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Articles 31 - 60 of 61
Full-Text Articles in Immune System Diseases
Haiti's Hiv Surveillance System: Past, Present, And Future, Chris Delcher, Ermane G. Robin, Daniella Myriam Pierre
Haiti's Hiv Surveillance System: Past, Present, And Future, Chris Delcher, Ermane G. Robin, Daniella Myriam Pierre
Pharmacy Practice and Science Faculty Publications
No abstract provided.
Cancer-Targeting Immunostimulatory Peptides As An Immunotherapeutic Approach To Cancer, Rachel Montel
Cancer-Targeting Immunostimulatory Peptides As An Immunotherapeutic Approach To Cancer, Rachel Montel
Seton Hall University Dissertations and Theses (ETDs)
This dissertation reports the synthesis and biological applications of bifunctional trimeric peptides with B7H6-derived NKp30 binding motifs that serve to activate an immunocytotoxic response in natural killer cells and a GRP78-binding motif that can target tumors that express surface GRP78. In this manner the cancer-targeting immunostimulatory peptides are anticipated to directly bind and activate effector NK92-MI cells while also recognizing and binding to target A549 tumor cells to facilitate NK cell-dependent immunocytotoxicity of the targeted tumors. The NKp30 binding peptide motifs are derived from the tumor associated B7H6 antigen that is often downregulated or shed from the surface of tumors …
Cancer Pain And The Risks Of Opioid Abuse, Yarelis Diaz
Cancer Pain And The Risks Of Opioid Abuse, Yarelis Diaz
College of Pharmacy Student Research
No abstract provided.
Vaccines In Current Culture: The Hpv Vaccine Controversy, Alyssa Johnston
Vaccines In Current Culture: The Hpv Vaccine Controversy, Alyssa Johnston
Senior Honors Theses
The use of vaccinations has drastically decreased mortality and morbidity rates related to infectious disease and has become an intrinsic part of modern health care. However, the fear of risks related to vaccines has been partially responsible for the decisions of many parents to delay or avoid vaccinating their children. The human papilloma virus (HPV) vaccine specifically is one of the most controversial vaccines in current culture due to reports of new onset or exacerbation of autoimmune diseases, infertility, and even death following its administration. This review synthesizes information regarding the relevance and safety of the HPV vaccine, as well …
Tobacco/Hiv-1-Induced Myeloid Cell-Derived Extracellular Vesicles In Hiv-1 Pathogenesis, Sanjana Haque
Tobacco/Hiv-1-Induced Myeloid Cell-Derived Extracellular Vesicles In Hiv-1 Pathogenesis, Sanjana Haque
Theses and Dissertations (ETD)
Introduction. Smoking, which is highly prevalent in people living with HIV/AIDS, has been shown to exacerbate HIV-1 replication, in part via cytochrome P450 (CYP)-induced oxidative stress. CYP enzymes metabolize cigarette smoke condensate (CSC), causing oxidative stress and cytotoxicity. Our previous studies have demonstrated that CSC and specific CSC constituents, benzo(a)pyrene and nicotine, potentially induce CYPs, resulting in higher oxidative stress and subsequent exacerbation of HIV-1 replication in monocytes and macrophages. However, the exact mechanism behind tobacco-induced, oxidative stress-mediated enhancement of HIV-1 replication is still poorly understood. Extracellular vesicles (EVs) have recently gained attention for their unique nature as intercellular messengers …
Delivery Of Small Molecule And Rna Using Synthetic Polymeric Micelles And Multifunctional Exosomes For The Treatment Of Type 1 Diabetes, Yang Peng
Theses & Dissertations
Type 1 diabetes is one of the most challenging chronic autoimmune diseases. The destruction and dysfunction of insulin-secreting β cells are the results of inflammatory infiltration and the synergistic effect of multiple immune cells. The aim of this dissertation is to develop novel and reliable therapeutic approaches to advance the treatment of T1D: including chemical modification of a broad-spectrum immunosuppressant, co-application of small molecule based immune intervention and siRNA based β cell preservative therapy, and administration of a PI3K-δ/γ dual inhibitor to specifically target immune cells, utilizing synthetic polymeric micelles or natural produced multi-functional exosomes derived from human bone marrow …
Recent Advances Spark Significant Guideline Change: Antiretroviral Therapy (Art) At High Cd4+ Counts In The Treatment Naïve Patient, Joshua Ilenin, Kelly Fargo, Lisa Berni, Kristen Thatcher, Caitlin Swann, Andrew Roecker
Recent Advances Spark Significant Guideline Change: Antiretroviral Therapy (Art) At High Cd4+ Counts In The Treatment Naïve Patient, Joshua Ilenin, Kelly Fargo, Lisa Berni, Kristen Thatcher, Caitlin Swann, Andrew Roecker
Pharmacy and Wellness Review
