Abstract：
BACKGROUND/AIM:Quinazolinone is a privileged chemical structure employed for targeting various types of cancer. This study aimed to demonstrate the antitumor activity of synthesized 6,7-disubstituted-2-(3-fluorophenyl) quinazolines (HoLu-11 to HoLu-14). MATERIALS AND METHODS:The cytotoxicity was assessed by the sulforhodamine B (SRB) assay. The cell cycle was examined by flow cytometry. The expression levels of cell cycle- and apoptosis-related proteins were estimated by western blotting. A xenograft animal model was used to explore the antitumor effects of HoLu-12. RESULTS:Among four synthetic quinazolinone derivatives, HoLu-12 significantly reduced the viability of oral squamous cell carcinoma (OSCC) cells. HoLu-12 induced G2/M arrest and increased the expression of cyclin B, histone H3 (Ser10) phosphorylation, and cleaved PARP, indicating that HoLu-12 could induce mitotic arrest and then apoptosis. Moreover, the combination of HoLu-12 and 5-fluorouracil (5-FU) displayed synergistic toxic effect on OSCC cells. HoLu-12 significantly inhibited tumor growth in vivo. CONCLUSION:HoLu-12 induces mitotic arrest and leads to apoptosis of OSCC cells. Furthermore, HoLu-12 alone or in combination with 5-FU is a potential therapeutic agent for OSCC.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Lai KC,Chia YT,Yih LH,Lu YL,Chang ST,Hong ZX,Chen TL,Hour MJdoi
10.21873/anticanres.14772subject
Has Abstractpub_date
2021-01-01 00:00:00pages
259-268issue
1eissn
0250-7005issn
1791-7530pii
41/1/259journal_volume
41pub_type
杂志文章abstract：:Colchicine is an alkaloid widely used for the treatment of inflammatory diseases, such as gout. It suppresses cell division by inhibiting mitosis. We investigated the anticancer effects of colchicine on human hypopharyngeal cancer cells and the mechanisms underlying its anticancer effects. XTT cell proliferation assay...
journal_title：Anticancer research
pub_type： 杂志文章
doi：10.21873/anticanres.12078
更新日期：2017-11-01 00:00:00
abstract：BACKGROUND:Since the anti-HER2 monoclonal antibody trastuzumab made its triumphant advance into breast cancer therapy, new selective agents, including pan-HER inhibitors are entering clinical practice. MATERIALS AND METHODS:This study investigates the expression of the four HER-family members, HER1-4, in 48 primary br...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2006-11-01 00:00:00
abstract：BACKGROUND:The upper outer quadrant (UOQ) of the breast is the most frequent site for incidence of breast cancer, but the reported disproportionate incidence in this quadrant appears to rise with year of publication. MATERIALS AND METHODS:In order to determine whether this increasing incidence in the UOQ is an artifac...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2005-05-01 00:00:00
abstract：:Evidence has been presented that tumor suppressor genes p53 and Rb play a crucial role in the development of both human prostate and bladder cancer. Patients with either cancer are at an increased risk for developing the other malignancy as compared to the general population. The purpose of the present study was to in...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1999-11-01 00:00:00
abstract：:This report describes a precise molecular analysis of a rare case of Philadelphia chromosome (Ph) positive acute myeloid leukemia (AML) (FAB classification M2). Phenotypic markers were positive for cells of the myeloid lineage, but negative for B cell and T cell lineage. The leukemic cells carried a Philadelphia chrom...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1997-01-01 00:00:00
abstract：:A universal intracellular factor, the "M phase-promoting factor" (MPF), triggers the G2/M transition of the cell cycle in all organisms. In late G2, it is present as an inactive complex of tyrosine-phosphorylated p34cdc2 and unphosphorylated cyclin Bcdc13. In M phase, its activation as an active MPF displaying histone...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1992-05-01 00:00:00
abstract：BACKGROUND/AIM:Biosimilar agents are biologic products that have no clinically meaningful differences in terms of quality, efficacy, safety and immunogenicity compared to an already approved reference biological product, with the potential to reduce the costs of biologics. Considering the increasing numbers of oncology...
