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Anti-cancer Agents in Medicinal Chemistry

Naresh Varma Seelam, Srinu Bodige, Parameshwar Ravula, Kali Charan Gulipalli, Srinivas Endoori, J N Narendra Sharath Chandra, Purna Koteswara Rao Cherukumalli, G R Vanaja
Phosphatidylinositol-3-kinase α (PI3Kα) is a ubiquitous intracellular enzyme, mainly involved in intracellular signaling pathways, promotes cellular growth, proliferation, and differentiation. Therefore, inhibition of PI3K can be a hotspot in molecular targeted therapy for the treatment of cancer. The present research work involves molecular docking studies performed to screen derivatives of urea and thiourea bearing thieno [3,2-d]-pyrimidines against the active site of PI3K enzyme using MOE.2008.10. The designed structures (6a-f) and (7a-j) were synthesized by the facile synthetic methods and evaluated for their anticancer activity against HT-29 and MCF-7 cell lines and inhibitory activity against PI3Kα enzyme...
February 9, 2018: Anti-cancer Agents in Medicinal Chemistry
Manjula Devi Ramamoorthy, Ashok Kumar, Mahesh Ayyau, Kannan Narayanan Dhiraviam
Reserpine, an indole alkaloid commonly used for hypertension, is found in the roots of Rauwolfia serpentina. Although the root extract has been used for the treatment of cancer, the molecular mechanism of its anti-cancer activity on hormonal independent prostate cancer remains elusive. Therefore, we evaluated the cytotoxicity of reserpine and other indole alkaloids, yohimbine and ajmaline on prostate cancer cells (PC3) using MTT assay. We investigated the mechanism of apoptosis using a combination of techniques including acridine orange/ethidium bromide staining, high content imaging of Annexin V-FITC staining, flow cytometric quantification of the mitochondrial membrane potential and reactive oxygen species (ROS) and cell cycle analysis...
February 9, 2018: Anti-cancer Agents in Medicinal Chemistry
Grazia Maugeri, Agata Grazia D Amico, Daniela Maria Rasa, Salvatore Saccone, Concetta Federico, Gaetano Magro, Sebastiano Cavallaro, Velia D Agata
Caffeine represents the most used psychoactive drug in the world acting as a non-selective adenosine receptor antagonist. It exerts an anti-cancer role in glioblastoma multiforme (GBM). This neoplasia is characterized by extensive hypoxic foci triggering hypoxia-inducible factors (HIFs) expression. Among these factors, HIF-1α performs a crucial role in the induction of vascular endothelium growth factor (VEGF), a key player in angiogenesis and cell migration. In this work, we have investigated whether caffeine counteracts GBM progression by modulating hypoxic event...
February 9, 2018: Anti-cancer Agents in Medicinal Chemistry
Ali Neshastehriz, Maziar Khateri, Habib Ghaznavi, Ali Shakeri-Zadeh
BACKGROUND AND PURPOSE: It has been well-known both gold nanoparticles (AuNPs) and cisplatin are potential radiosensitizers for radiotherapy of cancer. In this in vitro study, we investigated the chemo-radiotherapeutic effects of alginate nanogel co-loaded with AuNPs and cisplatin (ACA) on U87-MG human glioblastoma cells. METHODS: Based on the accomplished pilot studies, U87-MG cells were incubated with ACA and cisplatin at 10% inhibitory concentration (IC10) for 4 h...
January 30, 2018: Anti-cancer Agents in Medicinal Chemistry
Gomathi Priya Jeyapal, Mjn Chandrasekar, Rajendiran Krishnasamy, Jubie Selvaraj, Manal Mohammad, M J Nanjan
Pim kinases, also known as Serine/Threonine kinases, are intensively studied protein drug targets in cancer research. They play crucial role in the regulation of signal transduction cascades that promote cell survival, proliferation and drug resistance. Pim kinases are overexpressed in several hematopoietic and solid tumors and support in vitro/in vivo malignant cell growth and survival, through cell cycle regulation and inhibition of apoptosis. Pim kinases do not have an identified regulatory domain, as they are constitutively active...