Human immunodeficiency virus (HIV) targets CD4+ lymphocytes, a critical component to proper functioning of the human immune system. HIV is a significant public health concern, having resulted in over 27 million deaths since its discovery. Currently, several different treatment options exist, with combination antiretroviral therapy (ART) at the forefront. Despite the success of ART therapy, there are number of problems, including poor patient compliance. Due to this, the appropriate time to initiate therapy in the treatment naïve patient is under continuous scrutiny. Recently, several trials have demonstrated evidence suggesting that initiating ART at high CD4+ counts in the treatment naïve …
The Hiv Vaccine: Learning From Failure And Building On Success, Lindsey Mcclish, Kimberly Gathers, Katie Salay, Lisa Vranekovic, Kristin Seaman, Kelly M. Shields
The Hiv Vaccine: Learning From Failure And Building On Success, Lindsey Mcclish, Kimberly Gathers, Katie Salay, Lisa Vranekovic, Kristin Seaman, Kelly M. Shields
Pharmacy and Wellness Review
An effective vaccine for acquired immune deficiency syndrome (AIDS) has eluded researchers since the identification of the HIV virus. There are many challenges in developing an effective HIV vaccine, including the lack of knowledge regarding the immune response to the virus and its diverse nature. Ethical concerns further complicate research. A recent phase III trial was performed in Thailand and showed that a significant reduction in HIV infection is possible. Pharmacists need to stay informed of these important breakthroughs in AIDS research in order to provide quality health information to patients in their community. This paper aims to evaluate the …
Synthesis And Characterization Of Long-Acting Rilpivirine Prodrugs, James R. Hilaire
Synthesis And Characterization Of Long-Acting Rilpivirine Prodrugs, James R. Hilaire
Theses & Dissertations
Antiretroviral therapy (ART) requires lifelong daily dosing to suppress viral replication, restore or maintain immune function and improve quality of life. As an alternative, long-acting (LA) antiretrovirals (ARVs) aim to deliver therapeutic drug concentrations over an extended period, ultimately requiring monthly or even more extended dosing intervals. Specifically, the success of recent clinical trials examining LA cabotegravir and rilpivirine (CAB and RPV LA) highlight the advent of these novel HIV-1 therapeutics. Further optimization of LA dosage forms are required and rests upon improving dosing frequency, injection volumes and tissue distribution to viral compartments. To this end, we report the synthesis …
Retrospective Review Of Alternative Antibiotic Use In Patients With A Reported Penicillin Allergy At A Community Hospital, Rita Chamoun, Monica Tadros, Amy Montes, Heidi Clarke, Radhan Gopalani
Retrospective Review Of Alternative Antibiotic Use In Patients With A Reported Penicillin Allergy At A Community Hospital, Rita Chamoun, Monica Tadros, Amy Montes, Heidi Clarke, Radhan Gopalani
All Publications
No abstract provided.
Radical Social Ecology As Deep Pragmatism: A Call To The Abolition Of Systemic Dissonance And The Minimization Of Entropic Chaos, Arielle Brender
Radical Social Ecology As Deep Pragmatism: A Call To The Abolition Of Systemic Dissonance And The Minimization Of Entropic Chaos, Arielle Brender
Student Theses 2015-Present
This paper aims to shed light on the dissonance caused by the superimposition of Dominant Human Systems on Natural Systems. I highlight the synthetic nature of Dominant Human Systems as egoic and linguistic phenomenon manufactured by a mere portion of the human population, which renders them inherently oppressive unto peoples and landscapes whose wisdom were barred from the design process. In pursuing a radical pragmatic approach to mending the simultaneous oppression and destruction of the human being and the earth, I highlight the necessity of minimizing entropic chaos caused by excess energy expenditure, an essential feature of systems that aim …
Immune Checkpoint Inhibition And The Prevalence Of Autoimmune Disorders Among Patients With Lung And Renal Cancer, Sherif M. El-Refai
Immune Checkpoint Inhibition And The Prevalence Of Autoimmune Disorders Among Patients With Lung And Renal Cancer, Sherif M. El-Refai
Pharmaceutical Sciences Faculty Publications
PURPOSE: Immune checkpoint inhibition reactivates the immune response against cancer cells in multiple tissue types and has been shown to induce durable responses. However, for patients with autoimmune disorders, their conditions can worsen with this reactivation. We sought to identify, among patients with lung and renal cancer, how many harbor a comorbid autoimmune condition and may be at risk of worsening their condition while on immune checkpoint inhibitors such as nivolumab and pembrolizumab.
