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Anti-cancer Agents in Medicinal Chemistry

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https://www.readbyqxmd.com/read/29237384/ros-scavenging-and-anti-tyrosinase-properties-of-crocetin-on-b16f10-murine-melanoma-cells
#1
Seyed Hamed Hashemi-Shahri, Alireza Golshan, Seyed Ahmad Mohajeri, Javad Baharara, Elaheh Amini, Farzaneh Salek, Amirhossein Sahebkar, Zahra Tayarani-Najaran
BACKGROUND: Crocus sativus (Iridaceae) has been traditionally used in the Iranian folk medicine and as a culinary additive. Major components of the plant that are responsible for biological properties are saffranal, crocin, picrocrocin and crocetin. Although the level of crocetin is not high, some of the important activities of saffron such as antioxidant activity have been attributed to crocetin. OBJECTIVE: In the present study, we investigated the effects of crocetin on melanogenesis in B16 melanoma cells...
December 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29237383/the-effect-of-flubendazole-on-adhesion-and-migration-in-sw480-and-sw620-colon-cancer-cells
#2
Veronika Hanusova, Lenka Skalova, Vera Kralova, Petra Matouskovs
Colon cancer is the most common type of gastrointestinal cancer. Despite advances during the last two decades, the efficacy of colorectal cancer treatment is still insufficient and new anticancer agents are necessary. In our study, colon cancer cells derived from a primary tumor (SW480) and lymph node metastasis (SW620) from the same patient were used and compared. The effect of FLU on cell adhesion and migration was monitored using the x-CELLigence Real-Time Cell Analysis system. Expressions of molecules involved in adhesion and migration were analyzed using RT-PCR and western blot...
December 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29219059/inhibition-of-intercellular-communication-between-prostate-cancer-cells-by-a-specific-anti-steap-1-single-chain-antibody
#3
Seyed-Alireza Esmaeili, Foroogh Nejatollahi, Amirhossein Sahebkar
BACKGROUND: Six-Transmembrane epithelial antigen of the prostate-1 (STEAP-1) is present at the intercellular junctions of the secretory epithelium of prostate and is overexpressed in all steps of prostate cancer. STEAP-1 acts as a transporter protein or a putative channel between cancer cells while it has limited expression in normal human tissues. This protein has been suggested as an attractive target for prostate cancer immunotherapy. OBJECTIVE: This study aimed at the development of a specific single chain fragment variable (scFv) antibody against STEAP-1 epitope and testing the inhibitory effect of the selected scFv antibody in blocking gap junctions between tumor cells...
December 7, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29210666/a-newly-synthetized-ferrocenyl-derivative-selectively-induces-apoptosis-in-all-lymphocytes-through-mitochondrial-estrogen-receptors
#4
Marjan Aghvami, Jalal Pourahmad, Afshin Zarghi, Peyman Eshghi, Mohammad Hadi Zarei, Shabnam Farzaneh, Fatemeh Sattari
BACKGROUND: Estrogens, as the main female steroid hormones have multiple proven effects on reproductive and non- reproductive systems. Expression of ERα and ERβ, two dominant estrogen receptors, in peripheral blood mononuclear cells in certain B-cell malignancies and the existence of estrogens receptors on mitochondria is open to question that estrogen likely has an impact on the cancerous lymphocytes life span. Acute lymphoblastic leukemia (ALL) is the frequent pediatric malignity which is recurrent and hardly curable in many cases...
December 5, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29210665/synthesis-and-evaluation-of-a-new-series-of-arylidene-indanones-as-potential-anticancer-agents
#5
Ahmet Ozdemir, Sevtem Gokbulut, Belgin Sever, Gulsen Akalın Ciftci, Mehlika Dilek Altıntop
BACKGROUND: Arylidene indanones have attracted a great deal of interest due to their outstanding therapeutic applications. In particular, considerable research has pointed out the importance of arylidene indanones in the field of cancer research. OBJECTIVE: The aim of the current work was to design and synthesize arylidene indanone-based anticancer agents. METHOD: New arylidene indanones were obtained via the Claisen-Schmidt condensation of 5-chloro-6-methoxy-2,3-dihydro-1H-inden-1-one with p-substituted benzaldehyde derivatives...
