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Anti-cancer Agents in Medicinal Chemistry

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
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
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
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
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
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
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
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
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
Ri-Zhen Huang, Shi-Xian Hua, Cai-Yi Wang, Ying-Ming Pan, Jian-Mei Qin, Zhan-Yu Ding, Ye Zhang, Heng-Shan Wang
A set of novel 4-methylumbelliferones derivatives 3 (3a-3n) and 4 (4a, 4c, 4l, 4m, 4n) have been synthesized and evaluated for their antitumor activity. In vitro antiproliferative activities of all of these compounds against nine human cancer lines and HUVEC normal cell lines were assayed by standard MTT assay, using commercial anticancer drugs 5-fluorouracil (5-FU) and cisplatin as comparation. The staining results revealed that compound 4l could induce apoptosis in NCI-H460 cells. Successive studies conduced with 4l in NCI-H460 cells demonstrated that this compound induced the intracellular reactive oxygen species generation and calcium overload, suppressed nuclear factor-κB (NF-κB) activity and regulated anti- and pro-apoptotic proteins...
September 26, 2016: Anti-cancer Agents in Medicinal Chemistry
Loiy Elsir A Hassan, Muhammad Adnan Iqbal, Saad S Dahham, Yasser M Tabana, Mohamed B Khadeer Ahamed, Amin M S Abdul Majid
Cancer is characterized by uncontrolled cell division caused by dysregulation of cell proliferation. Therefore, agents that impair cancer cell proliferation could have potential therapeutic value. Higher plants are considered to be a good source of anticancer agents, and several clinically tested chemotherapeutic agents have been isolated from plants or derived from constituents of plant origin. In the present study, a prenylated flavone (isoglabratephrin) was isolated from aerial parts of Tephrosia apollinea using a bioassay-guided technique...
September 26, 2016: Anti-cancer Agents in Medicinal Chemistry
Wafa A Mera, Malek Alzihlif, Mutasem O Taha, Mohammad A Khanfar
Bruton's Tyrosine Kinase (BTK) is a one of the Tec tyrosine kinase family. It has an essential role in B-cell development and function. Activation of BTK has been associated with the pathogenesis of many types of lymphomas and leukemia, and involved in non-life threatening autoimmune diseases. In this study, exhaustive pharmacophore modeling was combined with QSAR analyses to examine the structural requirements for anti-BTK activities. Genetic function algorithm (GFA) was coupled with multiple linear regression (MLR) analysis to select the best combinations of physicochemical descriptors and pharmacophoric hypothesis capable of generating predictive and self-consistent QSAR models...
September 26, 2016: Anti-cancer Agents in Medicinal Chemistry
Sean L Kitson, Vincenzo Cuccurullo, Andrea Ciarmiello, Luigi Mansi
Radionuclide antibody conjugates (RACs) and antibody-drug conjugates (ADCs) can function as biotherapeutic missiles in order to target cancer cells and destroy them. The advent of new technology platforms consisting of imaging modalities, drug design and radiochemistry will facilitate the personalised approach for cancer patient treatment programmes. The utilisation of radionuclides and cytotoxic drugs conjugated to biovectors can deliver a cytotoxic drug payload with the ability to emit alpha and/or beta particles in the vicinity of the tumour by binding onto the cancer cells surface antigens initiating cell death...
September 26, 2016: Anti-cancer Agents in Medicinal Chemistry
Jinhong Liu, Zifei Zhu, Jia Tang, Qinghua Lin, Li Chen, Jianbo Sun
A total of 16 targeted NO-releasing betulinic acid (BA) derivatives were designed and synthesized as potential anticancer agents. Most IC50 values were under 1.0 μM in vitro test against HepG2 and B16. The result suggested that derivatives of BA with α,β-unsaturated ketone skeleton possessed significant cytotoxic activities than the others, among which derivatives with three carbons in diol linker (15b and 15c) exhibited the highest anti-cancer activity. NO-releasing amount detection of partial target compounds suggested that NO-releasing amount of this series of BA derivatives positively correlates with their cytotoxic activities...