METHODS: An administrative health care claims database, Truven MarketScan, was used to identify patients diagnosed with lung and renal cancer from 2010 to 2013. We assessed patients …
Cyclophosphamide For Suspected Primary Angiitis Of The Central Nervous System In A Patient With Human Immunodeficiency Virus: A Case Report, Martha M. Rumore, Samantha Su, Jake Pellinen
Cyclophosphamide For Suspected Primary Angiitis Of The Central Nervous System In A Patient With Human Immunodeficiency Virus: A Case Report, Martha M. Rumore, Samantha Su, Jake Pellinen
Touro College of Pharmacy (New York) Publications and Research
Introduction: Central nervous system (CNS) vasculitis is rare, including in human immunodeficiency virus (HIV), occurring in less than 1% of patients. Systemic vasculitis affecting the CNS is termed secondary CNS vasculitis, whereas primary CNS vasculitis, referred to as primary angiitis of the CNS (PACNS) refers to an extremely rare disease specifically confined to the CNS. Only some cases of PACNS in HIV patients have been reported in literature.
Case Report: We report a case of a 46-year-old female with HIV who developed probable primary CNS vasculitis, which was treated with intravenous cyclophosphamide and glucocorticoids for both induction and …
Improving The Renal Profile Of A Hiv Drug Combination Through Prodrug Alteration, Derek E. Murrell, Sam Harirforoosh
Improving The Renal Profile Of A Hiv Drug Combination Through Prodrug Alteration, Derek E. Murrell, Sam Harirforoosh
Pharmacy Faculty Articles and Research
"Human immunodeficiency virus (HIV) continues to alter the lives of countless individuals, who once infected, live on a continuum between viral suppression and acquired immunodeficiency syndrome. The former being achieved via the use of various antiretrovirals beginning with the release of zidovudine over a quarter-century ago; whereas the latter may result from treatment failure or lack of treatment such as in the absence of diagnosis or the inaccessibility of medication. As no cure is yet available, regimens must be continued lifelong. Thus, contemporary treatment is given as a combination of agents from various antiretroviral drug classes in an effort to …
Cationic Cell-Penetrating Peptides Are Potent Furin Inhibitors, Bruno Ramos-Molina, Adam N. Lick, Amir Nasrolahi Shirazi, Donghoon Oh, Rakesh Tiwari, Naglaa Salem El-Sayed, Keykavous Parang, Iris Lindberg
Cationic Cell-Penetrating Peptides Are Potent Furin Inhibitors, Bruno Ramos-Molina, Adam N. Lick, Amir Nasrolahi Shirazi, Donghoon Oh, Rakesh Tiwari, Naglaa Salem El-Sayed, Keykavous Parang, Iris Lindberg
Pharmacy Faculty Articles and Research
Cationic cell-penetrating peptides have been widely used to enhance the intracellular delivery of various types of cargoes, such as drugs and proteins. These reagents are chemically similar to the multi-basic peptides that are known to be potent proprotein convertase inhibitors. Here, we report that both HIV-1 TAT47-57 peptide and the Chariot reagent are micromolar inhibitors of furin activity in vitro. In agreement, HIV-1 TAT47-57 reduced HT1080 cell migration, thought to be mediated by proprotein convertases, by 25%. In addition, cyclic polyarginine peptides containing hydrophobic moieties which have been previously used as transfection reagents also exhibited potent furin inhibition in vitro …
Evaluating The Effects Of An Interdisciplinary Practice Model With Pharmacist Collaboration On Hiv Patient Co-Morbidities, Rebecca Cope, Leonard Berkowitz, Rebecca Arcebido, Jun-Yen Yeh, Nathan Trustman, Agnes Cha
Evaluating The Effects Of An Interdisciplinary Practice Model With Pharmacist Collaboration On Hiv Patient Co-Morbidities, Rebecca Cope, Leonard Berkowitz, Rebecca Arcebido, Jun-Yen Yeh, Nathan Trustman, Agnes Cha
Touro College of Pharmacy (New York) Publications and Research
