Design, synthesis and biological evaluation of novel furoxan-based coumarin derivatives as antitumor agents

AbstractIn order to find new anticancer drugs, a series of novel furoxan-based coumarin derivatives (10a–k) were synthesized and evaluated for their antiproliferative activities in vitro. All compounds displayed more potent inhibition on human cervical cancer HeLa cell proliferation than coumarin-3-carboxylic acid, and compounds10b, 10c, 10f, 10h, and10i with IC50 values ranging from 0.88 to 5.95  μM were even stronger than doxorubicin (IC50 = 10.21 μM). The further study showed that compound10i exerted the highest antiproliferative activity (IC50 = 0.60 μM) against human breast cancer MCF-7 cells, and compound10f had broader spectrum antiproliferative activity against five cancer cells with IC50 values in the low micromolar range of 1.86 –9.85 μM. More interestingly, compound10f had little effect on normal intestinal epithelial CCD841 cells. Our findings suggest that these novel furoxan-based coumarin derivatives may provide a new framework for the discovery of novel antitumor agents for the intervention of human carcinoma cells.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research

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Contributors : Naohiko Seki ; Yasutaka YamadaSeries Type : Expression profiling by arrayOrganism : Homo sapiensTo identify differentially expressed genes by anti cancer treatments (siRNAs) in human cancer, several cell lines (lung cancer, breast cancer and pancreatic cancer) were subjected to Agilent whole genome microarrays.
Source: GEO: Gene Expression Omnibus - Category: Genetics & Stem Cells Tags: Expression profiling by array Homo sapiens Source Type: research
Abstract Opisthorchiasis is a neglected tropical disease, caused by infection with the fish-borne trematode Opisthorchis viverrini sensu lato that afflicts more than 10million people in Southeast Asia, including Thailand, Lao PDR, Vietnam and Cambodia. The disease is characterized by a chronic infection that induces hepatobiliary inflammation, especially periductal fibrosis, which can be detected by ultrasonography. This chronic inflammation eventually leads to cholangiocarcinoma (CCA), a usually fatal bile duct cancer that develops in approximately 1% of O. viverrini-infected individuals. In Thailand alone, CCA k...
Source: Advances in Parasitology - Category: Parasitology Authors: Tags: Adv Parasitol Source Type: research
Abstract Innate, inflammatory responses towards persistent Opisthorchis viverrini (OV) infection are likely to contribute to the development of cholangiocarcinoma (CCA), a liver cancer that is rare in the West but prevalent in Greater Mekong Subregion countries in Southeast Asia. Infection results in the infiltration of innate immune cells into the bile ducts and subsequent activation of inflammatory immune responses that fail to clear OV but instead may damage local tissues within the bile ducts. Not all patients infected with OV develop CCA, and so tumourigenesis may be dependent on multiple factors including th...
Source: Advances in Parasitology - Category: Parasitology Authors: Tags: Adv Parasitol Source Type: research
Abstract Opisthorchiasis is a neglected tropical disease of major proportion, caused by the carcinogenic, Asian liver fluke, Opisthorchis viverrini. This hepatobiliary disease is known to be associated with malignant cancer (cholangiocarcinoma, CCA) and affects millions of people in Southeast Asia. No vaccine is available, and only one drug (praziquantel) is routinely employed against the parasite. Despite technological advances, little is known about the molecular biology of the fluke itself and the disease complex that it causes in humans. The advent of high-throughput nucleic acid sequencing and bioinformatic t...
Source: Advances in Parasitology - Category: Parasitology Authors: Tags: Adv Parasitol Source Type: research
BACKGROUND: An elevated risk of suicide after a diagnosis of prostate cancer has been reported previously in the USA and Sweden. We aimed to identify whether prostate cancer survivors resident in New South Wales Australia are at higher risk of suicide and ...
Source: SafetyLit - Category: International Medicine & Public Health Tags: Suicide and Self-Harm Source Type: news
The onset of diabetes after the age of 50 could be an early sign of pancreatic cancer, a new study suggests.
Source: CNN.com - Health - Category: Consumer Health News Source Type: news
PROSTATE cancer symptoms are triggered by a cancerous growth in this part of the male reproductive system. Early warning signs tend to include problems urinating, as the prostate tumour presses on the tubes for carrying urine. Watch out for these symptoms.
Source: Daily Express - Health - Category: Consumer Health News Source Type: news
UK Health Secretary Jeremy Hunt will give the go-ahead for them to be inoculated against the cancer-causing human papillomavirus, which causes cancer that kills 650 men a year.
Source: the Mail online | Health - Category: Consumer Health News Source Type: news
AbstractBackgroundCervical cancer is one of the most common malignant tumours of the female reproductive system, ranking second only to breast cancer in morbidity worldwide. Essential features of the progression of cervical cancer are invasion and metastasis, which are closely related to disease prognosis and mortality rate. At the present time there is no effective method to evaluate cancer invasion and metastasis before surgery. Here we report our study on molecular changes in biopsy tissue for the prognostic evaluation of cancer invasion and metastasis.Patients and methodsExpression of the epithelial –mesenchymal ...
Source: International Journal of Clinical Oncology - Category: Cancer & Oncology Source Type: research
AbstractA series of twelve 4-methyl-2-(2-, 3- and 4-pyridinyl)quinolines7 –9 was synthesized using modified Kametani reaction protocol and their in vitro cytotoxicity was tested against human cancer cell lines MCF-7, SKBR-3, PC3, HeLa, comparing with human dermis fibroblast as non-tumor cells. In general, these molecules displayed potent anticancer properties, but also demonstrated a narrow safe margin, as it was observed for doxorubicin. Compounds8a,8b,9a and9d showed prominent selective cytotoxicity with higher IC50 values compared with reference drug doxorubicin in prostate carcinoma, cervical epithelial carcinoma...
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research
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