January 30, 2018: Anti-cancer Agents in Medicinal Chemistry
Jucimara F Colombo, Bruna Victorasso Jardim-Perasssi, Joao Paulo Senna Ferreira, Cristine Zampieri Braga, Nathalia Martins Sonehara, Rubens de Paula Júnior, Marina Gobbe Moschetta, Ana Paula Girol, Debora Aparecida Pires De Campos Zuccari
Background NF-kB (nuclear factor kappa B) is a transcription factor composed of two subunits, p50 and p65, which plays a key role in the inflammatory process. Melatonin has oncostatic, antiangiogenic and antimetastatic properties, and some recent studies have indicated an inhibitory effect of melatonin on NF-kB in some types of cancer. This work aims to investigate the effects of melatonin treatment on the expression of NF-kB in breast and liver cancer models. Methods The breast cancer xenographic model was performed using female Balb/c nude athymic mice injected with MDA-MB-231 cells...
January 30, 2018: Anti-cancer Agents in Medicinal Chemistry
Mustapha M Bouhenna, Monica Vara Perez, Oualid Talhi, Khaldoun Bachari, Artur M S Silva, Walter Luyten, Nabil Mameri
Oncology treatments aim at selective toxicity for tumor (compared to normal) cells, and chromone-coumarin hybrids have shown such activity. In this study, we test a novel series of synthetic chromone and coumarin derivatives (1-9) for cytotoxic activity against a panel of tumor cell lines (MCF-7, A549, HepG2, HTC-116, B16) opposed to non-tumor cells (Caco-2 and HEK-293t). Electrical impedance spectroscopy was used to monitor cell viability in real time. Compound 8 showed the most potent activity, and it significantly diminished cancer cell proliferation and viability in different cell lines...
January 29, 2018: Anti-cancer Agents in Medicinal Chemistry
Sobhy El-Sayed Hassab El-Nabi, Gouda T M Dawoud, Islam Mohamed El-Garawani, Samraa Samy El Shafey
Coffee is a popular drink; it is one of the most commercialized food products and a rich source of biologically active compounds that are important for human health. This study aimed to prove the anticancer activity of green coffee (GC) and roasted coffee (RC) bean aqueous extracts (Coffea arabica) on breast cancer adenocarcinoma cell line (MCF-7) and the safety of both extracts on normal human peripheral blood lymphocytes culture (HPBL). Total phenolic content for GC and RC extracts was measured and result of both extracts were (0...
January 24, 2018: Anti-cancer Agents in Medicinal Chemistry
Ehab Mohamed Gedawy
Novel 4-substitutedaminothieno[2,3-d]pyrimidine derivatives 4a-i and 5a-c were synthesized via reacting corresponding 4-chlorothieno[2,3-d]pyrimidine derivatives 3a-c with N-methylpiperazine, morpholine, N-phenylpiperazine or 1,3-propanediamine. All of the newly synthesized compounds were submitted to the National Cancer Institute (USA) for anticancer evaluation. Six compounds (2a, 4d, 4e, 5a-c) were selected and evaluated using 60 different human tumor cell lines using a single dose (10-5 Molar). Compound 4d showed significant cytotoxicity against colon, renal, prostate and breast cancer...
January 24, 2018: Anti-cancer Agents in Medicinal Chemistry
Farzin Hadizadeh, Fatemeh Kalalinia, Mohammad Jouya, Alireza Khorsand Komachal, Aboutourabzadeh Seyed Mohammad, Gholamreza Karimi, Javad Behravan, Khalil Abnous, Leila Etemad, Hossein Kamali
PURPOSE: Some aromatase inhibitors are FDA-approved agents as first-line therapy in the treatment of endocrine-responsive breast cancer. In this study, we aimed to develop new azole derivatives with higher specificity and potency. METHODS: New aromatase inhibitors were designed by Molecular Operating Environment (MOE) software and synthesized in a one-step SN2 reaction. These compounds were characterized by melting point, 1H- and 13C-NMR, elemental analysis and mass spectra...
