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Anti-cancer Agents in Medicinal Chemistry

Mohammad Nabiuni, Danial Seyfi, Seyed Bahram Behzad, Kazem Parivar, Mohammad Tahmaseb, Elaheh Amini
OBJECTIVE: Metastasis phenotype is considered as a main challenge in colon cancer therapeutic methods. Furthermore, the side effects of conventional colorectal cancer treatment methods, has attracted a lot of attention into natural ingredients. The aim of the study was to assess the molecular mechanism of verbascoside as natural bio-compound in human HT29 colon cancer cells. METHODS: HT29 cells were cultured in RPMI-1640 medium containing 10% FBS and 1% penicillin/streptomycin at 37˚C and 5% CO2...
June 10, 2018: Anti-cancer Agents in Medicinal Chemistry
Zuhal Kilic-Kurt, Filiz Bakar-Ates, Bahriye Karakas, Ozgur Kutuk
A series of new pyrrolo[2,3-d]pyrimidines containing urea moieties have been synthesized and evaluated for their anticancer activity against cancer cell lines including A549, PC3, SW480 and MCF-7. Among the synthesized compounds, 9e, 10a and 10b exhibited the most potent cytotoxic activities against different cancer cell lines. Compound 10a (IC50 = 0.19 µM) was found to be the most potent derivative against PC3 cells. Compound 10b and 93 showed the strong cytotoxic activity against MCF-7 and A549 cells with IC50 value of 1...
June 4, 2018: Anti-cancer Agents in Medicinal Chemistry
Cong Zhang, Jiangfei Zhou, Shengnan Li, Kairui Cai, Xiangling Guo, Chengshui Liao, Chen Wang
The bursa of Fabricius (BF) is acknowledged as central humoral immune organ unique to birds. Bursal hexapeptide (BHP, AGCCNG) is a recently reported bursal-derived bioactive peptide. However, there are few reports of the molecular basis of the mechanism on immune induction and potential antitumor activity of BHP. In this paper, Gene microarray analyses demonstrated that BHP regulated expression of 1347 genes, of which 832 were up-regulated and 515 were down-regulated. Differentially expressed genes involved in various pathways were identified, of which 16 pathways were associated with immune responses and tumorigenic processes...
June 3, 2018: Anti-cancer Agents in Medicinal Chemistry
Laxmidhar Das, Manjula Vinayak
BACKGROUND: Warburg effect is characterized by upregulation of HIF-1 and c-Myc regulated LDH-A, even aerobically owing to hypoxic environment and alterations in oncogenes or tumor suppressor genes in cancer. Reduced antioxidant defence system in transformed cells favors higher ROS production, which plays a significant role in carcinogenesis and acts as an important regulator of NF-κB. In addition, various proinflammatory cytokines play active roles in maintenance and progression of cancer...
June 3, 2018: Anti-cancer Agents in Medicinal Chemistry
Raquel Pantarotto Souza, Patricia de Souza Bonfim-Mendonca, Gabrielle Marconi Zago Ferreira Damke, Analine Rosa Barquez De Assis Carvalho, Bianca Altrao Ratti, Djaceli Sampaio de Oliveira Dembogurski, Vania Ramos Sela da Silva, Sueli Oliveira Silva, Denise Brentan da Silva, Marcos Luciano Bruschi, Silvya Stuchi Maria-Engler, Marcia Edilaine Lopes Consolaro
Artepillin C (3,5-diprenyl-4-hydroxycinnamic acid) is the main bioactive component of Brazilian green propolis, and possesses, among other things, anticancer properties. However, to the best of our knowledge, there are no studies of artepillin C in cervical cancer. To explore a new therapeutic candidate for cervical cancer, we have evaluated the effects of artepillin C on cellular viability in a comprehensive panel of human cervical cancer-derived cell lines including HeLa (human papillomavirus/HPV 18-positive), SiHa (HPV 16-positive), CaSki (HPV 16- and 18-positive) and C33A (HPV-negative) cells compared to a spontaneously immortalized human epithelial cell line (HaCaT)...
