keyword
MENU ▼
Read by QxMD icon Read
search

anticancer

keyword
https://www.readbyqxmd.com/read/29342447/design-synthesis-and-anticancer-studies-of-novel-aminobenzazolyl-pyrimidines-as-tyrosine-kinase-inhibitors
#1
Rupesh Chikhale, Sonali Thorat, Rajan Kumar Choudhary, Nikhil Gadewal, Pramod Khedekar
Abnormal signalling from the Protein tyrosine kinases (PTKs) like receptor tyrosine kinases and intracellular tyrosine kinases can lead to diseases such as cancer especially non-small cell lung cancer, chronic myeloid leukaemia and gastrointestinal stromal tumours. Various Protein tyrosine kinase inhibitors are available but face poor bioavailability, severe toxicities and recent cases of drug-resistant cancers prompts for development of better drug molecules. In this study we report the design and development of a novel Protein Tyrosine Kinase (PTK) inhibitor on the basis of pharmacophore modelling...
January 4, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29342415/lysosomes-targeting-imaging-and-anticancer-properties-of-novel-bis-naphthalimide-derivatives
#2
Rui-Xue Rong, Shan-Shan Wang, Xuan Liu, Ren-Feng Li, Ke-Rang Wang, Zhi-Ran Cao, Xiao-Liu Li
A series of novel N,N-bis(3-aminopropyl)methylamine bridged bis-naphthalimide derivatives NI1-NI8 containing saturated nitrogenous heterocycles were designed and synthesized, their cytotoxic activities against Hela, MCF-7, A549 and MGC-803 cells were investigated, Compounds NI1-NI4 modified with piperidine and piperazine exhibited good and selective cytotoxic activity, for instance, compounds NI1 and NI4 showed potent cytotoxic activity against Hela cells and MGC-803 cells with the IC50 values of 2.89, 060, 2...
January 9, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29342353/synthesis-and-computational-studies-demonstrate-the-utility-of-an-intramolecular-styryl-diels-alder-reaction-and-bht-assisted-1-3-shift-to-construct-anticancer-dl-deoxypodophyllotoxin
#3
Diana I Saavedra, Benjamin D Rencher, Doo-Hyun Kwon, Stacey J Smith, Daniel H Ess, Merritt B Andrus
Deoxypodophyllotoxin is a secondary metabolite lignan possessing potent anticancer activity with potential as a precursor for known anticancer drugs, but its use is limited by scarcity from natural sources. We here report the total synthesis of racemic deoxypodophyllotoxin (DPT) in seven steps using an intramolecular styryl Diels-Alder reaction (ISDA) strategy uniquely suited to assemble the deoxypodophyllotoxin core. Computational studies are also reported for this reaction that demonstrate the ability to overcome the limitations of slow reactivity and electronic mismatch of the diene and dieneophile...
January 17, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29342125/induction-of-pro-apoptotic-endoplasmic-reticulum-stress-in-multiple-myeloma-cells-by-neo214-perillyl-alcohol-conjugated-to-rolipram
#4
Thomas C Chen, Nymph Chan, Shirin Labib, Jiali Yu, Hee-Yeon Cho, Florence M Hofman, Axel H Schönthal
Despite the introduction of new therapies for multiple myeloma (MM), many patients are still dying from this disease and novel treatments are urgently needed. We have designed a novel hybrid molecule, called NEO214, that was generated by covalent conjugation of the natural monoterpene perillyl alcohol (POH), an inducer of endoplasmic reticulum (ER) stress, to rolipram (Rp), an inhibitor of phosphodiesterase-4 (PDE4). Its potential anticancer effects were investigated in a panel of MM cell lines. We found that NEO214 effectively killed MM cells in vitro with a potency that was over an order of magnitude stronger than that of its individual components, either alone or in combination...
January 17, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29342104/synthesis-anti-proliferative-activity-evaluation-and-3d-qsar-study-of-naphthoquinone-derivatives-as-potential-anti-colorectal-cancer-agents
#5
Julio Acuña, Jhoan Piermattey, Daneiva Caro, Sven Bannwitz, Luis Barrios, Jairo López, Yanet Ocampo, Ricardo Vivas-Reyes, Fabio Aristizábal, Ricardo Gaitán, Klaus Müller, Luis Franco
Colorectal cancer (CRC) is a disease with high incidence and mortality, constituting the fourth most common cause of death from cancer worldwide. Naphthoquinones are attractive compounds due to their biological and structural properties. In this work, 36 naphthoquinone derivatives were synthesized and their activity evaluated against HT-29 cells. Overall, high to moderate anti-proliferative activity was observed in most members of the series, with 15 compounds classified as active (1.73 < IC50 < 18.11 μM)...
