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Anti-cancer Agents in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28782465/pyramidatine-z88-sensitizes-vincristine-resistant-human-oral-cancer-kb-vcr-cells-to-chemotherapeutic-agents-by-inhibition-of-p-glycoprotein
#1
Zulong Liu, Hengrui Zhu, Shijin Qu, Lisha Tang, Lihuan Cao, Wenbo Yu, Xianmei Yang, Songmin Jiang, Dayuan Zhu, Changheng Tan, Long Yu
Multi-drug resistance (MDR) to anticancer drugs remains a major impediment in cancer therapy. A major goal for scientists is to identify more effective compounds that are able to circumvent MDR and simultaneously have minimal adverse side effects. Here, we reported that Pyramidatine (Z88), a cinnamic acid-derived bisamide compound isolated from the leaves of Aglaia perviridis, had potent anti-MDR activity. The average resistant fold (RF) of Z88 is 0.09 and 0.51 in KB/VCR (vincristine-resistant human oral cancer cells) and MCF-7/ADR (adriamycin-resistant human breast adenocarcinoma) cells...
August 3, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28762317/effects-of-plasma-activated-medium-on-head-and-neck-fadu-cancerous-cells-comparison-of-3d-and-2d-response
#2
Merbahi Nofel, Julie Chauvin, Patricia Vicendo, Florian Judée
OBJECTIVE: The aim of this work is to investigate the inhibitory effect of Plasma Activated Medium (PAM) on Head and Neck cancerous cells (FaDu).. The response of FaDu cells in monolayer cultures and Multi Cellular Tumor Spheroids (MCTS) after treatment with different PAMs will be compared. BACKGROUND: Head and Neck squamous cell carcinoma is a widespread cancer that responds poorly to anti-cancer treatments such as chemotherapy and radiotherapy. Recently growth interest in cold plasmas and their application in cancer therapy...
August 1, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28762316/hydrogen-peroxide-and-beyond-the-potential-of-high-voltage-plasma-activated-liquids-against-cancerous-cells
#3
Daniela Boehm, Paula Bourke
The use of plasma-activated liquids such as PBS, medium or simply plasma-activated water (PAW) has been receiving increasing attention for applications in cancer treatments. Amongst the reactive species contained in these solutions, hydrogen peroxide appears to play a pivotal role in causing cytotoxic effects. While H2O2 concentrations can be correlated with reduced cell viability and growth and used as an indicator of the potential efficacy of a plasma-activated water, comparisons to standard H2O2 kill curves demonstrate a potency in PAW which exceeds H2O2 associated toxicity, indicating that other plasma-generated species play an important role...
August 1, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28762315/targeting-protective-catalase-of-tumor-cells-with-cold-atmospheric-plasma-treated-medium-pam
#4
Georg Bauer
● Background Application of cold atmospheric plasma to medium generates "plasma-activated medium" that induces apoptosis selectively in tumor cells and that has an antitumor effect in vivo. The underlying mechanisms are not well understood. ● Objective Elucidation of potential chemical interactions within plasma-activated medium and of reactions of medium components with specific target structures of tumor cells should allow to define the active principle in plasma activated medium. ● Method Established knowledge of intercellular apoptosis-inducing reactive oxygen/nitrogen species-dependent signaling and its control by membrane-associated catalase was reviewed...
August 1, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28762318/the-application-of-the-cold-atmospheric-plasma-activated-solutions-in-cancer-treatment
#5
Dayun Yan, Jonathan H Sherman, Michael Keidar
Over past five years, the cold atmospheric plasma-activated solutions (PAS) has shown its promissing application in cancer treatment. Similar as the common direct cold plasma treatment, PAS shows a selective anti-cancer capacity in vitro and in vivo. However, different from the direct cold atmospheric plasma (CAP) treatment, PAS can be stored for a long time and can be used without dependence on a CAP device. The research on PAS is gradually becoming a hot topic in plasma medicine. In this review, we gave a concise but comprehensive summary on key topics about PAS including the development, current status, as well as the main conclusions about the anti-cancer mechanism achieved in past years...
July 31, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28748756/activity-of-saponins-from-medicago-species-against-hela-and-mcf-7-cell-lines-and-their-capacity-to-potentiate-cisplatin-effect
#6
Pinarosa Avato, Danilo Migoni, Mariapia Argentieri, Aldo Tava, Francesco Paolo Fanizzi
In the present paper we aim to describe the cytotoxic properties of saponin mixtures from M. arabica (tops and roots), M. arborea (tops) and M. sativa (tops, roots and seeds) and related prosapogenins from M. arborea and M. sativa (tops) against HeLa and MCF-7 cell lines. In addition, cytotoxicity of purified soyasaponin I and some purified saponins (1-8) of hederagenin, medicagenic and zanhic acid is also presented. Saponins from M. arabica tops and roots (mainly monodesmosides of hederagenin and bayogenin) were the most effective to reduce, at certain concentrations, proliferation of HeLA and MCF-7 cell lines, showing potential as anti-cancer agents against HeLa...
