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Anti-cancer Agents in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28071584/major-highlights-of-the-car-tcr-summit-boston-2016
#1
Vita Golubovskaya, Robert Berahovich, Shirley Xu, Hizkia Harto, Lijun Wu
Cellular immunotherapies such as CAR-T cell therapy and TCR-T cell therapy are relatively new, highly promising approaches for the treatment of cancer. In CAR-T cell therapy, a patient's T cells are engineered to express chimeric antigen receptors targeting tumor-associated cell surface antigens. In TCR-T cell therapy, the patient's T cells are engineered to express receptors targeting intracellular antigens. This report will summarize presentations from the recent CAR-TCR summit in Boston on September 13-16, 2016...
10, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28071583/anticancer-activities-of-new-n-hetaryl-2-cyanoacetamide-derivatives-incorporating-4-5-6-7-tetrahydrobenzo-b-thiophene-moiety
#2
Magda F Mohamed, Yasmin M Attia, Samia A Shouman, Ismail A Abdelhamid
Novel series of N-(4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl) cyanoacetamide derivatives are synthesized. The structure of these compounds was elucidated using different spectral tools. Compounds were evaluated for their cytotoxic activities against different types of human cancer cell lines including, breast (MCF-7, T47D, MDA MB231); liver (HEPG-2); colon (HCT116); prostate (PC3); and cervix (HELA) cells. In this study, we used compounds 11 and 12 that showed the highest cytotoxicity on PC3 and HEPG2 cells, to explore their effects on apoptosis, invasion ampamp; metastasis and angiogenesis...
January 10, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28044941/design-synthesis-and-biological-evaluation-of-a-phenyl-butyric-acid-derivative-n-4-chlorophenyl-4-phenylbutanamide-a-hdac6-inhibitor-with-anti-proliferative-activity-on-cervix-cancer-and-leukemia-cells
#3
Rodríguez-Fonseca Rolando Alberto, Sixto-López Yudibeth, Fragoso-Vázquez M Jonathan, Flores-Mejía Raúl, Cabrera-Pérez Laura Cristina, Vázquez-Moctezuma Ismael, Rosales-Hernández Martha Cecilia, Bello Martiniano, M Martínez-Archundia, Trujillo-Ferrara José Guadalupe, Becerra-Martínez Elvia, Correa-Basurto José
The epigenetic regulation of genes in cancer could be targeted by inhibiting Histone deacetylase 6 (HDAC6), an enzyme involved in several types of cancer such as lymphoma, leukemia, ovarian cancer, etc. Through in silico methods, a set of Phenyl butyric acid derivatives with possible HDAC6 inhibitory activity were designed, rendering monophenylamides and biphenylamides using tubacin (HDAC6 selective inhibitor) as reference. The target compounds were submitted to theoretical ADMET analyses and their binding properties on different HDAC6 conformers were evaluated through docking calculations...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28044940/cytotoxic-antiproliferative-and-apoptotic-effects-of-perillyl-alcohol-and-its-biotransformation-metabolite-on-a549-and-hepg2-cancer-cell-lines
#4
Ceren E Oturanel, İsmail Kıran, Özge Özşen, Gülşen A Çiftçi, Özlem Atlı
The monoterpene perillyl alcohol has attracted attention in medicinal chemistry since it exhibited chemo-preventive and therapeutic properties against a variety of cancers. In the present work, anticancer activities of perillyl alcohol and its biotransformation metabolite, dehydroperillic acid, produced through microbial biotransformation with Fusarium culmorum in a yield of 20.4 % were studied. In vitro anticancer studies, perillyl alcohol was found to exert cytotoxicity against HepG2 cell line with an IC50 value of 409...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28044939/inhibition-of-tgf-%C3%AE-signaling-in-tumor-cells-by-small-molecule-src-family-kinase-inhibitors
#5
Tobias Bartscht, Benjamin Rosien, Dirk Rades, Roland Kaufmann, Harald Biersack, Hendrik Lehnerta, Hendrik Ungefroren
