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Anti-cancer Agents in Medicinal Chemistry

Tohid Kazemi, Najibeh Shekari, Faezeh Asghari, Navideh Haghnavaz, Dariush Shanehbandi, Vahid Khaze, Behzad Baradaran
BACKGROUND: MicroRNAs are noncoding RNAs which play critical roles in response to anti-cancer agents. Let-7a and miR-21 are well-known tumor-suppressor and oncomiR miRNAs, respectively. They are involved in tumorigenesis of gastric cancer and have potential to be used as markers for response to the therapy. OBJECTIVE: We aimed to study alterations in the expression of let-7a and miR-21 and their targets in gastric cancer cell lines after treatment with docetaxel...
December 12, 2018: Anti-cancer Agents in Medicinal Chemistry
Anna Belanova, Darya Beseda, Victor Chmykhalo, Alisa Stepanova, Mariya Belousova, Vera Khrenkova, Nikolaos Gavalas, Peter Zolotukhin
BACKGROUND: Berberine has multitudinous anti-cancer stem cells effects making it a highly promising candidate substance for the next-generation cancer therapy. However, berberine modes of action predispose it to significant side-effects that probably limit its clinical testing and application. MATERIALS AND METHOD: HeLa cells were treated with two concentrations of berberine (30 and 100 μM) for 24 hours to asses the functioning of the NFE2L2/AP-1, NFκB and HIF1A pathways using 22 RNAs expression qPCR-based analysis...
December 11, 2018: Anti-cancer Agents in Medicinal Chemistry
Evgenii S Mozhaitsev, Alexandra L Zakharenko, Evgeniy V Suslov, Dina V Korchagina, Olga D Zakharova, Inna A Vasil'eva, Arina A Chepanova, Ellena Black, Jinal Patel, Raina Chand, Jóhannes Reynisson, Ivanhoe K H Leung, Konstantin P Volcho, Nariman F Salakhutdinov, Olga I Lavrik
BACKGROUND AND OBJECTIVE: The DNA repair enzyme tyrosyl-DNA-phosphodiesterase 1 (TDP1) is a current inhibition target to improve the efficacy of cancer chemotherapy. Previous studies showed that compounds combining adamantane and monoterpenoid fragments are active against TDP1 enzyme. This investigation is focused on the synthesis of monoterpenoid derived esters of 1-adamantane carboxylic acid as TDP1 inhibitors. METHOD: A new esters were synthesized by the interaction between 1-adamantane carboxylic acid chloride and monoterpenoid alcohols...
December 6, 2018: Anti-cancer Agents in Medicinal Chemistry
Yang Liu, Jingyin Zhang, Shuyun Feng, Tingli Zhao, Zhengzheng Li, Lai Wang, Puhai Wang, Hongzhi Du, Shengtao Yuan, Li Sun
OBJECTIVE: The aim of this study is to investigate the inhibitory effect of camptothecin derivative 3j on non-small cell lung cancer (NSCLCs) cells and the potential anti-tumor mechanisms. BACKGROUND: Camptothecin compounds are considered as the third largest natural drugs which are widely investigated in the world and they suffered restriction because of serious toxicity, such as hemorrhagic cystitis and bone marrow suppression. METHODS: Using cell proliferation assay and S180 tumor mice model, a series of 20(S)-O-substituted benzoyl 7-ethylcamptothecin compounds were screened and evaluated the antitumor activities in vitro and in vivo...
December 6, 2018: Anti-cancer Agents in Medicinal Chemistry
C P Coyne, Lakshmi Narayanan
Background - Traditional chemotherapeutics of low-molecular weight diffuse passively across intact membrane structures of normal healthy cells found in tissues and organ systems in a non-specific unrestricted manner which largely accounts for the induction of most sequelae which restrict dosage, administration frequency, and duration of therapeutic intervention. Molecular strategies that offer enhanced levels of potency, greater efficacy and broader margins-of-safety include the discovery of alternative candidate therapeutics and development of methodologies capable of mediating properties of selective "targeted" delivery...
