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Articles 901 - 930 of 1021
Full-Text Articles in Chemicals and Drugs
Transfusion Of Cxcr4-Primed Endothelial Progenitor Cells Reduces Cerebral Ischemic Damage And Promotes Repair In Db/Db Diabetic Mice, Ji Chen, Jianying Chen, Shuzhen Chen, Cheng Zhang, Liangqing Zhang, Xiang Xiao, Avik Das, Yuhui Zhao, Bin Yuan, Mariana Morris, Bin Zhao, Yanfang Chen
Transfusion Of Cxcr4-Primed Endothelial Progenitor Cells Reduces Cerebral Ischemic Damage And Promotes Repair In Db/Db Diabetic Mice, Ji Chen, Jianying Chen, Shuzhen Chen, Cheng Zhang, Liangqing Zhang, Xiang Xiao, Avik Das, Yuhui Zhao, Bin Yuan, Mariana Morris, Bin Zhao, Yanfang Chen
Pharmacology and Toxicology Faculty Publications
This study investigated the role of stromal cell-derived factor-1α (SDF-1α)/CXC chemokine receptor 4 (CXCR4) axis in brain and endothelial progenitor cells (EPCs), and explored the efficacy of CXCR4 primed EPCs in treating ischemic stroke in diabetes. The db/db diabetic and db/+ mice were used in this study. Levels of plasma SDF-1α and circulating CD34+CXCR4+ cells were measured. Brain SDF-1α and CXCR4 expression were quantified at basal and after middle cerebral artery occlusion (MCAO). In in vitro study, EPCs were transfected with adenovirus carrying null (Ad-null) or CXCR4 (Ad-CXCR4) followed with high glucose (HG) treatment for 4 days. For pathway block …
The Effects Of Supplemental Fish Oil On Blood Pressure And Morning Cortisol In Normotensive Adults: A Pilot Study, Eric E. Noreen, Josef Brandauer
The Effects Of Supplemental Fish Oil On Blood Pressure And Morning Cortisol In Normotensive Adults: A Pilot Study, Eric E. Noreen, Josef Brandauer
Health Sciences Faculty Publications
Purpose: To determine the effects of 6wk of supplementation with fish oil (FO) on blood pressure and the morning salivary cortisol concentration in normotensive adults.
Methods: Testing was performed following an overnight fast. Subjects (n=40; 35+/-13y, mean+/-SD) rested supine for 40 min, at which time blood pressure and heart rate were measured. Saliva was collected and analyzed for cortisol. Subjects were then randomly assigned to either: 4g/d of Safflower Oil (SO); pr 4g/d of FO supplying 1,600mg/d eicosapentaenoic acid and 800mg/d docosahexaenoic acid. Testing was repeated following 6wk treatment.
Results: Compared to SO, there was a significant decrease …
Situation Analysis Of Child Labour In Karachi, Pakistan: A Qualitative Study, Asaad Ahmed Nafees, Kausar S. Khan, Zafar Fatmi, Mubashir Aslam
Situation Analysis Of Child Labour In Karachi, Pakistan: A Qualitative Study, Asaad Ahmed Nafees, Kausar S. Khan, Zafar Fatmi, Mubashir Aslam
Community Health Sciences
In Karachi, large employment opportunities, burgeoning population and the availability of cheap labour might be the contributing factors for the increasing prevalence of child labour. A literature review was conducted in 2007 that included published and unpublished literature since 2000. Various organizations working in the field were also covered, while the perception of the child labourers was covered through three focus group discussions. Common health issues among the child labourers in Karachi included respiratory illnesses, fever and generalised pains, as well as drug and sexual abuse. Organisations working for child labour could be broadly categorised into those working for legal …
Pediatric Pharmacogenomics: A Systematic Assessment Of Ontogeny And Genetic Variation To Guide The Design Of Statin Studies In Children., Jonathan B. Wagner, J Steven Leeder
Pediatric Pharmacogenomics: A Systematic Assessment Of Ontogeny And Genetic Variation To Guide The Design Of Statin Studies In Children., Jonathan B. Wagner, J Steven Leeder
Manuscripts, Articles, Book Chapters and Other Papers
The dose-exposure-response relationship for drugs may differ in pediatric patients compared with adults. Many clinical studies have established drug dose-exposure relationships across the pediatric age spectrum; however, genetic variation was seldom included. This article applies a systematic approach to determine the relative contribution of development and genetic variation on drug disposition and response using HMG-CoA reductase inhibitors as a model. Application of the approach drives the collection of information relevant to understanding the potential contribution of ontogeny and genetic variation to statin dose-exposure-response in children, and identifies important knowledge deficits to be addressed through the design of future studies.