In a series of studies carried out over the last couple of years in various cell types, it was observed that the experimentally used Src family kinase inhibitors PP1 and PP2 and the clinically used Src/Abl inhibitors AZM475271 and dasatinib are potent inhibitors of TGF-β mediated cellular responses such as Smad and p38 mitogen-activated protein kinase phosphorylation, Smad-dependent transcriptional activation, growth inhibition, epithelial-mesenchymal transition (EMT), and cell motility. While for PP1/PP2 it was demonstrated shown that these agents directly inhibit the kinase activity of the TGF-β type I receptor activin receptor-like kinase 5, the mechanism of the anti-TGF-β effect of AZM475271 and dasatinib is less clear...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28044938/development-of-selective-cyclin-dependent-kinase-4-inhibitors-for-antineoplastic-therapies
#6
Haixing Guan, Yongli Du, Weiwei Han, Jingkang Shen, Qunyi Li
Cyclin-Dependent Kinases 4 (CDK4) belongs to a family of serine-threonine protein kinase and plays key regulatory role in G1-phase of cell cycle progression. Compelling evidences have shown that targeting CDK4 pathway is an attractive proposition for tumor therapy. Recent progresses of selective small molecule CDK4 inhibitors in cancer therapy have endorsed the field to be interested and attractive. In this review, we will discuss the recent developments of CDK4 inhibitors on several aspects such as the structure of CDK4, the working mechanism of CDK4 inhibitors, the structure activity relationships (SARs) of the selective CDK4 inhibitors and the latest developments of the selective CDK4 inhibitors in clinical trials...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28044937/cytokine-status-of-serum-in-ovarian-cancer-patients-with-different-tumor-neoadjuvant-chemotherapy-response
#7
Inna I Antoneeva, Tatyana V Abakumova, Dinara R Dolgova, Tatyana P Gening, Sabina S Pirmamedova, Dinara F Myasnikova, Snezhanna O Gening
The purpose of the study was to evaluate the cytokine status in the blood serum of ovarian cancer (OC) patients with different tumor neoadjuvant chemotherapy (NACT) response. We determined the levels of IL-1β, -1Ra, -10, TNF-α by enzyme-linked immunosorbent assay in the blood serum of 97 patients with primary ovarian cancer and 64 healthy women. Analysis of polymorphic variants of specific sections of cytokine genes was performed using allele- specific PCR. Polymorphic variants were selected within the promoters of IL-1β T- 31C gene (rs 1143627 ), TNF-α G-308A (rs 1800629) and IL-10 G-1082A (rs 1800896), presented in dbS`NP NCBI and SNP500 Cancer databases...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28044936/nano-delivery-in-pediatric-tumors-looking-back-moving-forward
#8
Marta Colletti, Virginia Di Paolo, Angela Galardi, Giuseppe Maria Milano, Angela Mastronuzzi, Franco Locatelli, Angela Di Giannatale
Recent advances in the treatment of pediatric tumors led to an improvement of survival in this population. As a result, many pediatric survivors experience long-term effects that impact their quality of life. Therefore, it is extremely important to identify new treatment approaches that may target the tumor minimizing the drug-related side effects. Over the past 10 years, remarkable advances in nanomedicine have provided several potential tools for cancer treatment. Recently, there has been a growing interest towards therapeutic nanocarriers in the pediatric field, since they represent a new strategy to enhance the drug efficacy and reduce the toxicity...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28044935/c-glycosyl-flavone-from-urginea-indica-inhibits-growth-and-dissemination-of-ehrlich-ascites-carcinoma-cells-in-mice
#9
Ganesh Babu Bevara, A D Naveen Kumar, K Koteswramma Laxmi, Anil Kumar Badana, Seema Kumari, Nagendra Sastry Yarla, Rama Rao Malla
C-glycosyl flavone, a phytochemical constituent of U. indica bulb, has been reported to possesses cytotoxic activity. In present study, acute and chronic toxicity along with antitumor activity of C-glycosyl flavone isolated from U.indica bulb were performed using in vitro and in vivo methods. Acute and chronic toxicity of C-glycosyl flavone was evaluated using Swiss albino mice. The effect of C-glycosyl flavone on proliferation of Ehrlich ascites carcinoma (EAC) cells was determined. Further, growth inhibition and dissemination was studied using EAC induced mice model...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28044934/anticancer-and-cytotoxic-activities-of-cu-c6h16n2o2-2-ni-cn-4-and-cu-c6h16n2o2-pd-cn-4-cyanidometallate-compounds-on-ht29-hela-c6-and-vero-cell-lines