December 3, 2018: Anti-cancer Agents in Medicinal Chemistry
Hua Li, Xin Xu, Yang Liu, Shunle Li, Di Zhang, Xiaofen Meng, Le Lu, Yiming Li
In this study, we identified MMP7 as one of the most up-regulated genes in T-DM1 resistant NCI-N87 gastric adenocarcinoma cells compared to matched naïve cell lines. Next, we established T-DM1 resistant NCI-N87 cell lines by exposed to T-DM1 in vitro while qPCR and Western blot showed elevated expression of MMP7 in T-DM1 resistant NCI-N87 cells. Moreover, exogenous overexpression of MMP7 promotes T-DM1 resistance and tumor growth in NCI-N87 cell lines while MMP7 knock-down enhanced sensitivity to T-DM1 in T-DM1 resistant NCI-N87 cell lines established previously...
December 2, 2018: Anti-cancer Agents in Medicinal Chemistry
Shuo Yu, Hui Ren, Yang Li, Xuan Liang, Qian Ning, Xue Chen, Mingwei Chen, Tinghua Hu
Drug-resistant phenotypes have been a major obstacle to cisplatin treat in non-small cell lung cancer. We found that AXL receptor tyrosine kinase (AXL) is one of the most up-regulated kinase-encoding genes in cisplatin-resistant lung adenocarcinoma. Both in vitro and in vivo, AXL promotes tumor growth and its expression is enriched in cisplatin-resistant lung adenocarcinoma. Clinically, AXL expression is correlated to the poor prognosis of lung cancer patients. Additionally, the activation of AXL is homeobox A4 (HOXA4)-dependent...
December 2, 2018: Anti-cancer Agents in Medicinal Chemistry
Anuka S Mendis, M Ira Thabrew, Meran K Ediriweer, Sameera R Samarakoon, Kamani H Tennekoon, Achyut Adhikari, E Dilip de Silva
Background/ Objective: Vernonia zeylanica (L) less is an endemic plant to Sri Lanka. The present study was designed to isolate potential cytotoxic compound/s from chloroform and ethyl acetate extracts of V. zeylanica by bio-activity guided isolation and to evaluate its anti-proliferative effects in three breast cancer phenotypes (MCF -7, MDA-MB-231, SKBR-3). METHOD: Combined chloroform and ethyl acetate extracts were subjected to chromatographic separations to isolate a compound (1) and the structure of the isolated compound was elucidated using 1H, 13C and mass spectroscopic techniques...
November 28, 2018: Anti-cancer Agents in Medicinal Chemistry
Ahmed Kamal, Siddiq Pasha Shaik, T Srinivasa Reddy, Satish Sunkari, A V Subba Rao, Korrapati Suresh Babu
A new series of 3-arylaminopropenone linked 2-arylbenzo[d]imidazo[2,1-b]thiazole conjugates (4a-z) were synthesized and screened for cytotoxic activity against four human cancer cell lines. These conjugates showed moderate to good antiproliferative activity in the range of 1.6 - 48.5 µM. Some conjugates like 4e, 4f, 4g, 4k, 4m, 4r and 4t exhibited good antiproliferative activity and the insights of structure activity relationships were developed. Among them, conjugate 4e showed significant potential particularly against HeLa cell line with IC50 value 1...
November 26, 2018: Anti-cancer Agents in Medicinal Chemistry
Subbarayan Sarathbabu, Satheesh Kumar Marimuthu, Souvik Ghatak, Subramanian Vidyalakshmi, Gurusubramanian Guruswami, Sankar Kumar Ghosh, Selvi Subramanian, Wenqing Zhang, Nachimuthu Senthil Kumar
OBJECTIVE: To explore the cytotoxic and apoptotic activity of the pierisin-6 protein in HPV HeLa and HepG2 cell lines. METHODS: In this study, isolation and purification of cytotoxic prierisin-6 from the larvae of Pieris napi by affinity column chromatography techniques.Characterization of full-length mRNA of pierisin-6 gene was performed using 3'/5' RACE PCR. The quantitative RT-PCR used to study the developmental stage-specific expression of pierisin-6 mRNA. The most effective concentration of pierisin-6 protein was determined by measuring cell proliferation...
