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Anti-cancer Agents in Medicinal Chemistry

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https://www.readbyqxmd.com/read/27928955/discovery-of-new-aminosubstituted-pyrrolopyrimidines-with-antiproliferative-activity-against-breast-cancer-cells-and-investigation-of-their-effect-towards-the-pi3k%C3%AE-enzyme
#1
Konstantinos Daniilides, Nikolaos Lougiakis, Thomas Evangelidis, Ioannis K Kostakis, Nicole Pouli, Panagiotis Marakos, Emmanuel Mikros, Alexios-Leandros Skaltsounis, Stéphane Bach, Blandine Baratte, Sandrine Ruchaud, Valia Karamani, Alexandra Papafotika, Savvas Christoforidis, Orestis Argyros, Eva Kouvari, Constantin Tamvakopoulos
A series of novel 2,4-diaminosubstituted pyrrolo[3,2-d]pyrimidines was synthesized together with their corresponding 7-phenyl or 7-isopropyl counterparts. Among the target derivatives, the 7-substituted analogues exhibited interesting cytotoxic activity against a panel of PI3Kα related human breast cancer cell lines, namely MCF7, T47D, MDA-MB-231 and HCC1954. Selected compounds were tested for potential PI3Kα inhibitory activity as well as for their cytotoxic effect in prostate cancer cell lines (DU145 and PC3)...
December 7, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27928954/ring-a-modified-derivatives-from-the-natural-triterpene-3-o-acetyl-11-keto-%C3%AE-boswellic-acid-and-their-cytotoxic-activity
#2
Tao Li, Peihong Fan, Yaqing Ye, Qian Luo, Hongxiang Lou
BACKGROUND: Natural triterpene boswellic acids (BAs) have attracted much interest due to their anticancer activity, but more chemical modification is necessary to explore their pharmacological value. In addition to subtle functionalization, transformations that alter the triterpene skeleton are viewed as an alternative approach. OBJECTIVE: In this study, transformations altering ring A of 3-O-acetyl-11-keto-β-boswellic acid (AKBA) were performed to obtain A-lactone, A-lactam, A-seco and A-contracted derivatives...
December 7, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27928953/novel-hybrid-molecules-on-the-basis-of-steroids-and-5z-9z-tetradeca-5-9-dienoic-acid-synthesis-anti-cancer-studies-and-human-topoisomerase-i-inhibitory-activity
#3
Vladimir A D Yakonov, Lilya U Dzhemileva, Regina A Tuktarova, Svetlana R Ishmukhametova, Milyausha M Yunusbaeva, Ilfir R Ramazanova, Usein M Dzhemilev
Novel steroid derivatives of 5Z,9Z-dienoic acids were prepared by the DCC/DMAP-catalyzed esterification of (5Z,9Z)-tetradeca-5,9-dienoic acid with hydroxy steroids. High cytotoxicity towards the HEK293, Jurkat, K562 cancer cell lines and human topoisomerase I (hTop1) inhibitory activity in vitro were found for the synthesized acids. A probable mechanism of topoisomerase I inhibition was hypothesized on the basis of in silico studies resorting to docking.
December 7, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27928952/in-vitro-anticancer-evaluation-of-platinum-ii-iv-complexes-with-diisoamyl-ester-of-s-s-ethylenediamine-n-n-di-2-propanoic-acid
#4
Bojana B Zmejkovski, Nebojša Pantelić, Lana Filipović, Sandra Aranđelović, Siniša Radulović, Tibor J Sabo, Goran N Kaluđerović
Platinum(II) and platinum(IV) complexes [PtCln{(S,S)-(i-Am)2eddip}] (n = 2, 4: 1, 2, respectively; (S,S)-(i-Am)2eddip = O,O'-diisoamyl-(S,S)-ethylenediamine-N,N'-di-2-propanoate) were synthesized and characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy and mass spectrometry. Quantum chemical calculations were used to predict formed isomers of 1 and 2. Furthermore, reduction of 2 with ascorbic acid was followed by time-dependant 13C NMR spectroscopy in order to enable assignation of the formed isomers for complex 1...
December 7, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27924733/design-and-synthesis-of-1-4-dihydropyridine-derivatives-as-anti-cancer-agent
#5
Denish Viradiya, Sheefa Mirza, Faraz Shaikh, Rajesh Kakadiya, Anand Rathod, Nayan Jain, Rakesh Rawal, Anamik Shah
A series of 1,4-dihydropyridine based compounds bearing benzylpyridinium moiety have been designed and evaluated for in vitro anticancer activity against glioblastoma U87MG, lung cancer A549 and colorectal adenocarcinoma Caco-2 cell lines using the MTT assay. Among these compounds, 7b, 7d, 7e, and 7f exhibited potent anticancer activity against the cell lines tested. The cytotoxicity of the synthesized derivatives was compared to standard drugs (carboplatin, gemcitabine, and daunorubicin). Thus, synthesized 1,4-dihydropyridines can be considered as the encouraging molecules for further drug development as anticancer agents...