January 15, 2018: Anti-cancer Agents in Medicinal Chemistry
Helen L Alvarado, Ana C Calpena, Maria L Garduno-Ramirez, Raul Ortiz, Consolacion Melguizo, Jose M Prados, Beatriz Clares
BACKGROUND: Triterpenoids are an important class of natural bioactive products present in many medicinal plants. OBJECTIVE: The aim of present study is to investigate the antioxidant and anticarcinogenic potential of oleanolic acid (OA) and ursolic acid (UA) on B16 murine melanoma cell line isolated from Plumeria obtusa, free and loaded in a nanoemulsion (NEm) system. METHOD: The nanoemulsion was characterized by dynamic light scattering, transmission electron microscopy...
January 11, 2018: Anti-cancer Agents in Medicinal Chemistry
Cheng Luo, Di Wu, Glory Magawa, Josephine Omodo, Changfeng Xue, Yanhui Sun, Dequn Liu, Chong Xie, Yaqin Wang, Christopher Frenz, Shanggui Deng
Different saponins from herbs have been used as tonic or functional foods, and for treatment of various diseases including cancers. Although clinical data has supported the function of these saponins, their underlying molecular mechanisms have not been well defined. With the simulated hypoxia created by 8 hours of Cu++ exposure and following 24 hour incubation with different concentration of saponins in HepG2 cells, ZC-4 had the highest rate of inhibition of cell proliferation by MTT assay, and the highest inhibition of migration rate by in vitro scratch assay, while ZC-3 had the highest inhibition of invasion ratio by transwell assay...
January 10, 2018: Anti-cancer Agents in Medicinal Chemistry
Hassiba Rouibah, Lahouel Mesbah, Wided Kebsa, Malek Zihlif, Mamoun Ahram, Bachaer Aburmeleih, Ibtihal Mostafa, Hemzeh El Amir
BACKGROUND: Pancreatic cancer is one of the most aggressive and lethal cancer, with poor prognosis and high resistant to current chemotherapeutic agents. Therefore, new therapeutic strategies and targets are underscored. Propolis has been reported to exhibit a broad spectrum of biological activities including anticancer activity. OBJECTIVE: This study was carried out to assess the possible efficacy of Algerian propolis on the antitumor effect of doxorubicin on human pancreatic cancer cell line (PANC-1)...
January 10, 2018: Anti-cancer Agents in Medicinal Chemistry
Ping Jin, Fei Xiao Chen, Yang Zi Li, Qing Qing Zhang, Jian Zhang
BACKGROUND/OBJECTIVE: Forkhead Box M1 (FOXM1) is frequently activated in tumors. We studied the expression and the possible mechanism of FOXM1 and evaluated the effects of thiostrepton in an endometriotic rat model. STUDY DESIGN: This was a randomized study in a rat model of endometriosis. Fifty female Wistar rats were surgically induced with endometriosis. After 4 weeks of observation, twenty and thirty rats were randomly allocated to an ovariectomized (OVX) group and a treatment group, respectively...
January 7, 2018: Anti-cancer Agents in Medicinal Chemistry
Xue Zhu, Ke Wang, Kai Zhang, Yi Pan, Fanfan Zhou, Ling Zhu
Retinoblastoma is the most common intraocular malignant tumor in childhood. Although external beam radiation and enucleation are effective to control retinoblastoma, eye salvage and vision preservation are still significant challenges. Polyphyllin I (PPI), a natural compound extracted from Paris polyphylla rhizomes, has a wide range of activities against many types of cancers. However, the potential effect of this herbal compound on retinoblastoma has not yet been investigated. In the present study, we evaluated the cytotoxic effect of PPI on human retinoblastoma Y-79 cells as well as its underlying molecular mechanism...
