Synthesis, characterization, in vitro antimicrobial and anticancer studies of new platinum N-heterocyclic carbene (NHC) complexes and unexpected nickel complexes

Publication date: 15 October 2019Source: Journal of Organometallic Chemistry, Volume 898Author(s): Kar Bee Choo, Sui Mae Lee, Wai Leng Lee, Yuen Lin CheowAbstractA series of bidendate pyridine-functionalized metal N-heterocyclic carbene (NHC) complexes with various wingtip substituents (R = methyl, phenyl and tert-butyl) had been prepared from silver oxide-mediated transmetalation method. The basic backbone of the NHC ligands were prepared in two stepwise reactions: reduction of the commercially available 2-benzoylpyridine, followed by halogenation to yield 2-(chloro(phenyl)methyl)pyridine. Subsequent reactions with different imidazoles gave the desired imidazolium salts (or NHC precursors) with different R groups at the N wingtip (R = Me, Ph, t-Bu). Transmetalation of the imidazolium salts into platinum NHC complexes were achieved by using Ag2O mediated method with Pt(cod)Cl2 as the transmetalating agent. On the other hand, nickel NHC complexes were obtained via one pot synthesis method with nickel chloride as the transmetalating agent and reflux in the presence of a base. Following recrystallisation, the molecular structure of Pt NHC complex ( ± )-5a had been successfully elucidated via single crystal X ray diffraction (XRD) analysis. The six-membered ring of the platinum NHC complexes adopted a boat conformation with the phenyl ring arranged at the axial position. Meanwhile, two unexpected nickel complexes, i.e. a simple nickel coordination complex and a nic...
Source: Journal of Organometallic Chemistry - Category: Chemistry Source Type: research

Related Links:

ConclusionsPET/CT was useful for early detection of EPCs. The use of PET/CT for the early detection and treatment of EPCs with no symptoms can improve treatment outcomes.
Source: Oral Surgery, Oral Medicine, Oral Pathology and Oral Radiology - Category: ENT & OMF Source Type: research
In conclusion, exposure to luminal neratinib resulted in a pronounced elevation in fluid secretion in the rat intestine. Increasing luminal calcium inhibits the neratinib‐associated fluid secretion in a dose‐dependent manner. These results suggest that CaSR activation may be a potent therapeutic target to reduce chemotherapy‐associated diarrhea.
Source: Pharmacology Research and Perspectives - Category: Drugs & Pharmacology Authors: Tags: ORIGINAL ARTICLE Source Type: research
The objective of this study was to formulate an anticancer preclinical lead, IIIM-290, loaded in solid dispersions to enhance its solubility, dissolution, and oral pharmacokinetics. IIIM-290 is an in-house preclinical anticancer lead prepared by semisynthetic modification of the natural product rohitukine. It is an orally bioavailable Cdk inhibitor showing efficacy in xenograft models of pancreatic, colon and leukemia cancer. It demonstrated in vivo efficacy at a relatively higher dose owing to its poor aqueous solubility (∼8.6 µg/mL). Binary and ternary solid dispersions containing PVP K-30, xanthan gum, and PEG...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research
Authors: Wang Z, Zhang M, Shan R, Wang YJ, Chen J, Huang J, Sun LQ, Zhou WB Abstract As a member of the myotubularin family, myotubularin related protein 3 (MTMR3) has been demonstrated to participate in tumor development, including oral and colon cancer. However, little is known about its functional roles in breast cancer. In the present study, the expression of MTMR3 in breast cancer was evaluated by immunohistochemical staining of tumor tissues from 172 patients. Online data was then used for survival analysis from the PROGgeneV2 database. In vitro, MTMR3 expression was silenced in MDA‑MB‑231 cells...
Source: Oncology Reports - Category: Cancer & Oncology Tags: Oncol Rep Source Type: research
Abstract The combination regimen of TAS-102, a novel oral nucleoside antitumor agent containing trifluridine and tipiracil hydrochloride, with bevacizumab (C-TASK FORCE), a selective monoclonal antibody inhibitor of vascular endothelial growth factor-A, as salvage-line therapy for metastatic colorectal cancer (mCRC) was established based on its high clinical effectiveness. The aim of the present study was to evaluate the prognostic accuracy of the modified Glasgow Prognostic Score (mGPS) in patients receiving TAS-102 plus bevacizumab. The study included 17 patients (12 men and 5 women, mean age 60.4±13.4 ye...
Source: Clinical Lung Cancer - Category: Cancer & Oncology Authors: Tags: Mol Clin Oncol Source Type: research
Conclusion: GE exerted a potential anti-proliferative activity against DENA in liver, stomach and colon via Nrf2 activation, whilst suppression of oxidation and inflammation. PMID: 31450931 [PubMed - in process]
Source: Asian Pacific Journal of Cancer Prevention - Category: Cancer & Oncology Tags: Asian Pac J Cancer Prev Source Type: research
WEDNESDAY, Aug. 21, 2019 -- Oral antibiotic use is associated with an increased risk for colon cancer and a reduced risk for rectal cancer, according to a study published online Aug. 20 in Gut. Jiajia Zhang, M.D., M.P.H., from the Bloomberg-Kimmel...
Source: Drugs.com - Pharma News - Category: Pharmaceuticals Source Type: news
Abstract The aim of this study was to determine the efficacy of oral recombinant methioninase (o-rMETase) on a colon cancer primary tumor using a patient-derived orthotopic xenograft (PDOX) nude mouse model. Forty colon cancer primary tumor PDOX mouse models were divided into 4 groups of 10 mice each (total 40 mice) by measuring the tumor size. The groups were as follows: untreated control; 5-fluorouracil (5-FU) (50 mg/kg, once a week for two weeks, N = 10 mice) and oxaliplatinum (OXA) (6 mg/kg, once a week for two weeks, N = 10 mice); o-rMETase (100 units/day, oral 14 consecutive days, N = 1...
Source: Biochemical and Biophysical Research communications - Category: Biochemistry Authors: Tags: Biochem Biophys Res Commun Source Type: research
Abstract Due to the decrease of the drugs side effects in controlled drug delivery systems, today's many research has been focused on designing the new controlled drug delivery systems. The main aim of the present work was the improving of the layered double hydroxide (LDH) properties as a drug delivery system through the encapsulation with carboxymethyl cellulose (CMC). In the first section, 5-fluorouracil (5-Fu) as a colon anticancer drug was loaded in LDH(Zn/Al) (about 87%). The FT-IR, SEM, and XRD analysis were used to probe the successful synthesis of LDH(Zn/Al) and 5-Fu loading in it. In the following, the n...
Source: International Journal of Biological Macromolecules - Category: Biochemistry Authors: Tags: Int J Biol Macromol Source Type: research
ConclusionsOverall risk of cancer in our MS cohort did not significantly differ from the controls. However, the age at diagnosis of breast cancer was statistically significantly higher among the MS patients in comparison with a control population from the same patient pool. Further population-based larger studies spanning longer follow-up periods and longer exposure to emerging MS therapies are needed to evaluate cancer risk related to MS treatments and breast cancer risk in particular.
Source: Multiple Sclerosis and Related Disorders - Category: Neurology Source Type: research
More News: Cancer | Cancer & Oncology | Chemistry | Chloride | Colon Cancer | Colorectal Cancer | Molecular Biology | Oral Cancer | Study