Prolonged Intermediate Syndrome Pue To Prganophosphate Poisoning, Nadeem Ullah Khan, Muhammad Junaid Patel, M. N.M. Hifath, Saima Kamal, Syed Ather Hussain
Prolonged Intermediate Syndrome Pue To Prganophosphate Poisoning, Nadeem Ullah Khan, Muhammad Junaid Patel, M. N.M. Hifath, Saima Kamal, Syed Ather Hussain
Department of Emergency Medicine
Organophosphate poisoning can present as acute cholinergic syndrome, Intermediate syndrome and delayed neuropathy. Intermediate syndrome secondary to organophosphate poisoning is a serious health problem leading to increased morbidity and mortality. The incidence of problem varies and range from 8%-84% of organophosphate poisoning cases. The factors account for this difference is nature of organophosphate compound, severity of poisoning and inadequate Oxime therapy. The recognition of this syndrome is important as organophosphate poisoning is common in our country. We presented this case of organophosphate poisoning leading to prolonged intermediate syndrome. The muscle weakness associated with this syndrome generally resolves in 5-18 days …
The Effect Of Pre-Operative Coumadin Therapy On Patients Who Develop Hemorrhagic Events Post Bariatric Surgery, Richard Boorse Md, Peter J. Bechtel Md, Cathleen Webber Rn, Mshs, Suzanne L. Smith Mba, Rrt, Tas, Cathy Fuhrman Rn, Msn
The Effect Of Pre-Operative Coumadin Therapy On Patients Who Develop Hemorrhagic Events Post Bariatric Surgery, Richard Boorse Md, Peter J. Bechtel Md, Cathleen Webber Rn, Mshs, Suzanne L. Smith Mba, Rrt, Tas, Cathy Fuhrman Rn, Msn
Department of Surgery
No abstract provided.
Under The Gun: Ongoing Assaults On Bahrain’S Health System, Richard Sollom, Holly G. Atkinson
Under The Gun: Ongoing Assaults On Bahrain’S Health System, Richard Sollom, Holly G. Atkinson
Publications and Research
In February 2011, the Government of Bahrain began targeting health professionals who treated protesters. In April 2012, PHR's Richard Sollom, Deputy Director, and Holly Atkinson, MD, FACP, past President of PHR's Board and volunteer expert, authored a report showing the devastation on Bahrain's health system that have resulted from the Government of Bahrain’s continued assault on doctors, patients, and the healthcare system.
Environmental Friendly Synthesis, Characterization Of Surface Modifiable Starch Encapsulated Gold Nanoparticles With Bactericidal And Catalytic Activity, Dillon Pender
Mahurin Honors College Capstone Experience/Thesis Projects
In the present study, we report the green synthesis of gold nanoparticles (GNPs), using potato starch as a reducing as well as a stabilizing agent in an aqueous buffer medium. The resulting starch-GNPs (St-GNPs) were near spherical in shape with an average diameter of 15 ± 5 nm. In this approach, St-GNPs were characterized and investigated for their antibacterial properties against both gram negative (Escherichia coli) and gram positive (Staphylococcus epidermidis) bacteria. These St-GNPs were found to possess significant dose dependent antibacterial activity against bacteria. Also, St-GNPs showed a significant catalytic activity and can easily be …
Genetic Ablation Of Cav1 Differentially Affects Melanoma Tumor Growth And Metastasis In Mice: Role Of Cav1 In Shh Heterotypic Signaling And Transendothelial Migration., Franco Capozza, Casey Trimmer, Remedios Castello-Cros, Sanjay Katiyar, Diana Whitaker-Menezes, Antonia Follenzi, Marco Crosariol, Gemma Llaverias, Federica Sotgia, Richard G Pestell, Michael P Lisanti
Genetic Ablation Of Cav1 Differentially Affects Melanoma Tumor Growth And Metastasis In Mice: Role Of Cav1 In Shh Heterotypic Signaling And Transendothelial Migration., Franco Capozza, Casey Trimmer, Remedios Castello-Cros, Sanjay Katiyar, Diana Whitaker-Menezes, Antonia Follenzi, Marco Crosariol, Gemma Llaverias, Federica Sotgia, Richard G Pestell, Michael P Lisanti
Department of Cancer Biology Faculty Papers