December 5, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29189182/design-synthesis-and-cytotoxicity-evaluation-of-new-3-5-disubstituted-2-thioxoimidazolidinones
#6
Khaled Abdellatif, Mostafa M Elbadawi, Mohammed T Elsaady, Amer Ali Abd El-Hafeez, Takashi Fujimura, Seiji Kawamoto, Ahmed I Khodair
Background Some 2-thioxoimidazolidinones have been reported as anti-prostate and anti-breast cancer agents through their inhibitory activity on topoisomerase I that is considered as a potential chemotherapeutic target. Objective A new series of 3,5-disubstituted-2-thioxoimidazolidinone derivatives 10a-f and their S-methyl analogs 11a-f were designed, synthesized and evaluated for cytotoxicity against human prostate cancer cell line (PC-3), human breast cancer cell line (MCF-7) and non-cancerous human lung fibroblast cell line (WI-38)...
November 29, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29189181/good-fashion-is-evolution-not-revolution-methods-to-enhance-existing-anticancer-medicines-primarily-with-use-of-transition-metal
#7
Magdalena Katarzyna Guzowska, Monika Kalinowska, Wlodzimierz Lewandowski
The constant search for a successful cancer therapies lasts for decades. Apart from the huge scientific effort and enormous sum of spent money, only a small amount of newly developed medicines move into clinical use (only 94 registered anticancer drugs in the last 12 years [1]). Anticancer regimes are still overcome by drugs invented over 50 years ago such as cisplatin and doxorubicin. Significant progress in the development of improved anticancer drugs was made due to multiple studies on the relationship between the molecular structure of chemical compounds and their cytostatic activity...
November 29, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29189180/design-synthesis-and-anti-breast-cancer-activity-of-some-novel-substituted-isoxazoles-as-anti-breast-cancer-agent
#8
Santosh N Mokale, Nikhil S Sakle, Swati A Bhavale, Deepak K Lokwani, Vishakha Shelke
A novel series of isoxazole (S21-S30) derivatives were designed, synthesized and screened for their anticancer activity against estrogen receptor-positive MCF-7 and negative MDA-MB-435 breast cancer cell lines. The synthesized derivative has ability to inhibit the growth of the human breast cancer cell line at low concentrations. In-vivo anticancer activity was performed on virgin female sprague dawley rats. The result shows that the compound S23 has more selectivity and marked estrogen modulator activity than the standard tamoxifen...
November 29, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29189179/computational-study-of-the-binding-modes-of-diverse-dpn-analogues-on-estrogen-receptors-er-and-the-biological-evaluation-of-a-new-potential-antiestrogenic-ligand
#9
Marlet Martinez, Benjamin Garcia, Brenda Colin, M Bello, Berenice Prestegui, Alma Chavez, Alfonso Duenas, Jonathan Fragoso, Jessica Mendieta, Edgar Rojano, David Ordaz, Rocio Garcia, D Castillo-Bautista, Jose Correa
Estrogen (17β-estradiol) is essential for normal growth and differentiation in the mammary gland. Previous investigations have revealed that estrogen receptor alpha (ERα) plays a critical role in breast cancer. More recently, observations regarding the widespread expression of ERβ-like proteins in normal and neoplastic mammary tissues have suggested that ERβ is also involved in the mentioned pathology. Design of new drugs both steroidal and nonsteroidal that target any of these receptors represents a promise to treat breast cancer...