January 17, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29341952/a-pharmacological-review-leptadenia-reticulata-wight-arn-jivanti-the-real-life-giving-plant
#6
Jayesh M Dhalani, Pankaj B Nariya
The present review reveals a comprehensive description of various pharmacological studies carried out on Leptadenia reticulata, a source of several active compounds, i.e. Leptadenia reticulata plant belonging to family Asclepiadaceae, it is also known as 'Jivanti', used for the treatment of various ailments in human civilization as well as used in folk medicine as a remedy in various reported herbal formulations. The plant has been found to exhibit diverse pharmacological activities like antibacterial activity, anticancer activity, lactogenic eff ect, antioxidant activity, anti-implantation activity, anti-asthmatic activity, modulating eff ect, activity of silver nano particles, hepatoprotective activity, antifungal activity, antidiabetic activity and anti-infl ammatory activity...
December 20, 2017: Folia Medica
https://www.readbyqxmd.com/read/29341908/induction-of-au-methotrexate-conjugates-by-sugar-molecules-production-assembly-mechanism-and-bioassay-studies
#7
Wei-Yuan Wang, Xiu-Fen Zhao, Xiao-Han Ju, Ping Liu, Jing Li, Ya-Wen Tang, Shu-Ping Li, Xiao-Dong Li, Fu-Gui Song
Au-methotrexate (Au-MTX) conjugates induced by sugar molecules were produced by a simple, one-pot, hydrothermal growth method. Herein, the Au(III)-MTX complexes were used as the precursors to form Au-MTX conjugates. Addition of different types of sugar molecules with abundant hydroxyl groups resulted in the formation of Au-MTX conjugates featuring distinct characteristics that could be explained by the diverse capping mechanisms of sugar molecules. That is, the instant-capping mechanism of glucose favored the generation of peanut-like Au-MTX conjugates with high colloidal stability while the post-capping mechanism of dextran and sucrose resulted in the production of Au-MTX conjugates featuring excellent near-infrared (NIR) optical properties with a long-wavelength plasmon resonance near 630-760 nm...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341617/enhancing-docetaxel-delivery-to-multidrug-resistant-cancer-cells-with-albumin-coated-nanocrystals
#8
Sheryhan F Gad, Joonyoung Park, Ji Eun Park, Gihan N Fetih, Sozan S Tous, Wooin Lee, Yoon Yeo
Intravenous delivery of poorly water-soluble anticancer drugs such as docetaxel (DTX) is challenging due to the low bioavailability and the toxicity related to solubilizing excipients. Colloidal nanoparticles are used as alternative carriers, but low drug loading capacity and circulation instability limit their clinical translation. To address these challenges, DTX nanocrystals (NCs) were prepared using Pluronic F127 as an intermediate stabilizer and albumin as a functional surface modifier, which were previously found to be effective in producing small and stable NCs...
January 17, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29341608/molecular-dynamics-pinpoint-the-global-fluorine-effect-in-balanoids-binding-to-pkc%C3%AE%C2%B5-and-pka
#9
Ari Hardianto, Fei Liu, Shoba Ranganathan
(-)-Balanol is an ATP mimic that inhibits protein kinase C (PKC) isozymes and cAMP-dependent protein kinase (PKA) with little selectivity. While PKA is known as a tumour promoter, PKC isozymes can be tumour promoters or suppressors. In particular, PKCε is frequently involved in tumorigenesis and a potential target for anticancer drugs. We recently reported that stereospecific fluorination of balanol yielded a balanoid with enhanced selectivity for PKCε over other PKC isozymes and PKA, although the global fluorine effect behind the selectivity enhancement is not fully understood...
January 17, 2018: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29341369/structural-factors-affecting-binding-of-platinum-anticancer-agents-with-phospholipids-influence-of-charge-and-phosphate-clamp-formation
#10
Anil Kumar Gorle, Junyong Zhang, Qin Liu, Susan J Berners-Price, Nicholas P Farrell
We report a detailed NMR and DFT study of the interaction of polynuclear platinum anticancer agents (PPCs) with negatively charged phospholipids as a mechanism for their cellular uptake. The reactions of fully 15N-labelled [{trans-PtCl(NH3)2}2(-trans-Pt(NH3)2{NH2(CH2)6NH2}2)]4+ (15N-1, 1,0,1/t,t,t) and the dinuclear [{trans-PtCl(NH3)2}2{-H2N(CH2)6NH2}]2+ (15N-2, 1,1/t,t) with the sodium salt of 1,2-dihexanoyl-sn-glycero-3-phosphate (DHPA) were studied at 298 K, pH ~5.4, by [1H,15N] HSQC 2D NMR spectroscopy...