December 6, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27924732/the-effect-of-a-hexanoic-acid-linker-insertion-on-the-pharmacokinetics-and-tumor-targeting-properties-of-the-melanoma-imaging-agent-99mtc-hynic-cycmsh
#6
Vania Teixeira, Marcelo Fernández, Natalia Oddone, Xiuli Zhang, Fabio Gallazzi, Hugo Cerecetto, Juan Pablo Gambini, Williams Porcal, Pablo Cabral, Thomas P Quinn
BACKGROUND: Lactam cyclized alpha-melanocyte stimulating hormone (α-MSH) analogues exhibit high stability and affinity for the MC1-R receptors over expressed in melanoma cells. Recently, we reported a novel <sup>99m</sup>Tc-HYNIC-cycMSH<sub>4-13</sub> analogue with the HYNIC chelator directly attached to the lactam cyclized ring. OBJECTIVE: In this study we proposed the introduction of a 6-aminohexanoic acid (Ahx) linker between the HYNIC chelator and lactam cyclized peptide cycMSH4-13 to reduce steric hindrance and improve the melanoma targeting and imaging proprieties of the radiolabeled peptide...
December 6, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27924731/improved-immunogenicity-against-a-her2-neu-derived-peptide-by-employment-of-a-pan-hla-dr-binding-epitope-and-cpg-in-a-balb-c-mice-model
#7
Sahar Tahaghoghi-Hajghorbani, Jalil Tavakkol-Afshari, Mahmoud Reza Jaafari, Haniyeh Ghaffari-Nazari, Elham Masoumi, Seyed Amir Jalali
BACKGROUND: An efficient strategy to improve the immunogenicity of peptide vaccines is the use of a synthetic peptide containing cytotoxic T-lymphocyte (CTL) epitopes with T-helper (Th) inducing-epitopes. OBJECTIVE: Our purpose was to determine the use of human epidermal growth factor receptor-2 (Her2/neu)-specific CTL epitopes plus the pan HLA DR-binding epitope (PADRE) and CpG oligodeoxynucleotides (ODNs) to induce antitumor effects in vaccinated mice. METHOD: Female BALB/c mice were immunized with subcutaneously the different vaccines...
December 6, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27924730/congenital-malformations-attributed-to-prenatal-exposure-to-cyclophosphamide
#8
Padmanabhan Rengasamy
Cyclophosphamide (CPA) remains one of the most widely prescribed anticancer drugs. It is also used in the treatment of rheumatoid arthritis, childhood nephrotic syndrome and systemic lupus erythematosus. It is a potent immunosuppressive agent. It is commonly used in blood and bone marrow transplantation. With the growing trend among women postponing childbearing, the number of women who are diagnosed with breast cancer is also increasing thus escalating the chances of exposure of the unborn child to antineoplastic drugs...
December 6, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27804848/novel-1-2-4-triazol-4-3-a-pyridine-derivatives-as-potential-selective-c-met-inhibitors-with-improved-pharmacokinetic-properties
#9
Junjun Zhao, Shaohua Gou, Xiaobing Zhang, Yan Liang, Lei Fang
Total twenty-nine [1,2,4]triazolo[4,3-a]pyrazine derivatives were designed and synthesized. The target compounds, especially 4aa, showed potent activity to inhibit c-Met both in an enzyme assay and a cellular assay. The comprehensive screening for the inhibition of 60 different kinases revealed that 4aa could selectively inhibit c-Met while had no effect on other kinases, indicating 4aa is an excellent c-Met selective inhibitor. The flow cytometry studies found that 4aa had a similar behavior to the positive control SGX-523 in the terms of causing the tumor cell apoptosis and blocking cell-cycle progression...
October 31, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27804847/the-warburg-effect-and-the-hallmarks-of-cancer
#10
Laurent Schwartz, Claudiu T Supuran, Khalid O Alfarouk
It is a longstanding debate whether cancer is one disease or a set of very diverse diseases. The goal of this paper is to suggest strongly that most (if not all) the hallmarks of cancer could be the consequence of the Warburg's effect. As a result of the metabolic impairment of the oxidative phosphorylation, there is a decrease in ATP concentration. To compensate the reduced energy yield, there is massive glucose uptake, anaerobic glycolysis, with an up-regulation of the Pentose Phosphate Pathway resulting in increased biosynthesis leading to increased cell division and local pressure...