November 29, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29173186/comparison-of-physicochemical-properties-of-generic-doxorubicin-hcl-liposome-injection-with-the-reference-listed-drug
#10
Subhas Bhowmick, Kuntal Maiti, Pankaj Jain, Murlidhar Zope, Keyur Doshi, Thennati Rajamannar
BACKGROUND: Liposomal doxorubicin is widely used for treating ovarian cancer and Kaposi's sarcoma. Encapsulation of doxorubicin in highly complex polyethylene glycol-coated (stealth) liposomes prolongs residence time and avoids the systemic toxicity associated with administration of the free drug. Small variations in physicochemical properties introduced during manufacture of liposomes can influence the payload of encapsulated drug, stability of liposomes under physiological conditions, and release of drug at the target tissue...
November 21, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29173185/effects-of-melatonin-in-cancer-potential-mechanisms
#11
Tomris Ozben, Aysegul Hanikoglu, Ertan Kucuksayan, Rana Cagla Akduman
This systematic review aims to elucidate the role of melatonin (N-acetyl-5-metoxy-tryptamine) (MLT) in the prevention and treatment of cancer. MLT is a pineal gland secretory product, an evolutionarily highly conserved molecule; it is also an antioxidant and an impressive protector of mitochondrial bioenergetic activity. MLT is characterized by an ample range of activities, modulating the physiology and molecular biology of the cell. Its physiological functions relate principally to the interaction of G protein-coupled MT1 and MT2 trans-membrane receptors (GPCRs), a family of guanidine triphosphate binding proteins...
November 21, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29173184/natural-compounds-in-the-chemoprevention-of-malignant-melanoma
#12
Corina Danciu, Codruta Soica, Diana Antal, Alexa Ersilia, Roxana Ghiulai, Ioana Pavel, Florina Ardelean, Roxana Babuta, Alexandra Popescu, Cristina Dehelean
Malignant melanoma is a very aggressive form of skin cancer, with increasing rates every year, with an etiology that derives from the transformation and uncontrolled growth of melanocytes. There are several treatment options which can be used as unique treatment or combined, depending upon the stage of melanoma including surgical excision, chemotherapy, immunotherapy, targeted therapy. Plant Kingdom displays an unequalled potential for the synthesis of highly diversified chemical structures. Although natural compounds are synthesized in order to help the plant to interact with the environment, a large number of phytochemicals act as drugs within the human or animal body by activating various biochemical pathways...
November 21, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29173183/a-comparison-of-fucoidan-conjugated-to-paclitaxel-and-curcumin-for-the-dual-delivery-of-cancer-therapeutic-agents
#13
Nam Hoang Phan, Thao Thanh Ly, Minh Nguyet Pham, Thinh Duc Luu, Toi Van Vo, Phuong Ha-Lien Tran, Thao Truong-Dinh Tran
The aim of this study was to develop and compare polymeric micelles of fucoidan, a sulfated polysaccharide, and hydrophobic drugs such as paclitaxel and curcumin. Paclitaxel and curcumin are both known for their medicinal properties, including anticancer efficacy. However, their very low water solubility, absorption and rapid metabolism leads to reduced bioavailability. To redress these problems and enhance anti-cancer therapeutics using fucoidan, polymeric micelles were synthesized from conjugates of fucoidan and hydrophobic drugs...
November 21, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29173187/trichinella-spiralis-and-tumors-cause-coincidence-or-treatment
#14
Chengshui Liao, Xiangchao Cheng, Mingyuan Liu, Xuelin Wang, Pascal Boireau
Conventional therapeutic strategies for tumors have had limited success, and innovative and more effective approaches to treatment are urgently required. The ancient idea that various biological, bacterial, yeast, viral, and parasitic agents can be used as cancer therapeutics has gradually attracted considerable interest. Certain parasites have been widely discussed in association with human and animal tumors. Many researches have provided proofs that Trichinella spiralis (T. spiralis) possesses antitumor activities...
November 20, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29141565/radio-modulatory-potential-ofcaffeic-acid-phenethyl-ester-a-therapeutic-perspective
#15
Km Anjaly, Ashu Tiku
Use of natural agents is an upcoming area of research in cancer biology. Caffeic acid phenethyl ester has received great attention because of its therapeutic potential in various conditions including cancer. It is an active/abundant component of propolis. Propolis is a honey bee hive product produced by bees using their enzyme-rich digestive secretions on resinous mix, bee wax and pollen from plants. It is used to protect the beehive against bacteria and other infections.Although a lot of work has been done on chemotherapeutic aspects of CAPE, its role as a radiomodulator is yet to be delineated...