Treatment of HIV now occurs largely within the primary care setting, and the principal focus of most visits has become the management of chronic disease states. The clinical pharmacist’s potential role in improving chronic disease outcomes for HIV patients is unknown. A retrospective cohort study was performed for HIV-positive patients also diagnosed with diabetes, hypertension, or hyperlipidemia. Characteristics and outcomes in 96 patients treated by an interdisciplinary team which included a clinical pharmacist (i.e., the intervention group) were compared to those in 50 patients treated by an individual healthcare provider (i.e., the control group). Primary outcomes were changes from baseline …
Customized Order-Entry Sets Can Prevent Antiretroviral Prescribing Errors: A Novel Opportunity For Antimicrobial Stewardship, Yi Guo, Philip Chung, Caryn Weiss, Keith Veltri, Grace Y. Minamoto
Customized Order-Entry Sets Can Prevent Antiretroviral Prescribing Errors: A Novel Opportunity For Antimicrobial Stewardship, Yi Guo, Philip Chung, Caryn Weiss, Keith Veltri, Grace Y. Minamoto
Touro College of Pharmacy (New York) Publications and Research
Background: Patients with human immunodeficiency virus (HIV) infection on antiretroviral (ARV) therapy are at increased risk for medication errors during transitions of care between the outpatient and inpatient settings. This can lead to treatment failure or toxicity. Previous studies have emphasized the prevalence of medication errors in such patients, but few have reported initiatives to prevent errors from occurring.
Methods: The study was conducted in a 1,400-bed health care center with a state-designated Acquired Immunodeficiency Syndrome (AIDS) Center in the Bronx, New York. The antimicrobial stewardship team and HIV specialists developed customized order-entry sets (COES) to guide ARV …
Majority Of Hiv/Hcv Patients Need To Switch Antiretroviral Therapy To Accommodate Direct Acting Antivirals, Rebecca Cope, Aaron Pickering, Thomas Glowa, Samantha Faulds, Peter Veldkamp, Ramakrishna Prasad
Majority Of Hiv/Hcv Patients Need To Switch Antiretroviral Therapy To Accommodate Direct Acting Antivirals, Rebecca Cope, Aaron Pickering, Thomas Glowa, Samantha Faulds, Peter Veldkamp, Ramakrishna Prasad
Touro College of Pharmacy (New York) Publications and Research
The impact of drug–drug interactions (DDIs) between interferon-free direct acting antiviral (DAA) regimens and antiretrovirals (ART) among HIV/HCV co-infected individuals in clinical practice settings is unknown. A singlecenter, retrospective chart review of co-infected patients was conducted from June 2014 to February 2015. Significant interactions between simeprevir (SMV), ledipasvir (LDV), and paritaprevir/ritonavir/ombitasvir plus dasabuvir (3D regimen) with ART were identified based on available literature. SMV had the largest number of DDIs and was further investigated to determine the feasibility of ART switch to allow for DAA use. Of 127 subjects, 23% had advanced liver disease; 86% of those with known HCV …
Compliance To The Consort Statement On Participant Flow Diagrams In Infectious Disease Randomized Clinical Trials, Onyeka P. Godwin, Brandon Dyson, Paul S. Lee, Soon Park, Euni Lee
Compliance To The Consort Statement On Participant Flow Diagrams In Infectious Disease Randomized Clinical Trials, Onyeka P. Godwin, Brandon Dyson, Paul S. Lee, Soon Park, Euni Lee
Pharmacy Faculty Articles and Research
Background: The Consolidated Standard of Reporting Trials (CONSORT) Guidelines were developed to support adequate reporting of randomized controlled trials (RCTs).
Method: A systematic review was conducted including RCTs of infectious diseases published in the top general medical and infectious disease journals in 2010. The level of compliance to flow diagram and its association with the CONSORT endorsement by the journals were evaluated.
