Chemicals and Drugs Commons^™

Click Chemistry Inspired One-Pot Synthesis Of 1, 4-Disubstituted 1, 2, 3-Triazoles And Their Src Kinase Inhibitory Activity, Dalip Kumar, V. Buchi Reddy, Anil Kumar, Deendayal Mandal, Rakesh Tiwari, Keykavous Parang

Pharmacy Faculty Articles and Research

Two classes of 1,4-disubstituted 1,2,3-triazoles were synthesized using one-pot reaction of α-tosyloxy ketones/α-halo ketones, sodium azide, and terminal alkynes in the presence of aq. PEG (1:1, v/v) using the click chemistry approach and evaluated for Src kinase inhibitory activity. Structure-activity relationship analysis demonstrated that insertion of C6H5- and 4-CH3C6H4- at position 4 for both classes and less bulkier aromatic group at position 1 in class 1 contribute critically to the modest Src inhibition activity (IC50 = 32-43 µM) of 1,4-disubstituted 1,2,3-triazoles.

Inhibition Of Multi-Drug Resistant Hiv-1 Reverse Transcriptase By Nucleoside Beta-Triphosphates, Chandravanu Dash, Yousef Ahmadibeni, Michael J. Hanley, Jui Pandhare, Mathias Gotte, Stuart F. J. Le Grice, Keykavous Parang

Pharmacy Faculty Articles and Research

Despite the success of potent reverse transcriptase (RT) inhibitors against human immunodeficiency virus type 1 (HIV-1) in combination regimens, the development of drug resistant RTs constitutes a major hurdle for the long-term efficacy of current antiretroviral therapy. Nucleoside β-triphosphate analogs of adenosine and nucleoside reverse transcriptase inhibitors (NRTIs) (3′-azido-2′,3′-dideoxythymidine (AZT), 3′-fluoro-2′,3′-dideoxythymidine (FLT), and 2′,3′-didehydro-2′,3′-dideoxythymidine (d4T)) were synthesized and their inhibitory activities were evaluated against wild-type and multidrug resistant HIV-1 RTs. Adenosine β-triphosphate (1) and AZT β-triphosphate (2) completely inhibited the DNA polymerase activity of wild type, the NRTI multi resistant, and nonnucleoside RT inhibitors (NNRTI) resistant HIV-1 RT at 10 …

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. …

Neo-Adjuvant Chemotherapy And Radiation Therapy In Patients With Stage Iiia (N2) Non-Small Cell Lung Cancer (Nsclc): A Retrospective Analysis With Lessons Learned, Eliot L. Friedman Md, Michael F. Szwerc Md, Charles Andrews Md, Robert Kruklitis Md, Kathleen A. Leies, Ferdy Santiago

Department of Medicine

No abstract provided.

Pseudo-Cushing’S Syndrome In A Hiv Patient With Complete Resolution Following Discontinuation Of Darunavir/Ritonavir, Rashmi Sharma Md, Margaret Hoffman-Terry Md, Facp

Department of Medicine

No abstract provided.

Does Tranexamic Acid Effectively And Safely Reduce Menstrual Blood Loss (Mbl) In Women With Menorrhagia Or Iud Induced Mbl?, Veronica W. Chang

PCOM Physician Assistant Studies Student Scholarship

OBJECTIVE: To determine if Tranexamic Acid effectively and safely reduce menstrual blood loss (MBL) in women with Menorrhagia or IUD induced MBL?

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 …

The Role Of Ghrelin And Leptin In Obesity: Is Exogenous Administration Of These Hormones A Possible Drug Therapy?, Peri Eckstein

The Science Journal of the Lander College of Arts and Sciences

Ghrelin and leptin are two hormones that have been recognized to have a major influence on energy balance. Leptin is a mediator of long term regulation of energy balance, suppressing food intake and thereby inducing weight loss. Ghrelin, on the other hand, is a fast acting hormone, playing a role in meal initiation. As a growing number of people suffer from obesity, understanding the mechanisms by which various hormones and neurotransmitters influence energy balance has been a subject of intense research. This paper provides background on leptin and ghrelin hormones, their role in food intake and body weight in humans, …

The Effect Of Melatonin On The Ovaries, Jaclyn Starr

The Science Journal of the Lander College of Arts and Sciences

Melatonin is a very small molecule whose effects can be both detrimental and beneficial to the ovaries depending on its concentration. Too much of anything is usually not good and so is the case with melatonin. Very high doses can be damaging, but in the right amount melatonin may be able to combat various diseases and increase the chances for fertility in women.