journal_title：Anticancer research
pub_type： 杂志文章
doi：10.21873/anticanres.13552
更新日期：2019-07-01 00:00:00
abstract：:The purpose of this study was to investigate the nature of the action of N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) as the modulator of gene expression. Practically, both the acceleration of daily liquid consumption following salt-hydrocortisone conditioning (sea water adaptation phenomenon) and the suppressive effec...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1992-03-01 00:00:00
abstract：:In-111 pentetreotide is a new radiolabelled [OctreoScan 111, Mallinckrodt Medical BV, Petten] somatostatin analog with high affinity to somatostatin receptors (SR). introduced for the in vivo imaging of SR positive tissues. In an attempt to evaluate its clinical usefulness for tissue characterization in malignancies w...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1997-05-01 00:00:00
abstract：:This study is a sequel in our continuing efforts to improve the colony forming efficiency of the Human Tumor Colony Assay. We have previously reported that the use of culture media supplemented with rat red blood cells and a low oxygen environment resulted in notable improvements in the clonal growth of three differen...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1987-05-01 00:00:00
abstract：:Using a cultured human colon cancer cell line (Col 2), a structurally diverse group of chemopreventive agents was evaluated for their potential to induce apoptosis. As a result, 1,4-phenylenebis(methylene)selenocyanate (p-xylylselenocyanate; p-XSC) was found to be active in this process. p-XSC, a synthetic organoselen...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2002-01-01 00:00:00
abstract：:The cyclin-dependent kinase inhibitor p21WAF1 participates in cell growth, differentiation, and apoptosis. p21WAF1 can be induced by green tea polyphenol EGCG in several cancer cell types, but its role in the oral cancer cell response to EGCG is not known. We found that EGCG upregulates p21WAF1 in an oral carcinoma ce...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2005-01-01 00:00:00
abstract：BACKGROUND:It is unclear whether radiomic phenotypes of brain metastases (BM) are related to radiation therapy prognosis. This study assessed whether a convolutional neural network (CNN)-based radiomics model which learned computer tomography (CT) image features with minimal preprocessing, could predict early response ...
journal_title：Anticancer research
pub_type： 杂志文章
doi：10.21873/anticanres.12875
更新日期：2018-09-01 00:00:00
abstract：:In a population-based study of posterior uveal malignant melanoma (755 incidence cases), the authors found a stabilized incidence in Israel from 1961-1996. Overall, Jewish immigrants to Israel had a relative rate (RR) of 2.2 [95% confidence interval [1.5-2.6] as compared to the reference population (Israeli-born Jews ...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2001-03-01 00:00:00
abstract：BACKGROUND:Chemotherapy is considered to have a marginal impact on survival. The purpose of this study was to evaluate the rate of long-term survival in patients treated with chemotherapy for advanced non-small cell lung cancer (NSCLC). PATIENTS AND METHODS:The case records of 109 patients with NSCLC treated with chem...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2007-11-01 00:00:00
abstract：:We have previously reported the presence of human beta-defensin-2 (HBD-2), a peptide with antimicrobial and cytotoxic properties, in oral squamous cell carcinomas. The aim of the present study was to measure the concentration of HBD-2 in abnormal tissues such as oral squamous cell carcinomas. HBD-2 was extracted from ...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2002-07-01 00:00:00
abstract：BACKGROUND:Mistletoe lectins (MLs) are the active components of aqueous mistletoe extracts widely used in complementary cancer therapy, however, it is not clear if they bind to carbohydrate residues only or whether they interact with proteins as well. Protein-protein interactions do not seem unlikely as MLs act at very...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2009-12-01 00:00:00
abstract：:Eldecalcitol [1α,25-dihydroxy-2β-(3-hydroxypropoxy)vitamin D(3)], an analog of calcitriol (1α,25-dihydroxyvitamin D(3)), possesses a hydroxypropoxy substituent at the 2β-position of calcitriol. Eldecalcitol has potent biological effects on bone disease such as osteoporosis. The marketing of eldecalcitol has very recen...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2012-01-01 00:00:00
abstract：BACKGROUND:Early detection before scintigraphic appearance of osseous metastatic spread might improve the outcome of breast cancer patients. The amino-terminal propeptide (PINP) of type I collagen as an indicator of bone formation is a very promising candidate among all markers of bone metabolism. We investigated the u...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2005-05-01 00:00:00
abstract：:Macrophages are thought to be the cells that initially respond to environmental information and transmit this information to other immune cells. We hypothesize that there is a "network system" consisting of various tissue macrophages; the macrophages respond to stimulation and transmit secondary information to neighbo...