November 26, 2018: Anti-cancer Agents in Medicinal Chemistry
Karolina Kró Lewska-Goliñska, Marcin J Cieślak, Milena Sobczak, Rafał Dolot, Ewa Radzikowska-Cieciura, Mariola Napiórkowska, Iwona Wybrañska, Barbara Nawrot
BACKGROUND: Novel derivatives of benzo[b]furan were found to be highly toxic towards human chronic myelogenous (K562), acute myelogenous (HL-60) and acute lymphoblastic (MOLT-4) leukemia cells. OBJECTIVE: Characterization of the biological activity of novel benzofurans (influence on apoptosis, mitogen activated protein kinases and on the cell cycle). Identification of cellular protein(s) targeted by test benzofurans and defining the mechanism of action. METHOD: chemical synthesis, fluorescence assays, flow cytometry, gene expression by DNA microarray and real time RT-PCR, western blotting, cytotoxicity assays, pull-down assay, mass spectroscopy, in vitro polymerization of tubulin, molecular docking...
November 22, 2018: Anti-cancer Agents in Medicinal Chemistry
Xue-Qing Zhang, Lu-Ting Yu, Pei Du, Tian-Qi Yin, Zhi-Yuan Zhang, Ying Xu, Xiang Li, You-Jie Li, Min Wang, Chen Luo
Regenerating islet-derived gene family member 4 (Reg4), a well-investigated growth factor in the regenerative pancreas, has recently been reported to be highly associated with a majority of gastrointestinal cancers. Pathological hyper-expression or artificial over-expression of Reg4 causes acceleration of tumor growth, migration, and resistance to chemotherapeutic 5-Fluorouracil (5-FU). Until now, no method has been successfully established for eliminating the effects of Reg4 protein. This study reports the production of an engineered immunoglobin, a single-chain variable fragment (scFv-Reg4), to specifically bind Reg4 and block the bioactivity...
November 21, 2018: Anti-cancer Agents in Medicinal Chemistry
Jarosław Lewkowski, Edyta Rzeszotarska, Agnieszka Matusiak, Marta Morawska, Gabriela Gajek, Karolina Nowak, Renata Kontek
Background The anticancer activity of aminophosphonic derivatives has been described extensively, some recent papers included furan-derived aminophosphonates and their cytostatic action against various cancer cells Objective A series of twelve furan-derived dibenzyl and diphenyl aminophosphonates 2a-f and 3a-f was synthesized and tested in aspect of their cytotoxic action on two cell lines of colorectal cancer: HT29 and HCT116. Seven of them are new compounds, while the rest five have already been published by us, together with their cytotoxic action against squamous esophageal cancer cells...
November 21, 2018: Anti-cancer Agents in Medicinal Chemistry
Élida Batista Vieira Sousa Cavalcanti, Mayara Barbalho FÉlix, Luciana Scotti, Marcus Tullius Scottia
Cancer is the main cause of death, so the search for active agents to be used in the therapy of this disease, is necessary. According to studies conducted, substances derived from natural products have shown promise in this endeavor. To these researches, one can associate the aid of computational chemistry, which is increasingly gaining in popularity, due to the possibility of developing alternative strategies that could help to choose an appropriate set of compounds, avoiding unnecessary expenses with resources that would generate unwanted substance...
November 18, 2018: Anti-cancer Agents in Medicinal Chemistry
Oscar Jovan Zacarías-Lara, David Méndez-Luna, Gustavo Martínez-Ruíz, José Ruben García-Sanchéz, Manuel Jonathan Fragoso-Vázquez, Martiniano Bello, Elvia Becerra-Martínez, Juan Benjamín García-Vázquez, José Correa-Basurto
Reports have demonstrated the role of the G protein-coupled estrogen receptor (GPER) in growth and proliferation of breast cancer cells. In an effort to develop new therapeutic strategies against breast cancer, we employed an in silico study to explore the binding modes of tetrahydroquinoline 2 and 4 to be compared with the reported ligands G1 and G1PABA. This study aimed to design and filtered ligands by in silico studies determining their Lipinsky rule, toxicity and binding properties with GPER to achieve experimental assays as anti-proliferative compounds of breast cancer cell lines...