Health Risks Of Very Low Cholesterol, Menachem Nagar

The Science Journal of the Lander College of Arts and Sciences

Cholesterol is a molecule central to all human physiological processes at systemic as well as cellular levels. Cholesterol, combined with Apolipoprotein B as low-density lipoprotein (LDL) has been the focus of scientific research because the molecule has been proven to play a role in the development of cardiovascular disease, a disease of pandemic proportions. Considerable scientific and medical attention has been devoted to identifying the role and management of high levels of total serum cholesterol in order to address this global health burden, creating large scale awareness regarding lowering cholesterol concentration in circulation. However, the same molecule, combined into various …

Substituted Coumarin Derivatives: Synthesis And Evaluation Of Antiproliferative And Src Kinase Inhibitory Activities, Abha Kathuria, Sarah Jalal, Rakesh Tiwari, Amir Nasrolahi Shirazi, Shilpi Gupta, Shiv Kumar, Keykavous Parang, Sunil K. Sharma

Pharmacy Faculty Articles and Research

Six classes of coumarin derivatives (i.e. 3-alkyl-4-methylcoumarins, pyranocoumarins, coumarin carboxamides, quaternary ammonium coumarins, 7-aminocoumarins, and 4-aminocoumarins) were synthesized and evaluated for inhibition of cell proliferation of colon adenocarcinoma (HT-29), breast carcinoma (MDA-MB-468 or MCF-7), and human ovarian adenocarcinoma (SK-OV-3) cells. C-3-Alkyl substituted analogs of 4-methylcoumarins and pyranocoumarins, 5 and 6, inhibited the cell proliferation of MDA-MB-468 and SK-OV-3 cells by 53-74%, while 3-decyl substituted pyranocoumarin 10 and triethyl substituted quaternary ammonium coumarin derivative 29 inhibited the cell proliferation of HT-29 and SK-OV-3 cells by 63-72% at a concentration of 50 μM. Among all the compounds studied, C-3 decyl substituted quaternary …

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.

Trends In The Clinical Characteristics Of Hiv Infected Patients Initiating Antiretroviral Therapy In Kenya, Uganda And Tanzania Between 2002 And 2009, Elvin H. Geng, Peter W. Hunt, Lameck O. Diero, Sylvester Kimaiyo, Geofrey R. Somi, Pius Okong, David R. Bangsberg, Mwebesa B. Bwana, Craig R. Cohen, Juliana A. Otieno, Deo Wabwire, Batya Elul, Denis Nash, Philippa J. Easterbrook, Paula Braitstein, Beverly S. Musick, Jeffrey N. Martin, Constantin T. Yiannoutsos, Kara Wools-Kaloustian

Publications and Research

Background: East Africa has experienced a rapid expansion in access to antiretroviral therapy (ART) for HIVinfected patients. Regionally representative socio-demographic, laboratory and clinical characteristics of patients accessing ART over time and across sites have not been well described.

Methods: We conducted a cross-sectional analysis of characteristics of HIV-infected adults initiating ART between 2002 and 2009 in Kenya, Uganda and Tanzania and in the International Epidemiologic Databases to Evaluate AIDS Consortium. Characteristics associated with advanced disease (defined as either a CD4 cell count level of less than 50 cells/mm3 or a WHO Stage 4 condition) at the time of ART initiation …

Androgen Receptor-Dependent Effects Of Resveratrol On Tnsin Mrna Levels In Prostate Cancer Cells, Courtney Pisano

PCOM Biomedical Studies Student Scholarship

The chemopreventive effects of resveratrol (RSV) on cancers, including prostate cancer, have been well documented; but the mechanisms are not well known. It has been reported recently that tensin, a matrix-adhesion protein, which is greatly down-regulated in prostate cancer, has been induced by RSV in several cancer cell lines. In order to know if RSV up-regulates tensin in prostate cells, we first treated LNCaP cells with RSV and demonstrated that tensin mRNA levels were upregulated by RSV in a time and dose dependent manner. Since LNCaP cells are androgen receptor (AR) positive and previous findings have shown that RSV down-regulates …

