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Anti-cancer Agents in Medicinal Chemistry

Shutao Ma, Xinjie Gu
BACKGROUND: The 26S proteasome is a proteolytic complex of multimeric protease, which operates at the executive end of the Ubiquitin-Proteasome System (UPS) and degrades the polyubiquitylated proteins Methods: After a brief introduction of 26S proteasome and Ubiquitin-Proteasome System (UPS), this review focuses on the structure and function of the 26S proteasome in intracellular protein level regulation. Then, physiological regulation mechanisms and processes are elaborated. In addition, the advantages and defects of approved 26S proteasome inhibitors were discussed...
August 13, 2018: Anti-cancer Agents in Medicinal Chemistry
Souad A El-Metwally, Ali K Khalil, Abeer M El-Naggar, Wael M El-Sayed
ackground: Developing new chemotherapeutic agents with molecular targets, larger margin of safety against normal cells and low cost is the target many scientists try to achieve. OBJECTIVE: The present study was undertaken to investigate the anticancer activity of a novel series of thiophene compounds and the molecular mechanisms associated. METHODS: A series of novel heterocyclic compounds including pyrimidine derivatives (2, 3, 4, 5 8, 11, 12, 13, 14, and 15), thiophene derivatives (6, 7, and 10) and oxoisothiazolidine derivative (9) was synthesized from 4,5,6,7-tetrahydrobenzo[b] thiophene (1)...
August 13, 2018: Anti-cancer Agents in Medicinal Chemistry
Habib Zarredar, Khalil Ansarin, Behzad Baradaran, Najibeh Shekari, Shirin Eyvazi, Fateme Safari, Safar Farajnia
BACKGROUND: MicroRNAs (miRNAs) play an important role in regulation of various genes involved in cell growth, development and the maintenance of body homeostasis. They are closely linked to different human diseases, in particularly in cancers. Amplification and overexpression of some miRNAs that called 'oncomiRs' or down-regulation of tumor suppressor miRNAs are associated with genetic alterations that are sufficient to drive tumorigenesis in humans. Lung cancer is the leading cause of cancer related deaths worldwide...
August 8, 2018: Anti-cancer Agents in Medicinal Chemistry
Wided Kebsa, Mesbah Lahouel, Hassiba Rouibah, Zihlif Malek, Ahram Mamoun, Abu-Irmaileh Bachaer, Mustafa Ebtihal, J Al-Ameer Hamzeh, Al Shhab Mohammad
BACKGROUND: Lung cancer is one of the most common malignancies with the highest incidence and mortality rate worldwide. Multidrug resistance (MDR) continues to pose a major challenge for the clinicians and pharmacologists to effectively treat this disease. New approach using natural substances with moderate or low cytotoxic properties become a promising hope for reversing multi drug resistance due to pgp- over expression. OBJECTIVE: This study aims to explore the efficacy of Algerian propolis in reversing multidrug resistance and sensitizing chemo-resistant lung cancer cells (A549/DOX) to chemotherapy with DOX...
August 7, 2018: Anti-cancer Agents in Medicinal Chemistry
Mohammad Ali Ebrahimzadeh, Alireza Tafazoli, Javad Akhtari, Pourya Biparva, Shahram Eslami
New modifications in nanoparticles changed the applications of them obviously. Green synthesis of nanoparticles and their biomedical utilizations have been the focus of increasing attention in recent years. Silver nanoparticles (AgNPs) demonstrated surprising effects and many advantageous features for cancer therapy. Investigations indicated the anticancer activity of AgNPs in different ways, comprising cell cycle arrest, DNA damaging and apoptosis, alteration of P53 function, up/down regulation of some important cytokine genes and so on...
August 7, 2018: Anti-cancer Agents in Medicinal Chemistry
Lukmanul Hakkim, Seemaisamy Revathi, Govind Rajan, Gattu Sampath, Ramesh Kumar, Mohammed Al Buloshi, Sidgi Syed Anwar, Hamid Bakshi, Kayalvizhi Nagarajan
BACKGROUND: Colon cancer is the most aggressive form of cancers, that causes 0.5 million deaths per year around the globe. Targeting colon cancer by conventional therapeutic options elicits toxicity. Traditional medicines take lead to alleviate the existing clinical challenges. OBJECTIVE: To investigate anti bacterial activity against Helicobacter Pylori and in vitro anti colon cancer activity by Acacia nilotica extract (ACE) and its active constituent pyrogallol...
August 5, 2018: Anti-cancer Agents in Medicinal Chemistry
Yuanyuan Yue, Yuping Xu, Lirong Huang, Donghui Pan, Zhicheng Bai, Lizhen Wang, Runlin Yang, Junjie Yan, Huizhu Song, Xiaotian Li, Min Yang
Glucagon-like peptide 1 receptor (GLP-1R) is an important biomarker for diagnosis and therapy of the endocrine cancers due to overexpression. Recently, in human prostate cancer cell lines the receptor was also observed, therefore it may be a potential target for the disease. 18F-Al-NOTA-MAL-Cys39-exendin-4 holds great promise for GLP-1R. Therefore, the feasibility of the 18F-labeled exendin-4 analog for prostate cancer imaging was investigated; 2) Methods: New probe 18F-Al-NOTA-MAL-Cys39-exendin-4 was made through one-step notation, quality controlled and stability in vitro analyzed...