November 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29141564/a-review-on-the-management-of-small-renal-masses-active-surveillance-versus-surgery
#16
Giancarlo Marra, Marco Oderda, Marco Allasia, Stefania Munegato, Steven Joniau, Paolo Gontero
Despite the rise of small renal tumour (SRMs) diagnosis and related surgeries, death rate of kidney cancer is increasing, suggesting a non-optimal management of SRMs. Active Surveillance (AS) for kidney cancer was introduced to face this paradox. However, incertitude remains on whether and when AS can replace surgery in selected patients. We performed a literature search, reviewed and discussed the evidence in favour of AS or surgery for SRMs. Histopathology and natural history of SRMs, including the percentage of benign tumours amongst SRMs, tumour growth rate, life expectancy of SRMs patients being generally older, and current results of AS series seem to support its use in selected groups...
November 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29141563/ganoderma-lucidum-polysaccharides-as-an-anti-cancer-agent
#17
Didem Sohretoglu, Shile Huang
The mushroom Ganoderma lucidum (G. lucidum) has been used for centuries in Asian countries to treat various diseases and to promote health and longevity. Clinical studies have shown beneficial effects of G. lucidum as an alternative adjuvant therapy in cancer patients without obvious toxicity. G. lucidum polysaccharides (GLP) is the main bioactive component in the water soluble extracts of this mushroom. Evidence from in vitro and in vivo studies has demonstrated that GLP possesses potential anticancer activity through immunomodulatory, anti-proliferative, pro-apoptotic, anti-metastatic and anti-angiogenic effects...
November 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29141562/a-review-of-electroporation-based-antitumor-skin-therapies-and-investigation-of-betulinic-acid-loaded-ointment
#18
Monika Bakonyi, Szilvia Berko, Gabor Eros, Gabor Varju, Cristina Dehelean, Maria Budai Szucs, Erzsebet Csanyi
BACKGROUND: Electrochemotherapy is a novel treatment for cutaneous and subcutaneous tumors utilizing the combination of electroporation and chemotherapeutic agents. Since tumors have an increasing incidence nowadays as a result of environmental and genetic factors, electrochemotherapy could be a promising treatment for cancer patients. OBJECTIVE: The aim of this article is to summarize the novel knowledge about the use of electroporation for antitumor treatments and to present a new application of electrochemotherapy with a well-known plant derived antitumor drug betulinic acid...
November 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29141561/steroidal-anticancer-agents-an-overview-of-estradiol-related-compounds
#19
Renata Minorics, Istvan Zupko
Research of steroidal compounds as anticancer agents started almost 50 years ago. During the past decades several innovative new steroids, like cyproterone, finasteride, estramustin, exemestane and fulvestrant have successfully become part of routine clinical practice. Meanwhile, a vast amount of new information have accumulated about the functions of the endogenous steroid system (including the characterization of enzymes, receptors, transcription pathways, etc.) and about the role of steroids in carcinogenesis...
November 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29141560/growth-kinetics-and-oncologic-outcomes-for-small-renal-masses-managed-with-active-surveillance-a-review-of-the-literature
#20
Benjamin T Ristau, Thomas W Fuller, Ricardo Rios, Cristina Ho, Jeffrey J Tomaszewski
An increasing number of enhancing renal masses are being discovered incidentally on cross-sectional imaging. Many can be characterized as small renal masses (SRMs), the natural history of which is heterogeneous and poorly understood. Active surveillance has been proposed as an initial management strategy for these tumors, particularly in the old and infirmed patient population. Herein, a rigorous review of the literature is provided to explore the incidence and epidemiology of SRMs as well as the growth kinetics and oncologic outcomes of SRMs under observation...
November 13, 2017: Anti-cancer Agents in Medicinal Chemistry
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