subgroups analyses were used to explore potential sources of between-study heterogeneity. Publication bias was estimated using Egger’s regression asymmetry test. Results: Finally, 9 articles involving 6,464 cataract cases and 112,447 participants were included in this meta-analysis. Pooled results suggested that highest vegetables consumption level compared with lowest level was inverse with the risk of age-related cataract [summary relative risk (RR) = 0.723, 95% CI = 0.594-0.879, I2 = 72.8%]. The associations were also significant in America [summary RR = 0.872, 95% CI = 0.791-0.960] and Europe [summary RR = 0.507, 95% CI = 0.416-0.619], but not in the other population. No publication bias was found. Conclusions: Higher vegetables consumption might be inversely associated with risk of cataract.
Vegetables, age-related cataract, meta-analysis
Association between vegetables consumption and the risk of age-related cataract: a meta-analysis
Guoqiang Huang,1 Laiwei Wu,2 Lianghui Qiu,1 Jiangfeng Lai,1 Zhengying Huang,3 and Li’an Liao4
Tamoxifen (TAM) and aromatase inhibitor (AI) therapies have been associated with increased risk of thromboembolic and cardiovascular events, respectively, in addition to other side effects. This study analysed the risk of these events and the overall survival (OS) benefit in breast cancer patients treated with AI, compared with TAM-treated patients, in a large population-based cohort.
This observational cohort study included women diagnosed with breast cancer and treated with TAM or AI. Data were extracted from primary care records in a population database (SIDIAP, System for the Development of Research in Primary Care). Incidence rates of study outcomes are reported. Survival analyses included Kaplan-Meier estimation and Cox proportional hazards models. Sensitivity analysis was carried out, using Fine and Gray models to account for competing risk of death. Confounding was minimized using propensity score adjustment and inverse probability weighting (IPW) adjustment.
Data from 3082 postmenopausal women treated with TAM, and 18,455 treated with AI, were available. Adjusted hazard ratios (HRs) [95% confidence interval (CI)] for AI users, compared with TAM group, were 0.93 (95%CI 0.69-1.26) for thromboembolic events (TEEs); 1.13 (95%CI 0.79-1.63) for cardiovascular events, and 0.76 (95%CI 0.70-0.82) for mortality. Additional analyses using competing risk analysis had similar results, while IPW adjustment showed a potential risk of pulmonary embolism (PE) [2.26 (95%CI 1.02-4.97)] in AI-treated patients.
AI users had >20% lower all-cause mortality compared with TAM users, without increasing risk to experience cardiovascular and TEEs. This would locate AI therapy on the first line in clinical practice. Thus, AI might be the most preferable option in adjuvant hormonal therapy choice.
aromatase inhibitor, breast cancer, cardiovascular events, overall mortality, tamoxifen, thromboembolic events
Thromboembolic, cardiovascular and overall mortality risks of aromatase inhibitors, compared with tamoxifen treatment: an outpatient-register-based retrospective cohort study
Marta Pineda-Moncusi, Natalia Garcia-Giralt, Adolfo Diez-Perez, Ignasi Tusquets, Sonia Servitja, Joan Albanell, Daniel Prieto-Alhambra, and Xavier Nogues