January 7, 2018: Anti-cancer Agents in Medicinal Chemistry
Mohammad Saleem, Jawaria Asif, Muhammad Asif, Uzma Saleem
Amygdalin is a cyanogenic glycoside which is described as a naturally occurring anti-cancer agent. In 1830s, French chemists Robiquet and Boutron-Charlard isolated amygdalin from bitter almonds. Apoptosis is an important mechanism in cancer treatment by amygdalin. Amygdalin can probably stimulate apoptotic process in cancerous cells by increasing activity of Bax (pro-apoptotic protein) and caspase-3 and decreasing expression of Bcl-2 (anti-apoptotic protein). Amygdalin promotes arrest of cell cycle in G0/G1 phase followed by decreasing number of S and G2/M phase cells...
January 5, 2018: Anti-cancer Agents in Medicinal Chemistry
Betul Kaya, Ozlem Atli, Gozde Gormus, Yusuf Ozkay, Zafer Asim Kaplancikli
A series of novel chalcone derivatives bearing diverse heterocycles have been synthesized and evaluated for their antiproliferative activity against A549 (human lung adenocarcinoma) and C6 (rat brain glioma) cells. Structures of the title compounds (3-18) were verified by FT-IR, 1H NMR, 13C NMR, HRMS spectral data and elemental analyses. Antiproliferative activities of the compounds were evaluated using MTT assay, BrdU method, and flow cytometric analysis. Compounds 9 and 15 were revealed as the most promising cytotoxic agents due to their selectivity towards A549 cells with a lower IC50 values (IC50=0...
January 5, 2018: Anti-cancer Agents in Medicinal Chemistry
Sarah Fernandes Teixeira, Cecilia Pessoa Rodrigues, Cicero Julio Silva Costa, Thais Narimatsu Pettinati, Ricardo Alexandre de Azevedo, Lisley Inata Mambelli, Salomao Doria Jorge, Rodrigo Nalio Ramos, Emer Suavinho Ferro, Jose Alexandre Marzagao Barbuto, Adilson Kleber Ferreira
Lung cancer is the most prevalent cancer and a high fatality disease. Despite all therapeutic approaches available, drug resistance and excessively toxic effects of chemotherapy agents for patients remain as obstacles. Therefore, we proposed the design of new drugs integrating immunotherapeutic and conventional cytotoxic effects as a powerful strategy in the treatment of cancer. Antineoplastic phospholipids combine both of these activities by affecting lipid metabolism and signaling through lipid rafts. Therefore, they emerge as interesting scaffolds for designing new drugs...
January 5, 2018: Anti-cancer Agents in Medicinal Chemistry
Francesco Cantiello, Stefano Manno, Antonio Cicione, Rocco Damiano
OBJECTIVE: Multiparametric Magnetic Resonance Imaging (mpMRI) has become a very useful tool in the management of low risk Prostate Cancer (PCa) patients eligible for Active Surveillance (AS). The aim of this systematic review was to critically review the latest literature concerning the role of mpMRI in this clinical setting, underlying current strengths and weakness. EVIDENCE ACQUISITION: A comprehensive literature research for English-language original and review articles was carried out using the National Center for Biotechnology Information PubMed database with the aim of identify studies on mpMRI for AS in low risk PCa patients...
January 4, 2018: Anti-cancer Agents in Medicinal Chemistry
Manvendra Kumar, Ramit Singla, Jyoti Dandriyal, Vikas Jaitak
In worldwide lung cancer shares 14% among the newly diagnosed cancer cases. Currently, the numbers of drugs that are in clinical practice are having a high prevalence of side effect and multidrug resistance. Researchers have made an attempt to expand a suitable anticancer drug that has no MDR and side effect. Coumarin scaffold became an attractive subject due to their broad spectrum of pharmacological activities. Coumarin derivatives extensively explored for anticancer activities as it possesses minimum side effect along with multi-drug reversal activity...
December 29, 2017: Anti-cancer Agents in Medicinal Chemistry
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