Medicine and Health Sciences Commons^™

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 7077% at a concentration of 50 μM. The unsubstituted phenyl (4d) and 3-nitrophenyl (4l) derivatives showed the inhibition of c-Src kinase …

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.

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. …

Aplastic Anemia: Clinicohaematological Features, Treatment And Outcome Analysis, Rabia Wali, Zehra Fidoo, Salman Adil, Muhammad Ahmed Naqvi

Department of Pathology and Laboratory Medicine

Objective: To determine the clinicohaematological features, treatment and outcome of children diagnosed with aplastic anemia at a single institution.

Study Design: Observational study.

Place and Duration of Study: The Aga Khan University Hospital, Karachi, from January 1999 till December 2008.

Methodology: Medical records of children aged less than 15 years of age diagnosed with aplastic anemia were reviewed. Clinicohaematological features, treatment and its response to therapy and outcome were recorded. Results were described in percentages.

Results: Ninety patients were diagnosed to have aplastic anemia (AA); 65 were male during the study period. Age ranged from 1 to 15 years. Fever …

A Concept Mapping Needs Assessment Of Young Families With Parental Cancer, Richard P. Durant

Antioch University Dissertations & Theses

The purpose of this research is to investigate the support needs of young families living with and beyond a parental diagnosis of cancer. The sample includes 56 participants comprised of 31 professional stakeholders and 25 patient stakeholders affiliated with the Charles R. Wood Cancer Center. It was hypothesized there would be differences in how the groups of stakeholders rated needs in terms of importance, satisfaction, and utilization. Differences in ratings are thought to be barriers to effective program development. While not a formal research hypothesis, it was anticipated other program development barriers germane to naturalistic clinical settings would emerge from …

Work Interrupted: A Questionnaire Assessing The Relationship Between Work-Related Distress And Psychological Adjustment To Cancer, Betsy A. Bates Freed

Antioch University Dissertations & Theses

Cancer is an increasingly survivable disease that significantly impacts the ability of individuals to negotiate successfully the developmental task most distinctly affiliated with middle adulthood: creating meaning through achievement, creativity, and service. For many adults, these goals are accomplished through employment. When cancer intrudes, patients may be deprived of the ability to participate fully in the “generativity” that developmental psychologist Erik Erikson deemed essential to a healthy adulthood. In qualitative studies, patients’ narratives speak of many work-related losses — of routine, normality, economic stability, social connection, purpose, and identity. While psychosocial issues and quality of life are viewed with increasing …

Oncolog, Volume 56, Number 01, January 2011, Bryan Tutt, Sunni Hosemann

OncoLog MD Anderson's Report to Physicians (All issues)

• New Drug Control Symptoms of Myeloproliferative Disorders and Improve Quality of Life for Patients: Recent clinical trials have demonstrated that a new class of drugs can effectively treat myeloproliferative disorders
• Compass: Metastatic Melanoma: Experimental treatments could be preferable to standard therapies for metastatic melanoma
• HOUS CALL: Breast Awareness: Guidelines recommend breast awareness rather than formal self-exams

Issues Related To Sentinel Lymph Node Assessment In The Management Of Breast Cancer—What Are Relevant In Pathology Reports?, Patricia Tai, Kurian J. Joseph, Edward Yu

Edward Yu

Most cancer centers now perform sentinel node (SN) biopsies. The limited number of SNs sampled compared with an axillary dissection has allowed more comprehensive lymph node analysis resulting in increased detection of micrometastases. Many node-negative cases are now reclassified as micrometastatic. Recent research on SN biopsy focuses on whether axillary dissection is always necessary when the SN is positive. Some subgroups of patients have a higher risk of more nodal metastases when completion axillary dissections were performed. This paper summarizes the different studies and examines what are the clinically relevant items to report on SN node pathology: volume or size …