June 3, 2018: Anti-cancer Agents in Medicinal Chemistry
Rafat M Mohareb, Nadia Y Megally Abdo, Karam A El-Sharkawy
BACKGROUND: Among wide range of heterocyclic steroidal derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Many pharmacological drugs containing the thiophene nucleus were known in the market. METHOD: A series of tetrahydrobenzothienopyridine derivatives were synthesized from the reaction 2-amino-3-benzoyl-4,5-dihydrobenzo[b]thiophen-6(7H)-one were synthesized and used for further heterocyclization reactions through the reaction with different reagent...
June 3, 2018: Anti-cancer Agents in Medicinal Chemistry
Xue Gao, Yuming Zhou, Xiaoqi Zheng, Hongliu Sun, Jing Zhang, Weizhong Liu, Xiaohong Pan
Peniciketal A (Pe-A) is a spiroketal compound isolated from saline soil-derived fungus Penicillium raistrickii. However, its role for biological processes has not been clarified. In this study, we for the first time investigated the anticancer effects and the underlying mechanisms of Pe-A in A549 lung cancer cells. Pe-A effectively inhibited proliferation, with IC50 values was 22.33 μM for 72 h. Mechanistic studies revealed that Pe-A caused cell cycle arrest at the G0-G1 phase by decreasing cyclinD1 expression and induced apoptosis through accelerating the mitochondrial apoptotic pathway...
June 3, 2018: Anti-cancer Agents in Medicinal Chemistry
Divya Rawat, Somi Shrivastava, Rayees Ahmad Naik, Saurabh Kumar Chhonker, Aditi Mehrotra, Raj Kumar Koiri
Liver cancer is the fifth most commonly diagnosed cancer and the second leading cause of cancer related deaths worldwide. Among the liver cancers, hepatocellular carcinoma has been reported to be responsible for 85-90% of primary liver cancer and it is the second most common cause of cancer mortality with 700,000 deaths documented annually. The major risk factors of HCC include chronic infections with the hepatitis B (HBV) or hepatitis C (HCV) virus, chronic liver diseases, alcoholism as well as dietary carcinogens, such as aflatoxins...
June 3, 2018: Anti-cancer Agents in Medicinal Chemistry
Chiara Fondello, Lucrecia Agnetti, Gerardo C Glikin, Liliana M E Finocchiaro
BACKGROUND: Three metastatic human melanoma cell lines generated from patient removed lymph nodes and spleen metastasis were established in our laboratory. OBJECTIVE: To investigate the mechanisms enhancing the cytotoxic effects of bleomycin (BLM), herpes simplex virus thymidine kinase/ganciclovir suicide gene (SG) and human interferon-β gene (hIFNβ) lipofection in early passages of these melanoma cell lines. METHODS: In these cell lines, we determined: cytotoxicity, bystander effect, lipofection efficiencies, apoptosis, necrosis, senescence, colony forming capacity and mitochondrial membrane depolarization after treatments...
June 3, 2018: Anti-cancer Agents in Medicinal Chemistry
Ilknur Ozgencli, Harun Budak, Mehmet Ciftci, Mustafa Anar
BACKGROUND: Thioredoxin reductase (E.C; TrxR) is a widely distributed flavoprotein that catalyzes the NADPH-dependent reduction of thioredoxin (Trx) in many cellular events such as DNA synthesis, DNA repair, angiogenesis, antioxidative defense, and regulating apoptosis. Although TrxR is indispensible in protecting cells against oxidative stress, the overexpression of TrxR is seen in many aggressive tumors. Therefore, targeted inhibition of TrxR has been accepted as a new approach for chemotherapy...
