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Microwave-Assisted Hirao and Kabachnik–Fields Phosphorus–Carbon Bond Forming Reactions
Published in Banik Bimal Krishna, Bandyopadhyay Debasish, Advances in Microwave Chemistry, 2018
All the synthesized compounds 6 were evaluated for both their progesterone receptor (PR) antagonist (T47D cell-based assay) and glucocorticoid receptor (GR) antagonist activity (A549 cell-based assay), and their corresponding activities were compared with those of mifepristone, the first competitive progesterone antagonist drug. A selective progesterone receptor (PR) antagonist has potential utility as a contraceptive and also in treating reproductive disorders, such as uterine leiomyomas and endometriosis, and hormone-dependent tumors (Jiang et al., 2006). Hence, the search for some novel class of selective progesterone receptor modulators (PRMs) having only the anti-progestational activity remains highly desirable, both in terms of clinical applications and basic endocrine research. Most of the compounds were potent PR antagonists (nanomolar range), with some showing better selectivity than mifepristone (IC50’s: 0.2 nM (T47D), 2.6 nM (A549); selectivity ratio: 13). Among the series, the most potent molecules were found to be 6a ((IC50’s: 9.9 nM (T47D), 237.7 nM (A549); selectivity ratio: 24), 6b (IC50’s: 3.58 nM (T47D), 660.15 nM (A549); selectivity ratio: 184), and 6c (IC50’s: 1.6 nM (T47D), 270.86 nM (A549); selectivity ratio: 169). In addition, some selected compounds showed modest oral progestin antagonist activity in rat uterus. From the view-point of structure-activity relationship, it was evident that when R1 and R2 are both alkoxy groups, the change in their size did not affect potencies, while a change in the electronics reduced the potency with a more electron-withdrawing group. It was also observed that substitution at the phenyl ring did not significantly change the potency (Jiang et al., 2006).
Assessment of Quercetin Isolated from Enicostemma Littorale Against Few Cancer Targets: An in Silico Approach
Published in A. K. Haghi, Ana Cristina Faria Ribeiro, Lionello Pogliani, Devrim Balköse, Francisco Torrens, Omari V. Mukbaniani, Applied Chemistry and Chemical Engineering, 2017
Some breast cancers require estrogen to continue growing. They can be identified by the presence of estrogen Receptors (ER) and progesterone Receptors (PR) on their surface (sometimes referred together as hormone receptors).14 These ER cancers can be treated with drugs that either block the receptors, for example, tamoxifen, or alternatively block the production of estrogen.
Prognostic elements extraction from documents to detect prognostic stage
Published in Computer Methods in Biomechanics and Biomedical Engineering, 2022
Pratiksha R. Deshmukh, Rashmi Phalnikar
Anatomic stage is an important task in cancer prognosis (Irena et al. 2014). Anatomic stage, also known as the Tumor-Node-Metastasis (TNM) stage which represents size and location of tumor, number of lymph node affected, and metastasis information. Biologic factors like grade, estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER2), etc. represent tumor biology in the cancer prognosis stage. Hence, the prognostic stage is a combination of TNM factors and biologic factors for cancer prognosis. It illustrates the variations in cancer survivors’ outcomes with different tumor biology but having the same TNM stage. Cancer patients with upper TNM stage and appropriate tumor biology have effective treatment than those with low-level TNM value but undesirable tumor biology. Hence, to improve breast cancer prognosis, automated extraction of biologic factors from unstructured medical records needs to be considered.
Dihaloplatinum(II) complexes having diimine ligands: crystal structure, thermal properties, cytotoxicity effects against breast cancer cells and application as a precursor towards nanoparticles
Published in Journal of Coordination Chemistry, 2019
Badri Zaman Momeni, Nastaran Fathi, Jan Janczak, Zahra Shahsavari
Platinum-based chemotherapy including three platinum-based cisplatin, carboplatin and oxaliplatin is used throughout the world [52]. Although the mechanism of cytotoxicity of the new anticancer compounds is still unclear, the preparation of new platinum complexes containing a variety of ligands with the aim of decreasing side effects and highly effective drugs has demonstrably drawn the attention for chemists [52, 53]. Breast cancer has been classified based on the estrogen receptor (ER), progesterone receptor (PR), and HER-2/neu receptor (HER-2) expressions [54]. Herein, the cytotoxic effects of some platinum complexes have been carried out against two selected human breast cancer cell lines of the MCF-7 and MDA-MB-468, which reveal the greater activity in the case of [PtCl2(bu2bpy)] (3). Interestingly, MDA-MB-468 as a triple negative breast cancer cell line (ER-, PR-, Her-2-) showed the best sensitivity to 3. These results indicate that the most active platinum compounds include the bipyridine ligand substituted in the 4,4'-position with the highest steric effects and electron-donating group as the "non-leaving group" as well as the electron-withdrawing chloride group as the "leaving group ligand".
A review of the impact of shift work on occupational cancer: Part 2 – mechanistic and health and safety evidence
Published in Policy and Practice in Health and Safety, 2018
J. O. Crawford, J. W. Cherrie, A. Davis, K. Dixon, C. Alexander, H. Cowie, D. M. McElvenny
Hoffman et al. (2010) reported statistically significant associations between single nucleotide polymorphisms associated with the CLOCK genes and breast cancer risk, which were modified by oestrogen receptor/progesterone receptor (ER/PR) status. Where there was more than one risk allele present the risk was only significantly increased in those with positive ER/PR status. Zienolddiny et al. (2013), in a large study of Norwegian nurses, showed that in women with long-term working for three consecutive night shifts, the risk of breast cancer was reduced in those with some variant alleles of CLOCK, PER3 and several other genes or melatonin signalling pathways. However, the associations were not reproducibly found in women who had worked four on more consecutive nights. Zhu et al. (2011) identified that long-term shift work exposure promotes hypomethylation of CLOCK and hypermethylation of CRY2 genes. In a small study (10 day workers and 10 long-term shift workers), Shi et al. (2013) identified circadian-relevant epigenetic changes in shift workers. They argued that these changes suggest that long-term night shift work results in down-regulation of miR-219, which may result in the down-regulation of immunomediated antitumor activity and an increase in breast cancer risk. While these studies add some support for the causality of night work for breast cancer they shed little light on the causal mechanism.