Both cell-autonomous and non-cell-autonomous factors contribute to tumor growth and metastasis of melanoma. The function of caveolin-1 (Cav1), a multifunctional scaffold protein known to modulate several biologic processes in both normal tissue and cancer, has been recently investigated in melanoma cancer cells, but its role in the melanoma microenvironment remains largely unexplored. Here, we show that orthotopic implantation of B16F10 melanoma cells in the skin of Cav1KO mice increases tumor growth, and co-injection of Cav1-deficient dermal fibroblasts with melanoma cells is sufficient to recapitulate the tumor phenotype observed in Cav1KO mice. Using indirect coculture experiments with fibroblasts and melanoma cells …
Chemosensitization Of Hepatocellular Carcinoma To Gemcitabine By Non-Invasive Radiofrequency Field-Induced Hyperthermia, Mustafa Raoof
Chemosensitization Of Hepatocellular Carcinoma To Gemcitabine By Non-Invasive Radiofrequency Field-Induced Hyperthermia, Mustafa Raoof
Dissertations and Theses (Open Access)
Gemcitabine is a potent nucleoside analogue against solid tumors however drug resistance rapidly emerges. Removal of gemcitabine incorporated in the DNA by repair mechanisms could potentially contribute to resistance in chemo-refractory solid tumors. In this study, we evaluated homologous recombination repair of gemcitabine-stalled replication forks as a potential mechanism contributing to resistance. We also studied the effect of hyperthermia on homologous recombination pathway to explain the previously reported synergy between gemcitabine and hyperthermia. We found that hyperthermia degrades and inhibits localization of Mre11 to gemcitabine-stalled replication forks. Furthermore, gemcitabine-treated cells that were also treated with hyperthermia demonstrate a prolonged passage …
Pharmacokinetic/Pharmacodynamic (Pk/Pd) Modeling Of Anti-Neoplastic Agents, Daniel Lexcen, Ahmed H. Salem, Walid F. Elkhatib, Virginia Haynes, Ayman Noreddin
Pharmacokinetic/Pharmacodynamic (Pk/Pd) Modeling Of Anti-Neoplastic Agents, Daniel Lexcen, Ahmed H. Salem, Walid F. Elkhatib, Virginia Haynes, Ayman Noreddin
Pharmacy Faculty Books and Book Chapters
"Development of tumor resistance to chemotherapeutics is related to inherent tumor variations regarding sensitivity to chemotherapeutics and to sub-optimal dosing regimens, including variation in patient pharmacokinetics that result in suboptimal exposure of tumor cells to anti-neoplastic drugs [1, 2]. The rate and extent of drug efficacy depends on the extent of drug exposure at the tumor site and the time above the effective concentration [3]. In vitro models that incorporate these pharmacokinetic and pharmacodynamic (PK/PD) principles to optimize therapeutic response may be considered the method of choice for optimizing dosing schedules before translating data from static assays to animals and …
Inhibition Of Adhesion And Invasion Of Pseudomonas Aeruginosa To Lung Epithelial Cells: A Model Of Cystic Fibrosis Infection, Ayman Noreddin, Ghada Sawy, Walid Elkhatib, Ehab Noreddin, Atef Shibl
Inhibition Of Adhesion And Invasion Of Pseudomonas Aeruginosa To Lung Epithelial Cells: A Model Of Cystic Fibrosis Infection, Ayman Noreddin, Ghada Sawy, Walid Elkhatib, Ehab Noreddin, Atef Shibl
Pharmacy Faculty Books and Book Chapters
"Over their life time, CF patients experience multiple infections by various pneumoniacausing bacteria [6]. With more patients surviving to adulthood, chronic infections with Pseudomonas aeruginosa are coming to the forefront as a leading cause of death [7]. Problems presented by infected CF lung are multi-dimensional; the electrolyte balance and pH of the fluids are abnormal. The mucus is thick and of an alternative composition compared to normal lung and may contribute to colonization with Pseudomonas aeruginosa [2, 3, 5]. As such, research is multi-pronged and includes gene therapy to correct the defective protein, amelioration of inflammatory response and thinning of …
Retrospective Comparison Of The Incidence Of Acute Kidney Injury In Patients Treated With Intravenous Polymyxin B Or Intravenous Colistimethate Sodium, Rebecca A. Sumner Pharmd, Jarrod W. Kile Rph, Bcps
Retrospective Comparison Of The Incidence Of Acute Kidney Injury In Patients Treated With Intravenous Polymyxin B Or Intravenous Colistimethate Sodium, Rebecca A. Sumner Pharmd, Jarrod W. Kile Rph, Bcps
Department of Pharmacy
No abstract provided.