May 24, 2018: Anti-cancer Agents in Medicinal Chemistry
Wan Huang, Jingxiu Huang, Yu Jiang, Xuanwei Huang, Wei Xing, Yaoxuan He, Handong Ouyang
OBJECTIVE: The aim of this study was to investigate the mechanism of oxaliplatin in the induction of neuropathic pain as a symptom of chemotherapy-induced peripheral neuropathy (CIPN). METHODS: The CIPN rat model was induced with a one-time injection of oxaliplatin, and the paw withdrawal response was determined using von Frey filaments. The paw withdrawal threshold (PWT) value was recorded and the dorsal horn (DH) and dorsal root ganglion (DRG) tissues were collected...
May 24, 2018: Anti-cancer Agents in Medicinal Chemistry
Halise Inci Gul, Mehtap Tugrak, Mustafa Gul, Hiroshi Sakagami, Naoki Umemura, Baris Anil
In this study, new azafluorenones, 4-(4-fluorophenyl)-2-(4-substitutedphenyl)-5H-indeno[1,2-b]pyridin-5-one, I1-I8 were synthesized and chemical structures were elucidated by spectral analysis. All compounds were reported for the first time here. Compounds were tested in terms of cytotoxicity. They were found as cytotoxins/anticancer compounds. It was found that the leader compounds of the series were I5 and I8 according to SI, TS, PSE calculations. When PSE values were considered, the compound I5 having the chlorine had the highest PSE value as 126...
May 24, 2018: Anti-cancer Agents in Medicinal Chemistry
Henah Balkhi, Ehtishamul Haq, Taseen Guler, Syed Sana
BACKGROUND: Caffeic acid phenethyl ester and Dasatinib in combination, when used in congruous proportions and durations, present an antitumor potential for glioma in vitro, suggesting a high therapeutic potential for glioma treatment. OBJECTIVE: In the present study, we addressed the question whether CAPE and Dasatinib target multiple pathways involved in tumor growth, proliferation and development on an in vivo rat model of glioma. METHODS: Expression analysis of proteins thought to be mediating proliferation, cell motility, angiogenesis, and invasion was carried out to delineate the antineoplastic action of CAPE and Dasatinib...
May 15, 2018: Anti-cancer Agents in Medicinal Chemistry
Correa-Basurto Jose, Jose G Trujillo-Ferrara, Mendoza-Lujambio Irene, Duenas-Gonzalez Alfonso, Chavez-Blanco Alma, Martinez-Archundia Marlet, M Bello, Garcia Sanchez Jose Ruben, Fragoso-Vazquez Manuel Jonathan, Mendez-Luna David, Prestegui-Martel Berenice, Martinez-Munoz Alberto
Recent reports have demonstrated the role of the G protein-coupled estrogen receptor (GPER1) on the growth and proliferation of breast cancer cells. The coupling of GPER1 to estrogen, tamoxifen or fulvestrant triggers cellular signaling pathways (PI3K and ERK) related to cell proliferation. In an effort to develop new therapeutic strategies against breast cancer, we performed an in silico study to explore the binding pose of a set of designed G15 and G1 analogue compounds, including phenol red. First, we included a carboxyl group instead of the acetyl group from G1 to form amides with several moieties to increase the affinity for GPER1...
May 10, 2018: Anti-cancer Agents in Medicinal Chemistry
Yichao Wan, Shengzhuo He, Wei Li, Zilong Tang
Currently, cancer continues being a dramatically increasing and serious threat to public health. Although many anti-tumor agents have been developed in recent years, the survival rate of patients is not satisfactory. The poor prognosis of cancer patients is closely related to the occurrence of drug resistance. Therefore, it is urgent to develop new anti-tumor agents to make up for the deficiency. Indazoles is an important class of heterocyclic compounds possessing a variety of biological activities, such as anti-tumor, anti-bacterial, anti-inflammatory, anti-depressant and anti-hypertensive...