January 17, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29341267/cross-linking-of-thiolated-paclitaxel-oligo-p-phenylene-vinylene-conjugates-aggregates-inside-tumor-cells-leads-to-chemical-locks-that-increase-drug-efficacy
#11
Lingyun Zhou, Fengting Lv, Libing Liu, Guizhi Shen, Xuehai Yan, Guillermo C Bazan, Shu Wang
How to reduce the resistance of certain tumor cells to paclitaxel (PTX) and related taxoid anticancer drugs is a major challenge for improving cure rates. An oligo(p-phenylenevinylene) unit with thiol groups and a PTX unit (OPV-S-PTX), which enhances drug efficacy and reverses resistance is thus designed. The mechanism involves diffusion of OPV-S-PTX into the cell, where π-π interactions lead to aggregation. Cross-linking of the aggregates via oxidation of thiol groups is favored in tumor cells because of the higher reactive oxygen species (ROS) concentration...
January 17, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29341223/disulfide-bond-based-polymeric-drug-carriers-for-cancer-chemotherapy-and-relevant-redox-environments-in-mammals
#12
REVIEW
Pei Zhang, Jilian Wu, Fengmei Xiao, Dujuan Zhao, Yuxia Luan
Increasing numbers of disulfide linkage-employing polymeric drug carriers that utilize the reversible peculiarity of this unique covalent bond have been reported. The reduction-sensitive disulfide bond is usually employed as a linkage between hydrophilic and hydrophobic polymers, polymers and drugs, or as cross-linkers in polymeric drug carriers. These polymeric drug carriers are designed to exploit the significant redox potential difference between the reducing intracellular environments and relatively oxidizing extracellular spaces...
January 17, 2018: Medicinal Research Reviews
https://www.readbyqxmd.com/read/29340404/a-highly-efficient-nucleophilic-substitution-reaction-between-r2p-o-h-and-triarylmethanols-to-synthesize-phosphorus-substituted-triarylmethanes
#13
Long Chen, Xin-Yue Fang, Yun-Xiang Zou
A highly efficient and general nucleophilic substitution reaction between dialkyl H-phosphonates or diarylphosphine oxides and triarylmethanols catalyzed by HOTf (trifluoromethanesulfonic acid) has been developed. It provides an atom-economical protocol for the synthesis of various symmetrical and unsymmetrical phosphorus-substituted triarylmethanes that constitute an emerging family of potent anticancer agents in rich diversity with 40 to 96% yields. The synthetic applicability of this protocol is demonstrated by gram-scale preparations...
January 17, 2018: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29340097/s-adenosyl-methionine-sam-alters-the-transcriptome-and-methylome-and-specifically-blocks-growth-and-invasiveness-of-liver-cancer-cells
#14
Yan Wang, ZhongSheng Sun, Moshe Szyf
S-adenosyl methionine (SAM) is a ubiquitous methyl donor that was reported to have chemo- protective activity against liver cancer, however the molecular footprint of SAM is unknown. We show here that SAM selectively inhibits growth, transformation and invasiveness of hepatocellular carcinoma cell lines but not normal primary liver cells. Analysis of the transcriptome of SAM treated and untreated liver cancer cell lines HepG2 and SKhep1 and primary liver cells reveals pathways involved in cancer and metastasis that are upregulated in cancer cells and are downregulated by SAM...
December 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29340073/ym155-exerts-potent-cytotoxic-activity-against-quiescent-g0-g1-multiple-myeloma-and-bortezomib-resistant-cells-via-inhibition-of-survivin-and-mcl-1
#15
Miyuki Ookura, Tatsuya Fujii, Hideki Yagi, Takuya Ogawa, Shinji Kishi, Naoko Hosono, Hiroko Shigemi, Takahiro Yamauchi, Takanori Ueda, Akira Yoshida
YM155, a novel small molecule inhibitor of survivin, shows broad anticancer activity. Here, we have focused on the cytotoxic activity of YM155 against multiple myeloma (MM) including cytokinetically quiescent (G0/G1) cells and bortezomib resistant cells. YM155 strongly inhibited the growth of MM cell lines with the IC50 value of below 10 nM. YM155 also showed potent anti-myeloma activity in mouse xenograft model. YM155 suppressed the expression of survivin and rapidly directed Mcl-1 protein for proteasome degradation...