November 18, 2018: Anti-cancer Agents in Medicinal Chemistry
Izabela Łasiñska, Jacek Mackiewicz
Despite the great progress in the development of targeted therapies for different types of cancer utilizing monoclonal antibodies (e.g., cetuximab for colorectal cancer and head and neck cancer therapy), kinase inhibitors (e.g., sorafenib for kidney cancer and gastrointestinal stromal tumours therapy), and immunomodulatory treatments (e.g., nivolumab and pembrolizumab for melanoma therapy and lung cancer therapy), there is still a need to search for new, more effective treatments. Integrins are responsible for intercellular adhesion and interacting with the cellular matrix...
November 18, 2018: Anti-cancer Agents in Medicinal Chemistry
Rafa S Almeer, Ahmed M Aref, Romisa A Hussein, Mohamed S Othman, Ahmed E Abdel Moneim
BACKGROUND: Berberine and cinnamic acid are natural compounds that exhibit potent anticancer activities through distinct molecular mechanisms. OBJECTIVE: In the present study, we aimed to investigate the proapoptotic potential of cinnamic acid and berberine in cancer cells by examining their effect on the expression of proapoptotic and antiapoptotic genes. Moreover, the effects of berberine and cinnamic acid on the antitumor activity of cisplatin were investigated in Ehrlich solid tumor-bearing mice...
November 16, 2018: Anti-cancer Agents in Medicinal Chemistry
Duong Tien Anh, Nguyen Thi Thuan, Pham-The Hai, Le-Thi-Thu Huong, Nguyen Thi Kim Yen, Byung Woo Han, Eun Jae Park, Yeo Jin Choi, Jong Soon Kang, Van Thi My Hue, Sang-Bae Han, Nguyen-Hai Nam
BACKGROUND: Histone Deacetylase (HDAC) inhibitors represent an extensive class of targeted anti-cancer agents. Among the most explored structure moieties, hydroxybenzamides and hydroxypropenamides have been demonstrated to have potential HDAC inhibitory effects. Several compounds of these structural classes have been approved for clinical uses to treat different types of cancer, such as givinostat (ITF2357) and belinostat (PXD-101). AIMS: This study aims at developing novel HDAC inhibitors bearing N-hydroxybenzamides and N-hydroxypropenamides scaffolds with potential cytotoxicity against different cancer cell lines...
November 13, 2018: Anti-cancer Agents in Medicinal Chemistry
Fan Zhongqi, Sun Xiaodong, Chen Yuguo, Lv Guoyue
BACKGROUND: Hepatocellular Carcinoma (HCC) is one of the most common cancers with high mortality rate. The effects of most therapies are limited. The immune checkpoint blockade (ICB) improves the prognosis in multiple malignancies. The application of immune checkpoint blockade to hepatocellular carcinoma patients has recently started. Early phase clinical trials have shown some benefits to cancer patients. METHODS/RESULTS: This review focuses on the immune system of liver and clinical trials of immune checkpoint blockage therapies...
November 13, 2018: Anti-cancer Agents in Medicinal Chemistry
Dattatraya G Raut, Sandeep B Patil, Vikas D Kadu, Mahesh G Hublikar, Raghunath B Bhosale
A novel series of 1-thiocarbamoyl pyrazole derivatives (4a-g) were accomplished by reacting pyrazolealdehyde 1 with appropriate aromatic ketone by using polyethylene glycol (PEG-300) as green reaction medium as well as catalyst to yield chalcone 2. The chalcones 2 reacted with thiosemicabazide 3 to yield asymmetric 1-thiocarbamoyl pyrazoles 4. The structural interpretations of newly synthesized compounds were based on chemical and spectroscopic evidences. The synthesized compounds were evaluated for their in vitro anticancer, antioxidant (H2O2, DPPH, SOR and NO radical scavenging activity) and anti-inflammatory activities...
November 12, 2018: Anti-cancer Agents in Medicinal Chemistry
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