May 9, 2018: Anti-cancer Agents in Medicinal Chemistry
Maher Elhashash, Eman El-Bordany, Magda Marzouk, Abeer ElSayed, Tarek Nawar, Wael El-Sayed
BACKGROUND: Fused heterocyclic containing pyrazolopyridine systems have several medicinal activities including cytotoxic and carcinostatic activities. OBJECTIVE: To investigate the antiproliferative activity and associated mechanism(s) of a novel series of nicotinonitrile derivatives. METHOD: The series has been synthesized by reaction of hydrazonoyl chlorides with each of 4-(4-methoxyphenyl)-3-methyl-6-oxo-6,7-dihydro-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile and 2-amino-4-(4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-3-carbonitrile in dioxane in basic medium...
May 9, 2018: Anti-cancer Agents in Medicinal Chemistry
Ci Ren, Hui Wang, Wencheng Ding, Chun Gao, Xiaomin Li, Hui Shen, Liming Wang, Da Zhu, Peng Wu, Ding Ma
Cervical cancer is the third-most common malignant tumor among women worldwide, which seriously endangers the life and health of Chinese women. The primary etiological factor of cervical cancer is persistent infection with high-risk human papillomavirus (HR-HPV), particularly HPV16 and HPV18. HR-HPV express oncoproteins E6 and E7, both of which play key roles in the progression of cervical carcinogenesis. Zinc Finger Nucleases (ZFNs) targeting HPVE7 induce specific shear of the E7 gene, weakening the malignant biological effects, hence showing great potential for clinical transformation...
May 9, 2018: Anti-cancer Agents in Medicinal Chemistry
Mehlika Dilek Altintop, Belgin Sever, Ahmet Ozdemir, Sinem Ilgin, Ozlem Atli, Gulhan Turan Zitouni, Zafer Asim Kaplancikli
In an effort to develop potent anticancer agents, the synthesis of a series of benzothiazole-based 1,3,4-thiadiazole derivatives (1-14) was described and their cytotoxic effects on A549 human lung adenocarcinoma, MCF-7 human breast adenocarcinoma, HepG2 human hepatocellular carcinoma and NIH/3T3 mouse embryonic fibroblast cell lines were investigated using MTT assay. Phenyl-substituted compounds (8-14) were found to be more effective than naphthyl-substituted compounds (1-7) on cancer cells. Compounds 8, 9, 10, 12, 13 and 14 were identified as the most potent anticancer agents on MCF-7 and HepG2 cell lines and therefore their effects on DNA synthesis and apoptotic/necrotic cell death in MCF-7 cell line were evaluated...
May 8, 2018: Anti-cancer Agents in Medicinal Chemistry
Mahmoud Ali Abdelaziz Mahmoud, Rafat Milad Mohareb, Mashari Ahmed Alshereef
BACKGROUND: Among wide range of heterocyclic steroidal derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Many pharmacological drugs containing the steroid nucleus were known in the market. OBJECTIVE: Our main aim of this work was to synthesis a seies of heterocyclic compounds especially thiophene and thienopyridine derivatives containing the estrone nucleuous. The synthesized compounds possising antitumor and kinases inhibitions...
May 7, 2018: Anti-cancer Agents in Medicinal Chemistry
Maryam Ranjpour, Deepshikha Pande Katare, Saima Wajid, Swatantra Kumar Jain
The network interactions link human disease proteins to regulatory cellular pathways leading to better understanding of protein functions and cellular processes. Revealing the network of signaling pathways in cancer through protein-protein interactions at molecular level enhances our understanding of hepatocellular carcinoma (HCC). A rodent model for study of HCC was developed by administrating N-Nitrosodiethylamine (DEN) and 2-aminoacetylfluorine (2-AAF) to male Wistar rats. Proteomic approaches such as 2D- Electrophoresis, PD-Quest, MALDI-TOF-MS and Western blot analyses have been used to identify, characterize and validate the differentially expressed proteins in HCC-bearing animals vis-a-vis controls...
May 7, 2018: Anti-cancer Agents in Medicinal Chemistry
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