Results: A total of 67 studies were included in the analysis and a half of the studies were HIV/AIDS RCTs. About 78% of the studies included the flow diagram and 66% of the studies described …
Analysis Of Humira, Electro-Acupuncture, And Pulsatile Dry Cupping On Reducing Joint Inflammation In Patients With Rheumatoid Arthritis, Natalie Noll
AUCTUS: The Journal of Undergraduate Research and Creative Scholarship
Humira, an anti-TNF drug aimed at decreasing inflammation in Rheumatoid Arthritis patients, can cause skin diseases from rashes to skin cancer. Humira works by blocking the chemical receptor RANKL which inhibits the production of osteoclasts. Osteoclasts are cells that attack and eat bone and cartilage therefore an inhibitory mechanism would cause inflammation.. By analyzing Humira’s effect on the human body, Humira can be compared to other treatments such as electro-acupuncture and pulsatile dry cupping to determine the viability of these alternative treatment methods in regards to their abilities to decrease inflammation in Rheumatoid Arthritis patients through blocking RANKL. An analysis …
Nanotoxicity In Cells Of The Immune System, Jonathan J. Pelc
Nanotoxicity In Cells Of The Immune System, Jonathan J. Pelc
Science Scholars
Nanoparticles (NPs) provide a new medical approach to drug therapy. As with every new approach, safety precautions need to be taken, and the immediate and long-term effects for many NPs are still unclear. When administering a medical treatment into the human body, the first issue that needs to be addressed is host detection of the medicine and inflammation as a possible result of the treatment. If a new NP treatment causes inflammation before it releases its medicine, that treatment may be ineffective, even damaging to the patient. Small metallic and organic particles have been shown to elicit an inflammatory responses …
Research Fatigue Among Injecting Drug Users In Karachi, Pakistan, Aysha Zahidie, Arshad Altaf, Adeel Ahsan, Tanzil Jamali
Research Fatigue Among Injecting Drug Users In Karachi, Pakistan, Aysha Zahidie, Arshad Altaf, Adeel Ahsan, Tanzil Jamali
Community Health Sciences
Background
Karachi is the largest metropolis of Pakistan and its economic hub attracting domestic migrants for economic opportunities. It is also the epicenter of HIV epidemic in the country. Since 2004, one pilot study and four behavioral and biological surveillance rounds have been conducted in Karachi. In addition many student research projects have also focused on key risk groups including injection drug users (IDUs). As a result of this extra ordinary exposure of same kind of questions, IDUs know how to respond to high value questions related to sharing of needles or unsafe sexual practices. The purpose of the study …
Chronic Hepatitis B And C Co-Infection Increased All-Cause Mortality In Haart-Naive Hiv Patients In Northern Thailand, N. Tsuchiya, P. Pathipvanich, A. Rojanawiwat, N. Wichukchinda, I. Koga, M. Koga, W. Auwanit, P. E. Kilgore, K. Ariyoshi, P. Sawanpanyalert
Chronic Hepatitis B And C Co-Infection Increased All-Cause Mortality In Haart-Naive Hiv Patients In Northern Thailand, N. Tsuchiya, P. Pathipvanich, A. Rojanawiwat, N. Wichukchinda, I. Koga, M. Koga, W. Auwanit, P. E. Kilgore, K. Ariyoshi, P. Sawanpanyalert
Department of Pharmacy Practice
A total of 755 highly active antiretroviral therapy (HAART)-naive HIV-infected patients were enrolled at a government hospital in Thailand from 1 June 2000 to 15 October 2002. Census date of survival was on 31 October 2004 or the date of HAART initiation. Of 700 (92.6%) patients with complete data, the prevalence of hepatitis B virus (HBV) surface antigen and anti-hepatitis C virus (HCV) antibody positivity was 11.9% and 3.3%, respectively. Eight (9.6%) HBV co-infected patients did not have anti-HBV core antibody (anti-HBcAb). During 1166.7 person-years of observation (pyo), 258 (36.9%) patients died [22.1/100 pyo, 95% confidence interval (CI) 16.7–27.8]. HBV …
Nonclinical Development Needs And Regulatory Requirements For Multipurpose Prevention Technologies: A Primer, Joseph W. Romano, Martha Brady, Judy Manning
Nonclinical Development Needs And Regulatory Requirements For Multipurpose Prevention Technologies: A Primer, Joseph W. Romano, Martha Brady, Judy Manning
HIV and AIDS
This summary outlines key development elements that will be necessary for various configurations of multipurpose prevention products for the simultaneous prevention of HIV, sexually transmitted infections, and/or pregnancy.
Shaping The Operations Research Agenda For Antiretroviral-Based Prevention Products For Women: Gels And Rings, Martha Brady, C. Elizabeth Mcgrory
Shaping The Operations Research Agenda For Antiretroviral-Based Prevention Products For Women: Gels And Rings, Martha Brady, C. Elizabeth Mcgrory
HIV and AIDS
This report summarizes discussions from a two-day international experts consultation meeting in 2012 on preparing for the successful introduction of women-centered antiretroviral-based HIV prevention methods. It examines the limits and expectations of operations research in antiretroviral health technologies.
