Synthesis and evaluation of new 4(3H)-Quinazolinone derivatives as potential anticancer agents

Publication date: Available online 19 September 2019Source: Journal of Molecular StructureAuthor(s): Srikanth Gatadi, Gauthami Pulivendala, Jitendra Gour, Satyaveni Malasala, Sushmitha Bujji, Ramulu Parupalli, Mujahid Shaikh, Chandraiah Godugu, Srinivas NanduriAbstractA series of new 4(3H)-quinazolinones were synthesized and evaluated for their cytotoxic activity against a set of human cancer cell lines MDA-MB-231 and MCF-7 (breast), HCT-116 and HT-29 (colon) and A549 (lung). Among the tested compounds, 22a exhibited promising cytotoxic activity against MDA-MB-231 (IC50: 3.21μM) and HT-29 (IC50: 7.23 μM) cell lines. The mechanism of action and the apoptosis inducing effect of the compound 22a were studied using the breast cancer cell line MDA-MB-231. Treatment of MDA-MB-231 cell line with compound 22a showed typical apoptotic morphology like cell shrinkage, chromatin condensation and horseshoe shaped nuclei formation. Flow cytometric analysis indicated that the compound induces G0/G1 phase of cell cycle arrest in a dose dependent manner. The binding modes of the potent compounds with EGFR target protein were investigated by docking studies.Graphical abstract
Source: Journal of Molecular Structure - Category: Molecular Biology Source Type: research

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CONCLUSION: The specific tumor profile in DS warrants an adapted screening program for breast, colon, cervical and testicular neoplasia. PMID: 31605815 [PubMed - as supplied by publisher]
Source: European Journal of Medical Genetics - Category: Genetics & Stem Cells Authors: Tags: Eur J Med Genet Source Type: research
ConclusionsDevelopment of PD-1 B-cell vaccine was successful, showing no evidence of toxicity or autoimmunity in mice, rabbits and beagle dogs. The combination vaccines could provide improved outcomes in early stage disease sparing patients the toxicity of chemotherapy. A phase 1 clinical trial with the PD-1 vaccine is under planning.Legal entity responsible for the studyThe authors.FundingNIH; Imugene.DisclosureAll authors have declared no conflicts of interest.
Source: Annals of Oncology - Category: Cancer & Oncology Source Type: research
Publication date: 1 January 2020Source: Sensors and Actuators B: Chemical, Volume 302Author(s): A. Zuchowska, A. Buta, B. Dabrowski, E. Jastrzebska, K. Zukowski, Z. BrzozkaAbstractMicrofluidic Lab-on-a-Chip systems have gained a lot of interest in cellular research. Currently, two- (2D) and three-dimensional (3D) cancer cell cultures are carried out under microfluidic conditions as new culture models. Mostly, they are used for the evaluation of cancer metastasis and effectiveness of anticancer therapy. Herein, we present a novel microfluidic tool for cancer cell cultures as 2D monolayer and 3D - spheroids simultaneously. T...
Source: Sensors and Actuators B: Chemical - Category: Chemistry Source Type: research
Publication date: 5 January 2020Source: Journal of Molecular Structure, Volume 1199Author(s): Walaa H. El-Shwiniy, Wesam S. Shehab, Wael A. ZordokAbstractThree novel metal complexes of 4-Amino-6-oxo-5-thiophen-2-yl-8-thioxo-3,5,6,7,8,9-hexahydro-4Hpyrano[2,3-d; 6,5d']dipyrimidin-2-yl)-acetonitrile(L1),5-Thiophen-2-yl-2-thioxo-2,3,5,7-tetrahydro-1H-pyrano[2,3-d; 6,5-d']dipyrimidine-4,6-dione (L2) and 6-Amino-5-thiophen-2-yl-2-thioxo-1,2,3,5-tetrahydro-pyrano[2,3-d; 6,5-d']dipyrimidin-4-one (L3) with Mn(II) were synthesized and characterized with physicochemical and spectroscopic techniques. The electron density of HOMOs is ...
Source: Journal of Molecular Structure - Category: Molecular Biology Source Type: research
ConclusionsAlcohol consumption was minimally associated with all-cancer risk. Cigarette smoking clearly increased all-cancer risk, with females being more affected than males. Combined use of alcohol and tobacco increased the risk of developing all, colon, and prostate cancers. A “U-shaped” multiplicative interaction was observed for breast cancer when alcohol and tobacco were used in combination.
Source: Cancer Causes and Control - Category: Cancer & Oncology Source Type: research
In this study, the subcellular localization of cripto-1 in glioblastoma cells was investigated in vitro with high-resolution microscopy techniques. Cripto-1 was found to be localized to dynamic and shed filopodia and transported between cells through tunneling nanotubes. Our results connect the refined subcellular localization of cripto-1 to its functions in cellular orientation and migration. PMID: 31543278 [PubMed - as supplied by publisher]
Source: European Journal of Cell Biology - Category: Cytology Authors: Tags: Eur J Cell Biol 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
Cancer survival rates for esophagus, stomach, colon, rectum, pancreas, lung,...Read more on AuntMinnie.comRelated Reading: AI predicts lung cancer survival from CT scan data Lancet: Cancer survival rates improve but vary widely Cancer deaths continue to fall, but CT lung screening lags ACS: U.S. cancer death rates continue to fall NEJM: Treatment, not screening, cuts breast cancer deaths
Source: AuntMinnie.com Headlines - Category: Radiology Source Type: news
The stimulator of IFN genes (STING) signaling pathway is a critical link between innate and adaptive immunity and induces antitumor immune responses. STING is expressed in vasculatures, but its role in tumor angiogenesis has not been elucidated. Here, we investigated STING-induced tumor vascular remodeling and the potential of STING-based combination immunotherapy. Endothelial STING expression was correlated with enhanced T cell infiltration and prolonged survival in human colon and breast cancer. Intratumoral STING activation with STING agonists (cGAMP or RR-CDA) normalized tumor vasculatures in implanted and spontaneous ...
Source: Journal of Clinical Investigation - Category: Biomedical Science Authors: 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
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