October 31, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27774878/docking-and-qsar-studies-of-aryl-valproic-acid-derivatives-to-identify-anti-proliferative-agents-targeting-the-hdac8
#11
Heidy Martínez-Pacheco, Guillermo Ramírez-Galicia, Midalia Vergara-Arias, Jürg Gertsch, Jonathan Manuel Fragoso-Vázquez, David Méndez-Luna, A L Abujamra, Cabrera-Pérez Laura Cristina, Rosales-Hernández Martha Cecilia, I Mendoza-Lujambio, José Correa-Basurto
Histone deacetylase 8 (HDAC8) is a plausible target for the development of novel anticancer drugs using a metal-chelating group and hydrophobic moieties as pharmacophores. It is known that valproic acid (administered as its salt, sodium valproate; VPANa+) is an HDAC8 inhibitor characterized by its hydrophobic chains. Nevertheless, VPA is hepatotoxic and VPA analogues might be explored for less hepatotoxic antiproliferative compounds. In this work, docking and QSAR studies of 500 aryl-VPA derivatives as possible HDAC8 inhibitors were performed in order to explore and select potential anti-proliferative compounds...
October 19, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27745548/enzyme-driven-chemo-and-radiation-therapy-with-12-pyrimidine-nucleoside-analogs-not-yet-in-the-clinic
#12
Sheldon Greer, Tieran Han, Cristina Dieguez, Nicola McLean, Rafael Saer, Isildinha Reis, Joe Levi, Victor E Marquez
Enzymatic activity from tumor and adjacent normal tissue of 200 patients involving deoxycytidine kinase (dCK), uridine/cytidine kinase (U/CK), cytidine deaminase (CD) and deoxycytidylate deaminase (dCMPD) was quantified. . Patients with brain (17), colon (24), and breast (30) tumors, 53, 67, and 73%, respectively, had an elevated T/N value (Specific Activity of tumor/ Specific Activity of normal tissue) involving dCK and dCMPD suggesting chemo therapy with 5-fluorodeoxycytidine (5-FdC) alone or in combination with thymidine plus deoxytetrahydrouridine, or with the radiosensitizer, 5-chlorodeoxycytidine (5-CldC) plus tetrahydrouridine (H4U)...
October 13, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27745547/human-cancer-cell-line-based-approach-of-1-3-4-thiadiazole-and-its-fused-ring-a-comprehensive-review
#13
Sudipta Saha, Vinit Raj, Amit Rai
The chemistry of heterocyclic containing, 1,3,4-thiadiazole has been an interesting field of study from ancient years. Subsequently, 1,3,4-thiadiazole nucleus constitutes a significant class of compounds for new drug development. Recently, various 1,3,4-thiadiazole derivatives have been synthesized and evaluated their biological activities including antimicrobial, antituberculosis, antioxidant, anti-inflammatory, anticonvulsants, antidepressant and anxiolytic, antihypertensive, anticancer and antifungal activity...
October 13, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27748173/flt3-inhibitors-in-the-management-of-acute-myeloid-leukemia
#14
Elisabetta Zappone, Marzia Defina, Lara Aprile, Alessandro Gozzetti, Giulia Bartalucci, Monica Bocchia
In recent years there has been a great improvement in molecular characterization of acute myeloid leukemia (AML) allowing the stratification of patients in different rate of risk. Patients with FLT3 mutated AML have poor prognosis because of resistance to induction chemotherapy or early relapse. Several first and second generation molecules, able to inhibit FLT3 signaling have been developed and many single agent or combination studies are ongoing. Of these, quizartinib seems to have the best clinical activity...
October 10, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27697038/bruton-kinase-inhibitors-in-chronic-lymphocytic-leukemia
#15
Alessandro Gozzetti, Veronica Candi, Corrado Zuanelli Brambilla, Giulia Papini, Alberto Fabbri, Monica Bocchia
Abnormality of the B-cell receptor (BCR) signaling is correlated to origin of many B-cell malignancies.. Bruton's tyrosine kinase (BTK), is described as a possible target in a many B-cell neoplasms. Ibrutinib is the most used inhibitor of BTK and has great tolerability and efficacy in chronic lymphocytic leukemia. This review summarizes results with ibrutinib in clinical trials and novel BTK inhibitors of interest.