December 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29340056/temozolomide-encapsulated-and-folic-acid-decorated-chitosan-nanoparticles-for-lung-tumor-targeting-improving-therapeutic-efficacy-both-in-vitro-and-in-vivo
#16
Kaidi Li, Naixin Liang, Huaxia Yang, Hongsheng Liu, Shanqing Li
Folic acid-conjugated temozolomide (TMZ)-loaded chitosan nanoparticles (CS-TMZ-FLA-NP) were developed to target lung cancer in the anticipation that folic acid would increase the affinity of nanoparticles for cancer cells. CS-TMZ-FLA-NP showed the highest anti-proliferative effect on the lung cancer cells in comparison to free TMZ and CS-TMZ-NP (nanoparticles without folic acid). A cellular uptake assay was performed on two different cell lines, L132 and A549. Cellular uptake efficiencies of CS-TMZ-NP and CS-TMZ-FLA-NP were found to be concentration-dependent in both cell lines...
December 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29340020/eya2-promotes-lung-cancer-cell-proliferation-by-downregulating-the-expression-of-pten
#17
Zhaoming Li, Ran Qiu, Xia Qiu, Tian Tian
Lung cancer is the leading cause of cancer-related death worldwide. Despite advances have been made in diagnosis and therapeutic strategies, the prognosis of lung cancer is still very poor. Eyes absent transcriptional cofactor EYA2 has been shown to promote lung cancer cell growth, however, the underlying molecular mechanism is still not fully understood. In the present study, we found that EYA2 was up-regulated in lung cancer, and EYA2 led to increased cell proliferation by inhibiting Phosphatase and tensin homologue (PTEN) expression via modulation of miR-93...
December 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29339720/plumbagin-inhibits-the-proliferation-and-survival-of-esophageal-cancer-cells-by-blocking-stat3-plk1-akt-signaling
#18
Ying-Ya Cao, Jing Yu, Ting-Ting Liu, Kai-Xia Yang, Li-Yan Yang, Qun Chen, Feng Shi, Jia-Jie Hao, Yan Cai, Ming-Rong Wang, Wei-Hua Lu, Yu Zhang
Esophageal squamous cell carcinoma (ESCC) is one of the deadliest cancers, and it requires novel treatment approaches and effective drugs. In the present study, we found that treatment with plumbagin, a natural compound, reduced proliferation and survival of the KYSE150 and KYSE450 ESCC cell lines in a dose-dependent manner in vitro. The drug also effectively inhibited the viability of primary ESCC cells from fresh biopsy specimens. Furthermore, plumbagin-induced mitotic arrest and massive apoptosis in ESCC cells...
January 16, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29339544/role-of-chromatin-damage-and-chromatin-trapping-of-fact-in-mediating-the-anticancer-cytotoxicity-of-dna-binding-small-molecule-drugs
#19
Elimelech Nesher, Alfiya Safina, Ieman Aljahdali, Scott Portwood, Eunice S Wang, Igor Koman, Jianmin Wang, Katerina V Gurova
Precisely how DNA-targeting chemotherapeutic drugs trigger cancer cell death remains unclear, as it is difficult to separate direct DNA damage from chromatin damage in cells. Recent work on curaxins, a class of small molecule drugs with broad anticancer activity, show that they interfere with histone-DNA interactions and destabilize nucleosomes without binding DNA or causing detectable DNA damage. Chromatin unfolding caused by curaxins is sensed by the histone chaperone FACT, which binds unfolded nucleosomes and causes chromatin trapping (c-trapping)...
January 16, 2018: Cancer Research
https://www.readbyqxmd.com/read/29339282/probing-the-interaction-of-two-chemotherapeutic-drugs-of-oxali-palladium-and-5-fluorouracil-simultaneously-with-milk-carrier-protein-of-%C3%AE-lactoglobulin
#20
Amineh Leilabadi-Asl, Adeleh Divsalar, Ali Akbar Saboury, Kazem Parivar
β-Lactoglobulin (βLG) is a basic element of globular carrier protein, which is the major protein in the whey of ruminant milk and is of main interest in the dairy industry. In the present study, the simultaneous effects of both of the important anticancer drugs of 5-fluorouracil (5-FU) and oxali-palladium, on the structure of βLG were investigated using different spectroscopic methods of fluorescence and circular dichroism (CD) in combination with a molecular docking at two temperatures of 25 and 37 °C...
January 12, 2018: International Journal of Biological Macromolecules
keyword
keyword
96154
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"