Retrospective Evaluation Of Admissions For Chemotherapy-Inducednausea, Vomiting, And Dehydration, Katelin Van Leer Pharmad, Janine Barnaby Rph, Bcop
Retrospective Evaluation Of Admissions For Chemotherapy-Inducednausea, Vomiting, And Dehydration, Katelin Van Leer Pharmad, Janine Barnaby Rph, Bcop
Department of Pharmacy
No abstract provided.
Bone Health Management In Prostate Cancer Patients Receiving Androgen Deprivation Therapy, Vishnuprabha Dhanapal, David J. Reeves
Bone Health Management In Prostate Cancer Patients Receiving Androgen Deprivation Therapy, Vishnuprabha Dhanapal, David J. Reeves
Scholarship and Professional Work – COPHS
Purpose. Patients receiving androgen deprivation therapy undergo a rapid decline in bone mineral density during the first 6 to 12 months of initiating therapy. The World Health Organization has developed and implemented the Fracture Risk Assessment Tool (FRAX) to predict the ten year risk of a major fracture & hip fracture. Additionally, the National Comprehensive Cancer Network and the National Osteoporosis Foundation have developed osteoporosis guidelines. This study aims to characterize the fracture risk (based on the FRAX tool) and the current management of bone health based on national guidelines compliance.
Methods. A retrospective chart review of patients receiving a …
Effective Non-Viral Delivery Of Sirna To Acute Myeloid Leukemia Cells With Lipid-Substituted Polyethylenimines, Breanne Landry
Effective Non-Viral Delivery Of Sirna To Acute Myeloid Leukemia Cells With Lipid-Substituted Polyethylenimines, Breanne Landry
Pharmacy Faculty Articles and Research
Use of small interfering RNA (siRNA) is a promising approach for AML treatment as the siRNA molecule can be designed to specifically target proteins that contribute to aberrant cell proliferation in this disease. However, a clinical-relevant means of delivering siRNA molecules must be developed, as the cellular delivery of siRNA is problematic. Here, we report amphiphilic carriers combining a cationic polymer (2 kDa polyethyleneimine, PEI2) with lipophilic moieties to facilitate intracellular delivery of siRNA to AML cell lines. Complete binding of siRNA by the designed carriers was achieved at a polymer:siRNA ratio of ~0.5 and led to siRNA/polymer complexes of …
Does The Use Of Intravenous Zoledronic Acid, In Combination With Chemotherapy Regimens, Arrest The Development And Spread Of Cancer Cells To Increase Disease-Free Survival In Breast Cancer Patients?, Dara Colasurdo
PCOM Physician Assistant Studies Student Scholarship
OBJECTIVE: The objective of this selective EBM review is to determine whether or not “Does the use of intravenous zoledronic acid, in combination with chemotherapy regimens, arrest the development and spread of cancer cells to increase disease-free survival in breast cancer patients.“
STUDY DESIGN: Review of three English language primary randomized controlled trials published between 2009 and 2010.
DATA SOURCES: Randomized controlled trials and open label, randomized, phase 2 trial comparing the use of zoledronic acid in combination with chemotherapy to the use of chemotherapy alone were found using Medline/PubMed and Cochrane Databases
OUTCOMES MEASURED: The outcomes measured were incidence …
Is Intravenous Ramosetron 0.3 Mg Effective In The Prevention Of Postoperative Nausea And Vomiting In Women Undergoing Gynecologic Surgery?, Keith S. Elsner
Is Intravenous Ramosetron 0.3 Mg Effective In The Prevention Of Postoperative Nausea And Vomiting In Women Undergoing Gynecologic Surgery?, Keith S. Elsner
PCOM Physician Assistant Studies Student Scholarship
OBJECTIVE: The objective of this selective EBM review is to determine whether or not intravenous ramosetron 0.3 mg is effective in the prevention of postoperative nausea and vomiting (PONV) in women undergoing gynecologic surgery.