September 28, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27677688/atra-entrapped-in-dspc-liposome-enhance-anti-metastasis-effect-on-lung-and-liver-during-b16f10-cell-line-metastasis-in-c57bl6-mice
#16
Reshma Mahima Reji, Siddik Uzzaman, Berlin Grace Vm
The high mortality rate of lung cancer is highly associated with faster metastasis spread. All Trans Retinoic Acid (ATRA), being the first choice drug for leukemia therapy is now under intense study for its therapeutic efficiency in other solid cancers. This study was aimed to investigate the anti-metastasis activity of free ATRA and liposome entrapped ATRA (5:4:1) in the experimental C57BL/6 mice model developed by the injection of B16F10 cell line into the tail vein. The ATRA drug was given via i.p for 21 days...
September 27, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27671303/tgf-%C3%AE-signal-transduction-in-pancreatic-carcinoma-cells-is-sensitive-to-inhibition-by-the-src-tyrosine-kinase-inhibitor-azm475271
#17
Tobias Bartscht, Benjamin Rosien, Dirk Rades, Roland Kaufmann, Harald Biersack, Hendrik Lehnert, Hendrik Ungefroren
BACKGROUND: Earlier results from our group have shown that in pancreatic ductal adenocarcinoma (PDAC)-derived cells transforming growth factor (TGF)-β1-dependent epithelial-mesenchymal transition (EMT) and cell motility was inhibited by the Src inhibitors PP2 and PP1 both of which targeted the TGF-β receptors for inhibition. OBJECTIVE: In this study we evaluated the impact of another Src inhibitor, AZM475271, on various TGF-β responses in PDAC cells. METHOD: The effect of AZM475271 on TGF-β1-induced random cell migration (chemokinesis), the expression of EMT and migration/invasion-associated genes, TGF-β-induced luciferase activity, and C-terminal phosphorylation of Smad2 and Smad3 was measured in the PDAC-derived Panc-1 and Colo357 cell lines using real-time cell migration assays, quantitative real-time PCR, luciferase reporter gene assays and phosphoimmunoblotting, respectively...
September 26, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27671302/thiosemicarbazone-derivative-induces-in-vitro-apoptosis-in-metastatic-pc-3-cells-via-activation-of-mitochondrial-pathway
#18
Saravana Kumar Sinniah, Kong Wai Tan, Seik Weng Ng, Kae Shin Sim
[(C6H5)3PCH2(C6H3OH)CH=N-NH-C(S)-N(CH3)2]+Cl-, a thiosemicarbazone, exhibited cytotoxicity towards PC-3 human prostate cancer cell line with IC50 value of 2.64±0.33 µM and selectivity index of 1.5. There were marked morphological changes observed in DM(tsc)T treated cells stained with acridine orange and ethidium bromide which were indicative of cell apoptosis. Treatment with DM(tsc)T showed that the cell cycle is arrested in the G0/G1 phase after 72 hours and manifested an apoptotic population in cells which are time- and concentration-dependent using annexin V/Propidium iodide analysis...
September 26, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27671301/polo-like-kinase-1-targeting-chitosan-nanoparticles-suppress-the-progression-of-hepatocellular-carcinoma
#19
Dongzhi Wang, Renan Chang, Gang Wang, Baoying Hu, Yong Qiang, Zhong Chen
BACKGROUND: Recent investigations have implicated that Chitosan-nucleotide nanoparticles might be useful non-viral carriers in gene therapy. Polo-like kinase 1 (PLK1) has been reported to be an important oncogene that exerted considerable therapeutic value in hepatocellular carcinoma (HCC). OBJECTIVE: We explored whether Galactosylated chitosan-graft-poly(ethylene glycol) (GCP) nanoparticle-mediated delivery of PLK1 siRNA nucleotides could serve as an effective anti-cancer agent for HCC therapy...
September 26, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27671300/synthetic-mono-di-halogenated-coumarin-derivatives-and-their-anticancer-properties
#20
Kabange Kasumbwe, Katharigatta N Venugopala, Viresh Mohanlall, Bharti Odhav
Coumarins are naturally occurring plant metabolites known for their various pharmacological properties such as anticoagulant, antimicrobial, anticancer, antioxidant, anti-inflammatory and antiviral properties. In the present investigation, mono/di-halogenated coumarins CMRN1-CMRN7 have been synthesized and evaluated for their anticancer activity. The cytotoxicity potential of the test compounds was evaluated against UACC-62, MCF-7 and PBM (Peripheral Blood Mononuclear) cell lines using MTT assay. The apoptotic potential of the coumarin compounds was evaluated against UACC-62 cell by assessing membrane change, mitochondria membrane potential, pro-apoptotic changes were investigated using the AnnexinV-PI staining, JC-1, caspase-3 enzyme kits respectively on flow cytometer...
September 26, 2016: Anti-cancer Agents in Medicinal Chemistry
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