July 27, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28745238/effect-of-number-of-bifunctional-chelating-agents-on-the-pharmacokinetics-and-immunoreactivity-of-177lu-labeled-rituximab-a-systemic-study
#7
Mohini Guleria, Tapas Das, Chandan Kumar, Rohit Sharma, Jeyachitra Amirdhanayagam, Haladhar D Sarma, Ashutosh Dash
OBJECTIVE: Monoclonal antibodies (mAbs) have been radiolabeled with a variety of radioisotopes utilizing various kinds of bi-functional chelating agents (BFCAs) with an aim to develop suitable agents for radioimmunotherapy. The number of BFCA moieties present per antibody molecule plays a significant role in determining the pharmacokinetics and immunoreactivity exhibited by the radiolabeled antibodies. The objective of the present study is to evaluate the effect of number of BFCA moieties present per antibody molecule on the pharmacokinetics and immunoreactivity of the 177Lu-labeled Rituximab...
July 25, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28745237/anethole-inhibits-the-proliferation-of-human-prostate-cancer-cells-via-induction-of-cell-cycle-arrest-and-apoptosis
#8
Ayman Ibrahim Elkady
BACKGROUND: Prostate cancer-associated mortality is increasing at an alarming rate, which highlights the inevitability for unearthing novel agent for the management of this disease. Anethole, a major constituent of Foeniculum vulgare (fennel) essential oil, is widely used in folk medicine; it possesses anti-oxidant, anti-inflammatory, anti-proliferative and tumoricidal potentialities. OBJECTIVE: The current research was conducted to assess the impact of anethole on prostate cancer cell line, PC-3, and to delineate the molecular mechanism of action...
July 25, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28745236/synthesis-of-pyridine-and-spiropyridine-derivatives-derived-from-2-aminoprop-1-ene-1-1-3-tricarbonitrile-together-with-their-c-met-kinase-and-antiproliferative-evaluations
#9
Rafat Milad Mohareb, Amr S Abouzied, Nermeen S Abbas
OBJECTIVE/METHOD: The multi-component reaction of 2-aminoprop-1-ene-1,1,3-tricarbonitrile (1) with aromatic aldehydes 2a-c and malononitrile (3a) or ethyl cyanoacetate (3b) to give the pyridine derivatives 5a-f. Compounds 5a-c were found to react with either hydrazine hydrate (6a) or phenylhydrazine (6b) to give 2-pyrazolylpyridine derivatives 7a-f, respectively. On the other hand, compound 1 reacted with cyclopentanone (8a) or cyclohexanone (8b) and malononitrile (3a) or ethyl cyanoacetate (3b) to give the spiro derivatives 9a-d, respectively...
July 25, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28745235/effects-of-ascorbic-acid-on-tax-nf-%C3%AE%C2%BAb-and-mmp-9-in-human-t-cell-lymphotropic-virus-type-1-positive-malignant-t-lymphocytes
#10
Steve Harakeh, Jihane Khalife, Elias Baydoun, Rania Azar, Ahmed Al-Hejin, Elie Barbour, Esam Azhar, Aleksandra Niedzwiecki, Soad Al Jaouni, Mona Diab-Assaf, Mohammad Amjad Kamal, Mathias Rath
BACKGROUND: HTLV-1 is a retrovirus that infects CD4-positive cells and leads to Adult T-cell leukemia by constitutive activation of nuclear factor kappa B. Ascorbic acid (AA) is an essential nutrient that possess anti-proliferative and pro-apoptotic activity against a number of malignant cell lines. This study delineates the effect of AA on Tax protein expression as well as NF-κB and MMP9 activity in two HTLV-1-positive leukemia cells (HuT-102 and C91-PL). METHODS: The cytotoxic and antiproliferative effect of AA were studied by LDH release and MTT tests respectively...