STUDY DESIGN: Review of three English language primary research articles published later than 1995.
DATA SOURCES: Randomized, double-blinded, controlled clinical trials comparing intravenous ramosetron to placebo or other control groups were identified using Ovid MEDLINE and Cochrane Library databases.
OUTCOMES MEASURED: Measured outcomes include a complete response to the intervention within the first 24-48 hours, the incidence of postoperative nausea and vomiting, need for rescue antiemetic, …
Is Aspirin Effective In Helping To Prevent Breast Cancer In Women Ages 45 Years And Older?, Kristen M. Quartuccio
Is Aspirin Effective In Helping To Prevent Breast Cancer In Women Ages 45 Years And Older?, Kristen M. Quartuccio
PCOM Physician Assistant Studies Student Scholarship
OBJECTIVE: The objective of this selective EBM review is to determine whether or not aspirin is effective in helping to prevent breast cancer in women ages 45 years and older.
STUDY DESIGN: Review of three English language primary studies published in 2005, 2007, and 2008
DATA SOURCES: Two randomized, double blind, placebo controlled clinical trials and one prospective, population based cohort study comparing aspirin to placebo were found using PubMed and Cochrane databases.
OUTCOMES MEASURED: Breast cancer development was measured in several ways. Tumor characteristics were measured at diagnosis, including size, metastasis to lymph nodes, histology of the mass, histology …
Is The Use Of Apixaban Or Enoxaparin, More Effective In The Prophylaxis Of Venous Thromboembolism Post-Orthopedic Surgery?, Jolene Bohensky
Is The Use Of Apixaban Or Enoxaparin, More Effective In The Prophylaxis Of Venous Thromboembolism Post-Orthopedic Surgery?, Jolene Bohensky
PCOM Physician Assistant Studies Student Scholarship
OBJECTIVE: The objective of this selective EBM review is to determine whether or not the use of Apixaban or Enoxaparin is more effective in the prophylaxis of venous thromboembolism post-orthopedic surgery.
STUDY DESIGN: Review of three English language randomized, double-blind, placebo-controlled clinical trials from 2009-2010.
DATA SOURCES: Randomized, double-blind placebo controlled, clinical trials comparing the effectiveness of Apixaban and Enoxaparin in the prophylaxis of Venous Thromboembolism (VTE) post-orthopedic surgery were found using PubMed, the Cochrane Database of Randomized Controlled Trials, and the Cochrane Databases of Systematic Reviews.
OUTCOMES MEASURED: Development of venous thromboembolism (VTE) post-orthopedic surgery including Total …
Severe Lamotrigine Neurotoxicity Treated With Intralipid Emulsion Therapy, Philip W. Moore Do, Megan C. Urquhart Do, Dale L. Mcmillion Do, Keith K. Burkhart Md, Louis R. Cantilena Jr, Md, J Ward Donovan Md
Severe Lamotrigine Neurotoxicity Treated With Intralipid Emulsion Therapy, Philip W. Moore Do, Megan C. Urquhart Do, Dale L. Mcmillion Do, Keith K. Burkhart Md, Louis R. Cantilena Jr, Md, J Ward Donovan Md
Department of Emergency Medicine
No abstract provided.
An Evaluation Of Warfarin Use And 30-Day Hemorrhage In Bariatric Surgery, Amanda M. Curry, Richard Boorse Md, Peter J. Bechtel Md, Cathy Fuhrman Rn, Msn, Cathleen Webber Rn, Mshs, Suzanne L. Smith Mba, Rrt, Tas
An Evaluation Of Warfarin Use And 30-Day Hemorrhage In Bariatric Surgery, Amanda M. Curry, Richard Boorse Md, Peter J. Bechtel Md, Cathy Fuhrman Rn, Msn, Cathleen Webber Rn, Mshs, Suzanne L. Smith Mba, Rrt, Tas
Department of Surgery
No abstract provided.