September 26, 2016: Anti-cancer Agents in Medicinal Chemistry
Andrea Ilaria Zotti, Elena Di Gennaro, Angela Corvino, Francesco Frecentese, Elisa Magli, Elisa Perissutti, Giuseppe Cirino, Fiorentina Roviezzo, Manuela Terranova-Barberio, Federica Iannelli, Giuseppe Caliendo, Vincenzo Santagada, Ferdinando Fiorino, Alfredo Budillon, Beatrice Severino
Protease activated receptor-1 (PAR1) is a G-coupled receptor activated by α-thrombin and other proteases. Several reports demonstrate PAR1 involvement in tumorigenesis and tumor progression. In order to investigate on potential use of PAR1 antagonists as antiproliferative agents, we have identified a series of arylpiperazine derivatives acting as PAR1 antagonists; the selected molecules have been evaluated for their antiproliferative properties. All the compounds inhibited the growth of a panel of cell lines expressing PAR1; two of them, compounds 13 and 15, were able to inhibit, in a dose dependent manner, the growth of the selected cell lines with the lowest IC50 values, and were further characterized to define the mechanism responsible for the observed antiproliferative effect...
September 26, 2016: Anti-cancer Agents in Medicinal Chemistry
Úrsula Amaranta Rossi, Liliana María Elena Finocchiaro, Gerardo Claudio Glikin
We evaluated the cytotoxic effects of the combination of bortezomib (BTZ) and interferon-β (IFNβ) gene lipofection on cultured melanoma cells. Four canine mucosal (Ak, Br, Bk and Ol) and two human dermal (A375 and SB2) melanoma cell lines were assayed. BTZ sub-pharmacological concentrations (5 nM) enhanced the cytotoxic effects of IFNβ transgene expression on melanoma cells monolayers and spheroids. The combination was also more effective than the single treatments when assayed for clonogenic survival and cell migration...
September 23, 2016: Anti-cancer Agents in Medicinal Chemistry
Sheefa Mirza, Aakanksha Vasaiya, Hemangini Vora, Nayan Jain, Rakesh Rawal
BACKGROUND: The ultimate goal of the study was to find a role of curcumin in targeting lung cancer stem cells by reducing their self-renewal efficiency causing DNA damage. MATERIALS AND METHODS: Circulating lung cancer stem cells were isolated by sphere formation assay and further analysed by flow-cytometry and qRT-PCR for the presence of stem cell and stem cell transcription markers. IC50 values of gemcitabine and curcumin was analysed by MTT assay, while curcumin induced DNA damage was scrutinized by single cell gel electrophoresis assay...
September 23, 2016: Anti-cancer Agents in Medicinal Chemistry
Marwa Ahmed, Naja Magdy
Cancer is a major health problem to human beings around the world. Many quinazoline derivatives were reported to have potent cytotoxic activity. Our aim in this work is the discovery of potent epidermal growth factor receptor (EGFR) inhibitors with anti-breast cancer activity containing 4-substituted quinazoline pharmacophore. Novel series of 4-substituted 6,8-dibromo-2-(4-chlorophenyl)-quinazoline derivatives have been designed and synthesized. New derivatives were tested against MCF-7 (human breast carcinoma cell line) and screened for their inhibition activity against epidermal growth factor receptor tyrosine kinase (EGFR-TK)...
September 23, 2016: Anti-cancer Agents in Medicinal Chemistry
Edward A Ratovitski
Dehydroleucodine (DhL), a natural sesquiterpene lactone from Artemisia douglassiana Besser (Argentine) and Gynoxys verrucosa (Ecuador) was shown to induce a cell death in cancer cells through senescence, apoptosis, and DNA damage. Here, we found that the DhL exposure upregulated the total and phosphorylated (p-Y99) levels of TP73 in human glioblastoma U87-MG cells. We further found that TP73 silencing led to a partial rescue of U87-MG cells from the cell death induced by DhL. Upon the DhL exposure numerous gene targets were upregulated and downregulated through a TP73-dependent transcriptional mechanism...
September 23, 2016: Anti-cancer Agents in Medicinal Chemistry
Xiaoping Zhan, Weixi Qin, Shuai Wang, Kai Zhao, Yuxuan Xin, Yaolin Wang, Qi Qi, Zhenmin Mao
A series of pyrrole derivatives were synthesized and determined for their anti-cancer activity against nine cancer cell lines and two non-cancer cell lines using MTT assay. The study of the structure-activity relationships revealed that the introduction of the electron-donation groups at the 4th position of the pyrrole ring increased the anti-cancer activity. Among the synthesized compounds, specially the compounds bearing 3,4-dimethoxy phenyl at the 4th position of the pyrrole ring showed potent anti-cancer activity, cpd 19 was the most potent against MGC 80-3, HCT-116 and CHO cell lines (IC50s = 1...
September 22, 2016: Anti-cancer Agents in Medicinal Chemistry
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