July 25, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28730964/ccl2-is-modulated-by-cytokines-and-ppar-g-in-anaplastic-thyroid-cancer
#11
Silvia Martina Ferrari, Giusy Elia, Simona Piaggi, Enke Baldini, Salvatore Ulisse, Mario Miccoli, Gabriele Materazzi, Alessandro Antonelli, Poupak Fallahi
BACKGROUND AND OBJECTIVE: Chemokine (C-C motif) ligand (CCL)2, the prototype Th2 chemokine, is secreted by tumor cells, and has growth promoting effects. Whether CCL2 protumorigenic activities will be validated, then CCL2 and its receptor CCR2 may be therapeutic targets in cancer. METHODS: We tested in "primary human anaplastic thyroid carcinoma (ATC) cells" (ANA) versus "normal thyroid follicular cells" (TFC): a) CCL2 secretion basally, after IFN-g and/or TNF-a stimulation; b) PPARg activation by thiazolidinediones (TZDs), rosiglitazone or pioglitazone, on CCL2 secretion, and on proliferation and apoptosis in ANA...
July 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28730963/increased-expression-of-ire1%C3%AE-associates-with-the-resistant-mechanism-of-osimertinib-azd9291-resistant-non-small-cell-lung-cancer-hcc827-osir-cells
#12
Zheng-Hai Tang, Min-Xia Su, Xia Guo, Xiao-Ming Jiang, Lin Jia, Xiuping Chen, Jin-Jian Lu
BACKGROUND: Osimertinib (OSI), also known as AZD9291, is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that has been approved for the treatment of non-small cell lung cancer (NSCLC) patients. OBJECTIVE: Establishment of the OSI-resistant HCC827/OSIR cell line and study of its resistant mechanism. METHOD: The anti-proliferative effect was studied through MTT and colony formation assays. The protein expression was detected by Western blot assay...
July 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28730962/phosphonium-salt-displays-cytotoxic-effects-against-human-cancer-cell-lines
#13
Dhanyalayam Dhanya, Giuseppe Palma, AnnaRita Cappello, Annaluisa Mariconda, Maria Stefania Sinicropi, Francesca Giordano, Vitale Del Vecchio, Anna Ramunno, Claudio Arra, Pasquale Longo, Carmela Saturnino
Aims/ Objective: Phosphonium salts are compounds whose structural characteristics enable them to cross the plasma and mitochondrial membrane with ease. Cancer cells have higher plasma membrane potentials than normal cells, phosphonium salts selectively accumulate in the mitochondria of neoplastic cells and inhibit mitochondrial function. METHOD: In the presente work, we investigate the cytotoxic activity of lipophilic phosphonium salt (11-methoxy11-oxo-undecyl) triphenylphosphonium bromide (MUTP) as well as of two new phosphine oxide salts, 3,3'-(methylphosphoryl) dibenzenaminium chloride (SBAMPO) and 3,3' (phenylphosphoryl) dibenzenaminium chloride (SBAPPO) on the proliferation of breast cancer cell line (MCF-7) and human uterin cervix adenocarcinoma cells (HeLa)...
July 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28730961/novel-fluorinated-porphyrins-sensitize-tumor-cells-to-photodamage-in-normoxia-and-hypoxia-synthesis-and-biocompatible-formulations
#14
Elizaveta V Belyaeva, Alina A Markova, Dmitry N Kaluzhnyb, Andrei L Sigan, Lev L Gervitz, Aida N Ataeva, Nikolai D Chkanikov, Alexander A Shtil
: Background. Hypoxia renders tumor cells refractory to treatment. One way to overcome this problem is the design of drug delivery systems that contain the antitumor agent within an oxygen supply medium. OBJECTIVE: to evaluate whether the perfluorocarbon liquids (capable of retaining up to 50% v/v amounts of O2 gas) can be tools for delivery of photosensitizers to hypoxic tumors. METHOD: We synthesized a series of compounds in which fluoroaliphatic or fluoroaromatic moieties were conjugated to the porphyrin ring in meso-positions...
July 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28707574/recent-progress-of-nano-drug-delivery-system-for-liver-cancer-treatment
#15
Feilong Zhou, Fangfang Teng, Peizong Deng, Ning Meng, Zhimei Song, Runliang Feng
Liver cancer is one of serious diseases which threaten human life and health. Studies on the treatment of liver cancer have attracted widespread attention. Application of nano-drug delivery system (NDDS) can not only improve selective drug delivery to liver tissue and improve the bioavailability of drug, but also can reduce the side effects of drugs when it is specially modified in the respects of structure modification or specific target molecules decoration. This review will address the latest development of liver-targeted drug delivery system...
