Synthesis, cytotoxicity against cancer and normal cell lines of novel hydrazide –hydrazone derivatives bearing 5H-chromen-5-one

AbstractThe reaction of cyclohexan-1,3-dione with either of malononitrile or ethyl cyanoacetate gave the 4-amino-6,7-dihydro-5H-chromen-5-one derivatives3a and3b, respectively. The reaction of the latter compounds with cyanoacetylhydrazine gave the hydrazide –hydrazone derivatives5a and5b, respectively. Compounds5a,b were used as the key starting materials for the synthesis of thiophen, coumarin, and pyridine derivatives. The newly synthesized compounds were evaluated against three human cancer cell lines, including HCT116 (colon carcinoma cell), MGC803 (gastric carcinoma cell), and Huh7 (hepatoma carcinoma cell). The results showed that3b,5b,6b,6d,8b,8c,8d,8f,10b.12a –h,14a –d,15a –h, and16b –h displayed higher cytotoxic activity than 5-FU against HCT116 and MGC803 cell lines. Compounds14d and16f were the most promising compounds with IC50’s 0.25 and 0.09 μM against HCT116 cell line. The most potent compounds were selected for the in vitro against peripheral blood lymphocytes (PBL) from healthy donors. All compounds were practically devoid of significant cytotoxic activity in quiescent lymphocytes, with GI50’s of 42–68 μM, while with the mitogenic stimulus phytohaemagglutinin (PHA), the GI50’s were reduced to about 20–32 μM.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research

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ConclusionOur study demonstrated a significant correlation between Nectin-4 expression and tumor grade as well as stages (p 
Source: Journal of Cancer Research and Clinical Oncology - Category: Cancer & Oncology Source Type: research
In this study, 60 mice were randomly divided into four groups: Control group, DD group, HCC group, HCC-DD group. Mice received a chronic dose of reserpine to establish depression model, followed by Diethylnitrosamine and Carbon tetrachloride administration to establish HCC models. Behavioral depression was assessed by sucrose preference test (SPT) and the expression of Serotonin 1A (5-HT1A) receptor in the hippocampal. The expression of Oatp2a1 and Oatp2b1 in the digestive system tissues was detected by PCR and western blotting. Results: Reserpine-administrated mice had a reducing sucrose preference at Day 14 compared with blank mice (P
Source: Biomed Res - Category: Research Authors: Tags: Biomed Res Int Source Type: research
Abstract Hepatocyte nuclear factor 4-alpha (HNF4α) is a highly conserved member of nuclear receptor superfamily of ligand-dependent transcription factors that is expressed in liver and gastrointestinal organs (pancreas, stomach, and intestine). In liver, HNF4α is best known for its role as a master regulator of liver-specific gene expression and essential for adult and fetal liver function. Dysregulation of HNF4α expression has been associated with many human diseases such as ulcerative colitis, colon cancer, maturity-onset diabetes of the young, liver cirrhosis, and hepatocellular carcinoma. How...
Source: World Journal of Gastroenterology - Category: Gastroenterology Authors: Tags: World J Gastroenterol Source Type: research
Publication date: Available online 26 July 2019Source: Pharmacology &TherapeuticsAuthor(s): Jean-François GOOSSENS, Christian BAILLYAbstractUrsodeoxycholic acid (UDCA) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. UDCA is also a long-established drug, largely used for the dissolution of cholesterol gallstones, the treatment of primary biliary cholangitis and other hepatobiliary disorders. The history of UDCA is briefly retraced here as well as its multifac...
Source: Pharmacology and Therapeutics - Category: Drugs & Pharmacology Source Type: research
Abstract BACKGROUND: The liver is affected by two of the most common groups of malignant tumours: primary liver tumours and liver metastases from colorectal carcinoma. Liver metastases are significantly more common than primary liver cancer and long-term survival rates reported for patients after radical surgical treatment is approximately 50%. However, R0 resection (resection for cure) is not feasible in the majority of patients. Cryotherapy is performed with the use of an image-guided cryoprobe which delivers liquid nitrogen or argon gas to the tumour tissue. The subsequent process of freezing is associated with...
Source: Cochrane Database of Systematic Reviews - Category: General Medicine Authors: Tags: Cochrane Database Syst Rev Source Type: research
In this study, gene expression profile is used for discriminating efficiently colon cancer cell lines from normal cells and cancer cells in blood samples of colon cancer patients and categorizing different types of gastrointestinal cancer. In particular, blood samples were collected from normal donors as well as from colon cancer patients. Peripheral blood mononuclear cells were isolated and gene expression analysis was performed for more than fifty genes. The same assays were performed for commercial cancer cell lines representing different types of gastrointestinal cancer. In order to examine whether the comparison of ge...
Source: Oncotarget - Category: Cancer & Oncology Tags: Oncotarget Source Type: research
Publication date: Available online 5 June 2019Source: Biosensors and BioelectronicsAuthor(s): MaríaG.H. Rangel, M. Luísa S. SilvaAbstractAn impedimetric biosensor was developed for the selective detection of the cancer-associated T antigen, using the lectin from Arachis hypogaea (peanut agglutinin, PNA) as the recognition element. The increase in the biosensor's impedance after sample incubation was indicative of lectin recognition and complex formation between PNA and glycoproteins containing T antigen. When using asialofetuin as model glycoprotein, a minimum amount of 100 ng of glycoprotein could be detec...
Source: Biosensors and Bioelectronics - Category: Biotechnology Source Type: research
Abstract The study aimed to estimate cancer mortality among indigenous peoples in Acre State, Brazil. This was a descriptive observational study based on the nominal bank of the Brazilian Mortality Information System for the period from January 1st, 2000, to December 31st, 2012. The study analyzed the distribution death frequencies by sex and age. Standardized mortality ratio (SMR) was calculated taking Goiânia (Goiás State), Acre State, and the North Region of Brazil as the references. A total of 81 deaths were identified, the majority in men (59.3%) and in individuals over 70 years of age. The five ...
Source: Cadernos de Saude Publica - Category: International Medicine & Public Health Authors: Tags: Cad Saude Publica Source Type: research
CONCLUSIONS: Our results suggest a reduced susceptibility to develop cancers, mostly of endodermal origin (stomach, colon and liver), but not of ectodermal/mesodermal origin, in carriers of G6PD deficiency. The effects of G6PD deficiency on carcinogenesis need further studies to better understand how cancer cells originating from different germ layers use pentose phosphate pathway to proliferate. PMID: 31109224 [PubMed - as supplied by publisher]
Source: Acta Oncologica - Category: Cancer & Oncology Authors: Tags: Acta Oncol Source Type: research
Conclusions: Based on the findings in this study, we suggest that FDG PET/MR might be an effective cancer screening modality in appropriate combination with other screening modalities. Table 1. Age distribution of subject and cancer detection rate in each age groupAgeNumber of subjects and percentage (%)Number with cancer and detection rate (%)20-2953 (1.90)1(1.49)30-39348(12.46)9(13.43)40-49996(35.65)15(22.39)50-59957(34.25)28(41.79)60-69361(12.92)11(16.42)70-7966(2.36)2(2.99)80 and above13(0.47)1(1.49)total2974 (100)67Table 2. 5 of 12 False positive cases detected by PET/MRNO.AgeSexorganHistological diagnosisMethods of c...
Source: Journal of Nuclear Medicine - Category: Nuclear Medicine Authors: Tags: Other Solid Tumors/ Hematologic Malignancies (Clinical) II Source Type: research
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