N-Myristoylglutamic Acid Derivative Of 3′-Fluoro-3′- Deoxythymidine As An Organogel, Bhupender S. Chhikara, Rakesh Tiwari, Keykavous Parang
N-Myristoylglutamic Acid Derivative Of 3′-Fluoro-3′- Deoxythymidine As An Organogel, Bhupender S. Chhikara, Rakesh Tiwari, Keykavous Parang
Pharmacy Faculty Articles and Research
Designing microbicidal gels of anti-HIV drugs for local application to prevent HIV infection is a subject of major interest. 3′-Fluoro-3′-deoxythymidine (FLT), a nucleoside reverse transcriptase inhibitor (NRTI), was conjugated with a N-myristoylglutamate scaffold. The conjugate showed gelation at 1% (w/w) in different organic solvents, such as toluene, dichloromethane, and chloroform. The gels were opaque and stable at room temperature. The results indicate that myristoyl glutamate derivative of FLT can form an organogel. The gel could have potential application as a topical anti-HIV microbicidal agent.
Hepatic Immunosuppressive Effects Of Systemically- Administered Novel Dextran-Methylprednisolone Prodrugs With Peptide Linkers In Rats, Imam H. Shaik, Hitesh K. Agarwal, Keykavous Parang, Reza Mehvar
Hepatic Immunosuppressive Effects Of Systemically- Administered Novel Dextran-Methylprednisolone Prodrugs With Peptide Linkers In Rats, Imam H. Shaik, Hitesh K. Agarwal, Keykavous Parang, Reza Mehvar
Pharmacy Faculty Articles and Research
The hepatic immunosuppressive activities of two novel dextran prodrugs of methylprednisolone (MP) containing one (DMP1) or five (DMP5) amino acids as linkers were studied in rats. At various times (02 weeks) after intravenous administration of single 5 mg/kg (MP equivalent) doses of each prodrug or MP succinate (MPS), livers were isolated and immunologically stimulated ex vivo with lipopolysaccharide. The concentrations of tumor necrosis factor (TNF)-a in the outlet perfusate were then quantitated to assess immune response. Additionally, the concentrations of DMP1, DMP5, and/or MP were measured in the liver. MPS, DMP5, or DMP1 injections caused a maximum of 48.9%, 63.5%, …
Facilitating Regulatory Approval Of Multipurpose Prevention Technologies For Sexual And Reproductive Health, Martha Brady
Facilitating Regulatory Approval Of Multipurpose Prevention Technologies For Sexual And Reproductive Health, Martha Brady
HIV and AIDS
This brief describes multipurpose prevention technologies (MPTs) that address women's sexual and reproductive health (SRH) needs, and how to go about facilitating regulatory approval of this technology. It outlines a strategic framework to examine current regulatory guidance, as well a product development pathway to bring MPTs to market.
Constructing A Critical Path For Product Development, Commercialization, And Access, Martha Brady
Constructing A Critical Path For Product Development, Commercialization, And Access, Martha Brady
HIV and AIDS
This brief discusses the Council's health technologies development and the product development path from conceptualization to market. It defines the steps in the Critical Path Framework, and examines activities at the preclinical and clinical stage.
Synthesis Of 3-Phenylpyrazolopyrimidine-1,2,3-Triazole Conjugates And Evaluation Of Their Src Kinase Inhibitory And Anticancer Activities, Anil Kumar, Israr Ahmad, Bhupender S. Chhikara, Rakesh Tiwari, Deendayal Mandal, Keykavous Parang
Synthesis Of 3-Phenylpyrazolopyrimidine-1,2,3-Triazole Conjugates And Evaluation Of Their Src Kinase Inhibitory And Anticancer Activities, Anil Kumar, Israr Ahmad, Bhupender S. Chhikara, Rakesh Tiwari, Deendayal Mandal, Keykavous Parang
Pharmacy Faculty Articles and Research
A series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chemistry approach. All compounds were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA-MB-361), and colon adenocarcinoma (HT-29). Hexyl triazolyl-substituted 3-phenylpyrazolopyrimidine exhibited inhibition of Src kinase with an IC50 value of 5.6 µM. 4-Methoxyphenyl triazolyl-substituted 3-phenylpyrazolopyrimidine inhibited the cell proliferation of HT-29 and SK-Ov-3 by 73% and 58%, respectively, at a concentration of 50 µM.