July 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28707573/synthesis-radiosynthesis-and-metabolism-of-131i-y-c-cgrraggsc
#16
Jilai Xie, Donghui Pan, Mudan Lu, Xuan Chen, Yu Chen, Ting Zhang, Yan Xie, Huan Zhou, Lu Liu, Min Yang, Jiajun Wang, Daozhen Chen
BACKGROUND: The formation of the complex interleukin-11(IL-11) and IL-11 receptor (IL-11R) is closely related with tumor progression. Binding of IL-11 to the IL-11 receptor α-chain (IL-11Rα) has been suggested as a target for human cancer. The cyclic peptide c(CGRRAGGSC) is a mimic of IL-11. OBJECTIVE: To explore 131I-Y-c(CGRRAGGSC) synthesis and radiosynthesis, and metabolism in SKOV3 tumor-bearing mice. METHOD: In this study, 131I labeled c(CGRRAGGSC) was designed and characterized...
July 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28699490/design-and-discovery-of-novel-quinoxaline-derivatives-as-dual-dna-intercalators-and-topoisomerase-ii-inhibitors
#17
Ibrahim H Eissa, Abeer M El-Naggar, Nour E A Abd El-Sattar, Ahmed S A Youssef
In attempt to develop new potent anti-tumor agents, a series of quinoxaline derivatives was designed and synthesized. The novel compounds were tested in vitro for their anti-proliferative activities against HePG-2, MCF-7 and HCT-116 cell lines. Additionally, DNA binding affinities as well as DNA-top II inhibitory activities of the synthesized compounds were investigated as potential mechanism for the anticancer activity. Compounds 13, 15, 16 and 19 exhibited good cytotoxicity activities against the three cell lines (IC50 ranging from 7...
July 10, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28699489/synthesis-and-evaluation-of-antioxidant-and-cytotoxicity-of-the-n-mannich-base-of-berberine-bearing-benzothiazole-moieties
#18
Bhupendra M Mistry, Young-Soo Keum, Muthuraman Pandurangan, Doo Hwan Kim, So Hyun Moon, Avinash A Kadam, Surendra Shinde, Han-Seung Shin, Rahul V Patel
The N-Mannich base of an isoquinoline alkaloid, berberine, bearing substituted benzothiazole moieties was obtained. Novel synthesized analogues were in vitro screened for antioxidant efficacy toward 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) free radicals and in vitro cytotoxicity towards cervical cancer cell lines (HeLa and CaSki), an ovarian cancer cell line (SK-OV-3) and human renal cancer cell line (Caki-2). Cytotoxicity of the compounds toward normal cell lines was examined using the Madin-Darby canine kidney (MDCK) non-cancer cell line...
July 10, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28554313/evaluation-of-multifunctional-hybrid-analogs-for-stilbenes-chalcones-and-flavanones
#19
Ali Çağır, Burcu Odacı, Mehmet Varol, İsmail Akçok, Özgür Okur, Ayşe T Koparal
Eleven simple-stilbene, chalcone, flavanone derivatives and 31 novel stilbene-fused chalcones and stilbene-fused flavanones were tested for their aromatase inhibition, anti-angiogenic and anti-proliferative properties in cancer (PC3, MCF-7) and healthy (HUVEC) cell lines. Results indicate that the simple-chalcone and flavanone derivatives were more cytotoxic than the simple-stilbenes in the both cancer cell lines. In contrast, the simple-stilbene structures were much more effective at aromatase inhibition. The cytotoxicity profiles of stilbene-fused chalcones in cancer cells imply that these molecules mostly mimic the simple chalcone structures...
May 29, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28530542/a-comparison-of-the-toxicity-of-mono-bis-tris-and-tetrakis-phosphino-silver-complexes-on-sno-esophageal-cancer-cells
#20
Zelinda Engelbrecht, Kariska Potgieter, Zenele Mpela, Rehana Malgas-Enus, Reinout Meijboom, Marianne J Cronje
Several silver(I) triphenylphosphine adducts were prepared as 1:1 to 1:4 ratios of silver nitrate to triphenylphosphine were used to determine their anticancer activity in a malignant SNO esophageal cell line. The silver-phosphine adducts include: [Ag(PPh3)]NO3 (1); [Ag(PPh3)2]NO3 (2); [Ag(PPh3)3]NO3 (3) and [Ag(PPh3)4]NO3 (4). In addition, the activity of 1-4 where compared to previously reported complexes [Ag(Ph2P(CH2)2PPh2)2]NO3 (5) and [Ag(Ph2P(CH2)3PPh2)2]NO3 (6). The cytotoxicity of complexes 1 to 6 was also evaluated in non-malignant human dermal fibroblast cells (HDF-a)...
May 22, 2017: Anti-cancer Agents in Medicinal Chemistry
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