July 31, 2018: Anti-cancer Agents in Medicinal Chemistry
T Kiran Kishore Kranthi, Abdul Basit Baba, Jaganathan Kowshik, G Bhanuprakash Reddy, Siddavaram Nagini
BACKGROUND AND OBJECTIVES: Aldose reductase (AR), a polyol pathway enzyme that mediates diabetic complications is implicated in tumour development and progression. This study was undertaken to determine whether gedunin, a neem limonoid prevents the hallmarks of cancer by inhibiting AR and the associated downstream PI3K/Akt/mTOR/ERK/NF-κB signalling axis in the SCC131 oral cancer cell line. METHODS: The expression of AR and key molecules involved in cell proliferation, apoptosis, autophagy, invasion and angiogenesis was analysed by qRT-PCR, and immunoblotting...
July 30, 2018: Anti-cancer Agents in Medicinal Chemistry
Mala Sharma, Chitranshu Pandey, Neha Sharma, M A Kamal, Usman Sayeed, Salman Akhtar
BACKGROUND: Nanotechnology pictures a breakthrough in the domain of cancer therapy owing to its novel properties and functions. This technology is quite amendable as it allows the scientists to engineer drug nanoparticles of dimensions 10nm - 500nm permitting them to pass via leaky vasculature of tumorigenic microenvironment with higher specificity, reduced cytotoxicity and effective release without any after effects. The central part of the review zooms onto the role of nanoparticles and their targeted delivery for the cure of cancer...
July 20, 2018: Anti-cancer Agents in Medicinal Chemistry
Emmanuel Adefemi Adeniji, Fisayo Andrew Olotu, Mahmoud Soliman
The difficulty in druggability has presented a hurdle in the treatment of cancer diseases associated with dysfunctional mutant K-ras. This has so far impeded the emergence of suitable inhibitors to discontinue its aberrant activities. Despite the identification of different interactive sites, limited information exists in literature about their characteristics that could aid the design and development of appropriate inhibitors that could bind at its catalytic or effector binding sites, thereby disrupting oncogenic activities...
July 17, 2018: Anti-cancer Agents in Medicinal Chemistry
Raji Reddy Chada, Nilesh Sasane, Muppidi Subbarao, Reddi Rani Valleti, Jonnalagadda Vijaykumar, Bhukya Supriya, Surender Singh Jadav, Ramesh Ummanni
BACKGROUND: The anti mitotic activity of podophyllotoxin derivative targeting tubulin enzyme proved them as strong polymerization inhibitors. The introduction of heteroatom along with different heteroaryl systems in naturally obtained lignans created a latitude for design of bioactive components. A novel one pot sequential propargylation/cycloaddition reaction strategy has been followed to synthesize triazolo-heterolignans. OBJECTIVE: To screen anti-proliferative activity of novel heterolignans and to determine their mode of action Methods: SRB assay, Cytotoxicity evaluation, PI uptake for analysis of cell cycle, caspase-3 activity, Western blot analysis and Immunofluorescence and molecular docking studies...
July 17, 2018: Anti-cancer Agents in Medicinal Chemistry
Sercan Ergun, Serkan Guney, Ebru Temiz, Nina Petrovic, Sezgin Gunes
Background In recent years, targeted cancer treatment methods at various molecular levels have been developed for non-small cell lung cancer (NSCLC), one of two major subtypes of lung cancer. miRNA-based clinical trials are currently the preferred targeted therapeutic strategy. Also, ceRNAs (competing endogenous RNA) would be the newest and the most effective approach to uncover novel interactions between mRNAs and miRNAs in NSCLC carcinogenesis. There are many factors influencing on efficiency of a miRNA to suppress or silence translation of the target mRNA...
July 17, 2018: Anti-cancer Agents in Medicinal Chemistry
Amany S Mostafa, Waleed A Bayoumi, Mohamed El-Mesery, Abdelaziz Elgaml
BACKGROUND: Two series of 3,4-dihydropyrimidin-2(1H)-one derivatives were designed based on the main structural features characterizing reported anticancer compounds with potent VEGFR-2 inhibiting activity. Target compounds were synthesized, and investigated for their in vitro anticancer activity. RESULT: Of these derivatives, compound 8b possessed significant activity against Caco-2 (IC50 of 24.9 µM) and MCF7 (IC50 of 29.4 µM), compound 10 showed excellent potency against HCT-116 (IC50 of 32...
July 17, 2018: Anti-cancer Agents in Medicinal Chemistry
Daipeng Xiao, Fen He, Dongming Peng, Junying Peng, Min Zou, Yanfei Liu, Zhenbao Liu
BACKGROUND: Berberine (BBR), an isoquinoline plant alkaloid isolated from plants such as Coptis chinensis and Hydrastis canadensis, own multiple pharmacological activities. OBJECTIVE: In this study, seven BBR derivatives were synthesized and their anticancer activity against HeLa cervical and A549 human lung cancer cell lines were evaluated in vitro. METHODS: The anti-cancer activity was measured by MTT assay, and apoptosis was demonstrated by the annexin V-FITC/PI staining assay...
July 17, 2018: Anti-cancer Agents in Medicinal Chemistry
Theivendren Panneerselvam, Selvaraj Kunjiappan, Balasubramanian Somasundaram, Shrinivas D Joshi, Indhumathy Murugan, Murugesan Sankaranarayanan, Sankarganesh Arunachalam
PURPOSE: To investigate N-succinyl chitosan nanoparticles (NSC NPs) encapsulation with Dunaliella bardawil (D. bardawil) biomass for high utilization enhanced effectiveness and least side effects for anticancer activity. METHODS: The potential bioactive compounds from D. bardawil biomass was encapsulate NSC NPs by ionotropic gelation method and to characterize its molecular shape, particle size, stability and polydispersity index using FTIR, XRD, SEM, TEM and Zetasize Nano analyzer...
June 28, 2018: 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
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