A Comparison Of Pharmacist Travel-Health Specialists' Versus Primary Care Providers' Recommendations For Travel-Related Medications, Vaccinations, And Patient Compliance In A College Health Setting, Melissa J. Durham, Jeffery A. Goad, Lawrence S. Neinstein, Mimi Lou

Pharmacy Faculty Articles and Research

Background. Pretravel medication and vaccination recommendations and receipt were compared between primary care providers (PCPs) without special training and clinical pharmacists specializing in pretravel health.

Methods. A retrospective chart review of patients seen for pretravel health services in a pharmacist-run travel clinic (PTC) compared to PCPs at a University Student Health Center. Vaccine/medication recommendations were assessed for consistency with national/international guidelines. Medical/pharmacy records were queried to determine the receipt of medications/vaccinations.

Results. The PTC recommended antibiotics for travelers' diarrhea were given more often when indicated (96% vs 50%, p < 0.0001), and patients seen in the PTC received their medications more often (75% vs 63%, p = 0.04). PCPs prescribed more antibiotics for travelers' diarrhea that were inconsistent with guidelines (not ordered when indicated 49% vs 6%, p < 0.0001 and ordered when not indicated 21% vs 3%, p < 0.0001). The PTC prescribed antimalarials more often when indicated (98% vs 81%, p < 0.0001), while PCPs prescribed more antimalarials that were inconsistent with guidelines (not ordered when indicated 15% vs 1%, p < 0.0001 and ordered when not indicated 19% vs 2%, p < 0.0001). The PTC ordered more vaccines per patient when indicated (mean = 2.77 vs 2.31, p = 0.0012). PTC patients were more likely to receive vaccines when ordered (mean = 2.38 vs 1.95, p = 0.0039). PCPs recommended more vaccines per patient that were inconsistent with guidelines (not ordered when indicated: mean = 0.78 vs 0.12, p < 0.0001, ordered when not indicated: mean 0.18 vs 0.025, p < 0.0001).

Conclusions. A pharmacist-run pretravel health clinic can …

Does Melatonin Have A Significantly Positive Effect On Night-Shift Workers' Overall Recovery, Mood, Tiredness, Alertness, Attention, And Sleep Quality?, Vincy Zachariah

PCOM Physician Assistant Studies Student Scholarship

OBJECTIVE: The objective of this systematic review is to verify whether or not Melatonin has a significantly positive effect on night -shift workers' overall recovery, mood, tiredness. alertness, attention. and sleep quality.

What Is The Safety And Efficacy Of Conjugated Linoleic Acid Used For Weight Loss Supplements?, Meghan M. Walsh

PCOM Physician Assistant Studies Student Scholarship

OBJECTIVE: The objective of this systematic review is to determine the safety and efficacy of conjugated linoleic acid for weight loss in obese individuals.

Is Sildenafil Citrate A Safe And Effective Treatment For Pulmonary Hypertension In Adults?, Atekelt Tadese

PCOM Physician Assistant Studies Student Scholarship

OBJECTIVE: To determine whether or not the Phosphodiesterase inhibitors drug Sildenafil Citrate is safe and effective treatment for Pulmonary Hypertension in adults

What Is The Safety And Efficacy Of Tarenflurbil (R-Flurbiprofen) In Mild To Moderate Alzheimer’S Disease?, Lauren Viscount

PCOM Physician Assistant Studies Student Scholarship

OBJECTIVE: The objective of this systematic review is to determine what is the safety and efficacy of Tarenflurbil (R-flubiprofen) in mild to moderate Alzheimer’s Disease.

Are Proton Pump Inhibitors A Safe And Effective Treatment For Gastroesophageal Reflux Disease In Infants Less Than Twelve Months Old?, Mariah Smith

PCOM Physician Assistant Studies Student Scholarship

OBJECTIVE: The objective of this systematic review is to determine whether or not proton pump inhibitors are a safe and effective treatment for gastroesophageal reflux disease in infants less than twelve months old.