#10
Ali Aydın, Şengül Aslan Korkmaz, Veysel Demir, Şaban Tekin
BACKGROUND: In cancer, apoptosis relevant proteins-such as CaM kinase, Bcl-2 or P53, topoisomerase I, cell migration feature and DNA/BSA-macromolecules represent significant targets for current chemotherapeutics. OBJECTIVE: We recently reported two coordination compounds-[Cu(C6H16N2O2)2][Ni(CN)4] (1) and [Cu(C6H16N2O2)Pd(CN)4] (2)-together with their IR spectra, magnetic properties, thermal analyses and crystal structures. Herein, we describe the ability of these complexes to induce apoptosis in relevant proteins and stimulate topoisomerase I activity, cell migration velocity and DNA/BSA binding properties...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28042778/personalized-nanoparticles-for-cancer-therapy-a-call-for-greater-precision
#11
Nare Sahakyan, Amir Haddad, Shye Richardson, Valery Forcha-Etieundem, Lee Christopher, Hanan Alharbi, Robert Campbell
Nanotechnology has brought about the advent of personalized medicine in the era of targeted therapeutic strategies for cancer therapy. The ability to exploit tumor features for therapeutic gain has made it possible to manufacture more effective nanomedicines for cancer treatment. However, known obstacles, including the inability to overcome pathophysiological barriers of tumors, have impeded disease management. In spite of this, recent efforts have been made to develop more functionalized nanosystems that utilize the active-targeting approach...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28042777/immune-checkpoints-aberrations-and-malignant-mesothelioma-assessment-of-prognostic-value-and-evaluation-of-therapeutic-potentials
#12
Hadeer Mohamed, Mostafa Eltobgy, Omar Abdel-Rahman
Malignant pleural mesothelioma (MPM) is a hard to treat malignancy arising from the mesothelial surface of the pleura. Immune checkpoint inhibitors are considered a promising therapeutic strategy in many hard-to-treat malignancies. In this review, we are trying to provide an in depth coverage of the prognostic value of immune checkpoints aberrations as well as discuss the different novel therapeutic strategies implementing these agents in the management of MPM.
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28042776/synthesis-and-evaluation-of-cytotoxic-activity-of-some-pyrroles-and-fused-pyrroles-running-title-fused-pyrroles-as-novel-anti-cancer-agents
#13
Samar S Fatahala, Mosaad S Mohamed, Mahmoud Youns, Rania H Abd-El Hameed
Pyrrole derivatives represent a very interesting class as biologically active compounds. The objective of our study was to investigate the cytotoxic and apoptotic effects and antioxidant activity of the newly synthesized pyrrole derivatives. A series of novel pyrroles and fused pyrroles (tetrahydroindoles, pyrrolopyrimidines, pyrrolopyridines and pyrrolotriazines) were synthesized and characterized using IR, 1H NMR, 13C NMR, MS and elemental analysis techniques. The antiproliferative activity of our synthesized compounds and their modulatory effect apoptotic pathway were investigated...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28042775/inhibition-of-epithelial-mesenchymal-transition-in-response-to-treatment-with-metformin-and-y27632-in-breast-cancer-cell-lines
#14
Camila Leonel, Lívia Carvalho Ferreira, Thaiz Ferraz Borin, Marina Gobbe Moschetta, Gabriela Scavacini Freitas, Michel Raineri Haddad, João Antonio de Camargos Pinto Robles, Debora Aparecida Pires de Campos Zuccari