Post Gastric Bypass Hypoglycemia: Four Cases Treated Successfully With Alphaglucosidase Inhibitor Therapy, Shavon S. Frankhouser Do, Aakif N. Ahmad Do, Gretchen A. Perilli Md, Benjamin J. Quintana Md, Marc A. Vengrove Do, Facp
Post Gastric Bypass Hypoglycemia: Four Cases Treated Successfully With Alphaglucosidase Inhibitor Therapy, Shavon S. Frankhouser Do, Aakif N. Ahmad Do, Gretchen A. Perilli Md, Benjamin J. Quintana Md, Marc A. Vengrove Do, Facp
Department of Medicine
No abstract provided.
Tlr4 Mutation Reduces Microglial Activation, Increases Aβ Deposits And Exacerbates Cognitive Deficits In A Mouse Model Of Alzheimer's Disease, Min Song, Jingji Jin, Jinghong Kou, Abhinandan Pattanayak, Jamaal Rehman, Hong-Duck Kim, Ken-Ichiro Fukuchi
Tlr4 Mutation Reduces Microglial Activation, Increases Aβ Deposits And Exacerbates Cognitive Deficits In A Mouse Model Of Alzheimer's Disease, Min Song, Jingji Jin, Jinghong Kou, Abhinandan Pattanayak, Jamaal Rehman, Hong-Duck Kim, Ken-Ichiro Fukuchi
NYMC Faculty Publications
BACKGROUND: Amyloid plaques, a pathological hallmark of Alzheimer's disease (AD), are accompanied by activated microglia. The role of activated microglia in the pathogenesis of AD remains controversial: either clearing Aβ deposits by phagocytosis or releasing proinflammatory cytokines and cytotoxic substances. Microglia can be activated via toll-like receptors (TLRs), a class of pattern-recognition receptors in the innate immune system. We previously demonstrated that an AD mouse model homozygous for a loss-of-function mutation of TLR4 had increases in Aβ deposits and buffer-soluble Aβ in the brain as compared with a TLR4 wild-type AD mouse model at 14-16 months of age. However, it …
Relationship Of Vitamin D Levels To Blood Pressure In A Biethnic Cohort, Rosario O. Sakamoto
Relationship Of Vitamin D Levels To Blood Pressure In A Biethnic Cohort, Rosario O. Sakamoto
Loma Linda University Electronic Theses, Dissertations & Projects
Background: Serum hydroxyvitamin D [25(OH)D] has been well-accepted as not an ordinary vitamin but a pro-hormone that has many benefits beyond its well-known effects on bone. Cardiovascular risk factors such as hypertension remain a huge health burden and Blacks have been recognized to have higher prevalence of hypertension compared to non-Hispanic Whites. Despite increasing evidence of the benefits of vitamin D on blood pressure control, there is much more to be learned about the relationship of serum 25(OH)D to blood pressure among different ethnicities.
Purpose: The goal of this study was to determine whether vitamin D serum 25(OH)D levels were …
Self-Reported Exercise And Risk Of Osteoporosis In Prostate Cancer Patients Receiving Androgen Deprivation Therapy, Lori J. Mennen-Winchell
Self-Reported Exercise And Risk Of Osteoporosis In Prostate Cancer Patients Receiving Androgen Deprivation Therapy, Lori J. Mennen-Winchell
Loma Linda University Electronic Theses, Dissertations & Projects
Prostate cancer is stimulated to grow in response to testosterone. Androgen deprivation therapy (ADT) leads to chemical castration and suppression of prostate cancer cell production. Testosterone levels less then 300ng/ml decreases bone mineral density and could result in osteoporosis. Studies have shown that during the first year of ADT, fracture risk, mainly in hips and spine increases about 50%. In men, 40% of hip fractures result in death. Exercise may reduce the risk of osteoporosis and thus contribute to the prevention of hip and other fractures. There is limited data regarding whether exercise is associated with a reduced risk of …
Serum 25-Hydroxyvitamin D Level And Acute-Phase Reaction Following Initial Intravenous Bisphosphonate., Tarak Srivastava, Hongying Dai, Connie J. Haney, Uri S. Alon
Serum 25-Hydroxyvitamin D Level And Acute-Phase Reaction Following Initial Intravenous Bisphosphonate., Tarak Srivastava, Hongying Dai, Connie J. Haney, Uri S. Alon
Manuscripts, Articles, Book Chapters and Other Papers
No abstract provided.