journal_title：Anticancer research
pub_type： 杂志文章,评审
doi：
更新日期：2006-11-01 00:00:00
abstract：:Induction of apoptosis by green tea polyphenols has been observed in various tumor cell systems, but whether green tea polyphenol-induced apoptosis requires caspase 3 for execution has not been confirmed. We previously reported that green tea polyphenol-induced apoptosis involved Apaf-1 accumulation and caspase 3 acti...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2003-03-01 00:00:00
abstract：BACKGROUND:Carcinoma of the ampulla of Vater is an infrequent tumor that can be diagnosed, early. PATIENTS AND METHODS:Twenty-four patients with histologically proven carcinoma of the ampulla of Vater were retrospectively studied and their data were analyzed. RESULTS:Most common presenting symptoms were jaundice (67%...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1999-09-01 00:00:00
abstract：BACKGROUND:Pure or metaplastic squamous cell carcinoma (SCC) of the breast is a rare entity with an unclear pathogeny and aggressive clinical behaviour. An attempt was made to characterize its differential immunohistochemical and biological profile. PATIENTS AND METHODS:Twenty-seven cases of SCC (pure or not) of the b...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2007-01-01 00:00:00
abstract：:Cisplatin is one of the most widely used and effective chemotherapeutic agents for the treatment of several human malignancies. Although the effectiveness of cisplatin is high, its toxicities justify the demand for improved formulations of this drug. A liposomal formulation of cisplatin, Lipoplatin, was developed in o...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2004-07-01 00:00:00
abstract：:A female patient with stage IV-M1c (distant lymph node and breast metastases), chemotherapy-refractory melanoma was treated with the cytotoxic T-lymphocyte antigen 4 (CTLA-4)-inhibitory monoclonal antibody ipilimumab. At first evaluation following induction treatment, there was marked increase in the volume of the lym...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2012-04-01 00:00:00
abstract：BACKGROUND/AIM:Long-term results of a study investigating potential prognostic factors for treatment outcomes in patients with stage III esophageal cancer are presented. PATIENTS AND METHODS:In 64 patients, the impact of tumor cell expression of erythropoietin (EPO) and erythropoietin-receptor (EPO-R) and ten addition...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2014-08-01 00:00:00
abstract：BACKGROUND:Pathological examination of sentinel lymph nodes (SLNs) and non-SLNs in colon cancer is frequently not performed to the same extent. We examined whether non-SLNs were truly negative in tumors with tumor-negative SLNs using reverse transcriptase-polymerase chain reaction (RT-PCR). PATIENTS AND METHODS:RT-PCR...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2007-07-01 00:00:00
abstract：BACKGROUND/AIM:Invasive bladder cancer mortality remains high despite progresses made in early diagnosis and surgical procedures. Thus, there is a need to define new markers for bladder cancer. CLIC1 has not been previously studied in bladder cancer and thus, we aimed to assess its immunohistochemical expression in rel...
journal_title：Anticancer research
pub_type： 杂志文章
doi：10.21873/anticanres.14710
更新日期：2020-12-01 00:00:00
abstract：BACKGROUND/AIM:Ras-related associated with diabetes (RRAD), a member of the Ras-related GTPase superfamily, is frequently methylated in several human cancers, though its methylation profile remains unclear in esophageal cancer. MATERIALS AND METHODS:We examined RRAD promoter hypermethylation using real-time quantitati...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2013-11-01 00:00:00
abstract：BACKGROUND:Recently, we reported on the existence of activated protein kinase Cα (PKCα) in blood and the possibility for its use in cancer diagnosis. MATERIALS AND METHODS:In the present study, serum samples collected from patients with different lung cancer types (small-cell cancer, adenocarcinoma, and anaplastic can...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2013-02-01 00:00:00