BACKGROUND: ROCK-1 expression is associated with the malignant character of tumors, while inhibiting this molecule results in a significant suppression of tumor metastasis. Likewise, transforming growth factor beta (TGF-β) is associated with this malignancy by having the ability to induce epithelial-mesenchymal transition (EMT). Metformin, a drug used in the treatment of diabetes, has previously been shown to inhibit EMT in breast cancer cells. OBJECTIVE: The aim of this study is to evaluate the TGF-β1 action model for induction of EMT and the action of metformin and ROCK-1 inhibitor (Y27632) in EMT process in breast cancer cell lines...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28017128/role-of-azoles-in-cancer-prevention-and-treatment-present-and-future-perspectives
#15
Khurshid Ahmad, Mohd Kalim A Khan, Mohammad Hassan Baig, Mohd Imran, Girish Kumar Gupta
Cancer has gradually become one of the leading causes of death worldwide. The incidence of cancer among the population worldwide has increased in an alarming way over the last 2 decades, primarily due to an increasing population of immune-compromised patients and the continuing rise in anti-cancer drug resistance. Azole found privileged structure in medicinal chemistry and pharmaceutical industry and also found very effective against a number of biological targets including antioxidant; antimicrobial, antihelmintic, anticancer, antiviral, anti-parasitic, anti-inflammatory, anti-HIV, and antihypertensive activities...
December 21, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28003000/double-edge-sword-behavior-of-carbendazim-a-potent-fungicide-with-anti-cancer-therapeutic-properties
#16
Karan Goyal, Ajay Sharma, Ridhima Arya, Rohit Sharma, Girish K Gupta, Anil K Sharma
A number of benzimidazole derivatives such as benomyl and carbendazim have been known for their potential role as agricultural fungicides. Simultaneously carbendazim has also been found to inhibit proliferation of mammalian tumor cells specifically drug and multidrug resistant cell lines. Studies carried out with fungal and mammalian cells have highlighted the potential role of carbendazim in inhibiting proliferation of cells, thereby exhibiting therapeutic implications against cancer. Because of its promising preclinical antitumor activity, Carbendazim had undergone phase I clinical trials and is under further clinical investigations for treatment of cancer...
December 21, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28002999/targeting-leptin-as-a-therapeutic-strategy-against-ovarian-cancer-peritoneal-metastasis
#17
Xiao Wei, Yi Liu, Cheng Gong, Teng Ji, Xiaoshui Zhou, Taoran Zhang, Dongyi Wan, Sen Xu, Ping Jin, Xin Yang, Xiaoting Li, Ding Ma, Zongyuan Yang, Qinglei Gao
Epithelial ovarian cancer (OC) is the leading cause of death in patients with gynecologic malignancy. Malignant ascites,a shared symptom of advanced OC patients, plays an important role in the peritoneal metastasis cascade of OC. Since leptin existed in great amount in malignant ascites, we speculated that it might be involved in the modulation of tumor cells malignant behavior. Here, we demonstrated that blocking of leptin could significantly suppress ovarian malignant ascites-induced metastatic aggravation of OC cells...
December 21, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28002998/targeting-leptin-as-a-therapeutic-strategy-against-ovarian-cancer-peritoneal-metastasis
#18
Xiao Wei, Yi Liu, Cheng Gong, Teng Ji, Xiaoshui Zhou, Taoran Zhang, Dongyi Wan, Sen Xu, Ping Jin, Xin Yang, Xiaoting Li, Ding Ma, Zongyuan Yang, Qinglei Gao
Epithelial ovarian cancer (OC) is the leading cause of death in patients with gynecologic malignancy. Malignant ascites,a shared symptom of advanced OC patients, plays an important role in the peritoneal metastasis cascade of OC. Since leptin existed in great amount in malignant ascites, we speculated that it might be involved in the modulation of tumor cells malignant behavior. Here, we demonstrated that blocking of leptin could significantly suppress ovarian malignant ascites-induced metastatic aggravation of OC cells...
December 21, 2016: Anti-cancer Agents in Medicinal Chemistry
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
#19
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
#20
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
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