3-Substitued Indoles: One Pot Synthesis And Evaluation Of Anticancer And Src Kinase Inhibitory Activities, V. Kameshwara Rao, Bhupender S. Chhikara, Amir Nasrolahi Shirazi, Rakesh Tiwari, Keykavous Parang, Anil Kumar
3-Substitued Indoles: One Pot Synthesis And Evaluation Of Anticancer And Src Kinase Inhibitory Activities, V. Kameshwara Rao, Bhupender S. Chhikara, Amir Nasrolahi Shirazi, Rakesh Tiwari, Keykavous Parang, Anil Kumar
Pharmacy Faculty Articles and Research
An efficient and economical method was developed for the synthesis of 3-substituted indoles by one pot three-component coupling reaction of a substituted or unsubstituted benzaldehyde, N-methylaniline, and indole or N-methylindole using Yb(OTf)3-SiO2 as a catalyst. All the synthesized compounds were evaluated for inhibition of cell proliferation of human colon carcinoma (HT-29), human ovarian adenocarcinoma (SK-OV-3), and c-Src kinase activity. The 4-methylphenyl (4o and 4p) and 4-methoxyphenyl (4q) indole derivatives inhibited the cell proliferation of SK-OV-3 and HT-29 cells by 7077% at a concentration of 50 μM. The unsubstituted phenyl (4d) and 3-nitrophenyl (4l) derivatives showed the inhibition of c-Src kinase …
Thiazolyl N-Benzyl-Substituted Acetamide Derivatives: Synthesis, Src Kinase Inhibitory And Anticancer Activities, Asal Fallah-Tafti, Alireza Foroumadi, Rakesh Tiwari, Amir Nasrolahi Shirazi, David G. Hangauer, Yahao Bu, Tahmineh Akbarzadeh, Keykavous Parang, Abbas Shafiee
Thiazolyl N-Benzyl-Substituted Acetamide Derivatives: Synthesis, Src Kinase Inhibitory And Anticancer Activities, Asal Fallah-Tafti, Alireza Foroumadi, Rakesh Tiwari, Amir Nasrolahi Shirazi, David G. Hangauer, Yahao Bu, Tahmineh Akbarzadeh, Keykavous Parang, Abbas Shafiee
Pharmacy Faculty Articles and Research
KX2-391 (KX-01/Kinex Pharmaceuticals), N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide, is a highly selective Src substrate binding site inhibitor. To understand better the role of pyridine ring and N-benzylsubstitution in KX2-391 and establish the structure-activity relationship, a number of N-benzyl substituted (2-morpholinoethoxy)phenyl)thiazol-4-yl)acetamide derivatives containing thiazole instead of pyridine were synthesized and evaluated for Src kinase inhibitory activities. The unsubstituted N-benzyl derivative (8a) showed the inhibition of c-Src kinase with GI50 values of 1.34 μM and 2.30 M in NIH3T3/c-Src527F and SYF/c-Src527F cells, respectively. All the synthesized compounds were evaluated for inhibition of cell proliferation of human colon carcinoma (HT-29), breast carcinoma (BT-20), and leukemia (CCRF-CEM) cells. …
Fatty Acyl Amide Dderivatives Of Doxorubicin: Synthesis And In Vitro Anticancer Activities, Bhupender S. Chhikara, Nicole St. Jean, Deendayal Mandal, Anil Kumar, Keykavous Parang
Fatty Acyl Amide Dderivatives Of Doxorubicin: Synthesis And In Vitro Anticancer Activities, Bhupender S. Chhikara, Nicole St. Jean, Deendayal Mandal, Anil Kumar, Keykavous Parang
Pharmacy Faculty Articles and Research
Doxorubicin is an anticancer drug extensively used in anticancer therapy. Doxorubicin is highly hydrophilic, has short half-life, and its use is associated with severe side effects at high doses. Fatty acyl amide derivatives of doxorubicin were synthesized with the expectation to improve the lipophilicity and anticancer activity of the drug. The lipophilicity was enhanced with the increase in chain length of fatty acyl moiety. Conjugation of 4-amino group with fatty acids through an amide bond reduced the anticancer activity in leukemia, breast, ovarian, and colon cancer cell lines, suggesting that the presence of free amino group is required for anticancer …