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A biocompatible fluorogenic chemosensor (N-(3-carboxy acryloyl)) rhodamine B (RHA) comprising a furan-2,5-dione receptor and a rhodamine fluorophore via an iminohydrazine crosslinker has been prepared for more scrutinizing optical properties and utilization in molecular imaging of living cells. The consequences indicated that RHA not only is a good pH indicator in acidic media but also can be used as a great sensitive fluoroionophore with high selectivity. The fluorescence emission of the molecule RHA is quite stable in the presence of 15 diverse cations, 18 anions (especially H 2 PO 4 - , S 2 , and F - ), and 5 amino acids with the different functional group as a model, except Cu 2+ ions with observable emission intensity changing. The Cu 2+ probe has a dual functional effect, an "on-off" mechanism in solvent media, and an "off-on" mechanism in Phosphate Buffered Saline (PBS) in acidic pH conditions. The detection limits for Cu 2+ in acetone-water media was 0.69 μM and 0.18 μM in pH = 5.0. Moreover, RHA can fluorescently and colorimetrically image Cu 2+ ions in acidic and neutral pH with low cytotoxicity in living cells., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: This work was supported by National Institute for medical research development, NIMAD, with the foundation number of 957590. We would like to thank our colleagues in Motamed Cancer Institute for providing a good contribution in all aspects of the project., (Copyright © 2019 Elsevier B.V. All rights reserved.)

A series of 4-amino-5-cinnamoylthiazoles 3a-p were designed and synthesized as chalcone-like anticancer agents. The synthesized derivatives 3a-p were evaluated for their in vitro antiproliferative activities against three different human cancer cell lines including MCF-7, HepG2 and SW480. Most of compounds could significantly prevent proliferation of tested cell lines. In particular, the pyrrolidine derivative 3e namely ( E )-1-(4-amino-2-(pyrrolidin-1-yl)thiazol-5-yl)-3-(2,4-dichlorophenyl)prop-2-en-1-one showed promising activity, especially against HepG2 cells (IC 50  = 10.6 μg/ml). Flow cytometric analyses revealed that the prototype compound 3e can prevent the proliferation of HepG2 cells by blockade of the cell cycle at the G2 phase and induction of apoptosis. [ABSTRACT FROM AUTHOR]

Purpose: Bone marrow-derived mesenchymal stem cells (MSCs) have the potential ability to differentiate into bone, muscle, fat, and cartilage lineage cells. Furthermore, MSCs are known to migrate into tumor-associated stroma of cancer. This tumor microenvironment consists of a dynamic network of growth factors, immune cells, fibroblasts, extracellular matrix, and MSCs. MSCs as nonhematopoietic stem cells affect tumor, epithelial cells by alteration proliferative capacity, morphology, and aggregation pattern of tumor cells. Materials and Methods: This research aimed to further elucidate the MSCs effects in the progress of proliferation, cell cycle, and apoptosis in breast cancer by gene expression analysis in human breast cancer cell lines exposed to MSCs conditioned media (CM). Expression pattern of two genes, including survivin (Birc5) as anti-apoptotic gene and serine threonine kinase 15 as proliferative gene, were studied. Results: Anti-apoptotic and proliferative genes were up-regulated in co-cultured breast tumor cells with MSCs-CM that correlate with tumor progression and poor prognosis. Conclusion: Our results and other findings indicate the interaction of breast tumor cells with MSCs through paracrine factors. Also, the applications of MSCs as therapeutic tools are facing controversial concerns. [ABSTRACT FROM AUTHOR]

Inhibition of angiogenesis is a promising strategy for the treatment of cancer. Herein, we describe the design and synthesis of thieno[2,3- d pyrimidine-1,3,4-thiadiazole-aryl urea derivatives 11a-m to evaluate their efficacy in the chick chorioallantoic membrane (CAM) assay. Among target agents, 11i had a considerable activity against prostate cancer cell line, PC3 (IC 50 = 3.6 μ M). Moreover, induction of apoptosis, good inhibitory activity against the growth of capillary blood vessels, and inhibition of VEGFR-2 phosphorylation were noticeable parameters which convinced us that 11i could be considered as a promising candidate for the discovery of novel drugs to treat tumors, particularly prostate cancer. Image 1 • Thienopyrimidine-based compounds bearing the diaryl urea functionality were designed and synthesized. • 11i could inhibit the proliferation of PC3 cells by nearly 4-fold, respectively compared to sorafenib. • CAM assay revealed that the growth of blood vessels was inhibited by 11i tremendously. • Western blot analysis of 11i revealed the inhibition of VEGFR-2 phosphorylation. [ABSTRACT FROM AUTHOR]