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3 results on '"Matthew A. Helppi"'

1. Factors influencing the cytotoxicity of α-methylene-γ-hydroxy esters against pancreatic cancer

Author

Arlie L. Lehmkuhler, Michele T. Yip-Schneider, Jennifer M. Marchi, P. Veeraraghavan Ramachandran, C. Max Schmidt, and Matthew A. Helppi

Subjects
endocrine system diseases, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Antineoplastic Agents, Biochemistry, Structure-Activity Relationship, chemistry.chemical_compound, Cell Line, Tumor, Pancreatic cancer, Drug Discovery, medicine, Humans, Molecule, Structure–activity relationship, Methylene, Cytotoxicity, Molecular Biology, Cell Proliferation, Dose-Response Relationship, Drug, Molecular Structure, Cell growth, Organic Chemistry, Esters, Prodrug, medicine.disease, digestive system diseases, Pancreatic Neoplasms, chemistry, Michael reaction, Molecular Medicine, Drug Screening Assays, Antitumor
Abstract

A systematic study to identify the factors influencing the cytotoxicity of α-methylene-γ-hydroxy esters against three pancreatic cancer cell lines (Panc-1, MIA-PaCa-2, and BxPC-3) has established that, in addition to Michael acceptor abilities, the possibility to lactonize to α-methylene-γ-butyrolactones is as important. The substitution pattern and the number of carbons between the hydroxy and ester moieties also influence the bio-activity.

Published
2015
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2. ChemInform Abstract: Synthetic α-(Aminomethyl)-γ-butyrolactones and Their anti-Pancreatic Cancer Activities

Author

C. Max Schmidt, Matthew A. Helppi, Michele T. Yip-Schneider, Pravin D. Gagare, P. Veeraraghavan Ramachandran, Hari Nair, and Daniel R. Nicponski

Subjects
Pancreatic cancer cell, Chemistry, Pancreatic cancer, education, medicine, Cancer research, General Medicine, medicine.disease, humanities
Abstract

A variety of aminolactones such as (III) are synthesized which exhibit excellent activities against three pancreatic cancer cell lines

Published
2014
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3. Synthetic α-(aminomethyl)-γ-butyrolactones and their anti-pancreatic cancer activities

Author

C. Max Schmidt, Matthew A. Helppi, Michele T. Yip-Schneider, P. Veeraraghavan Ramachandran, Hari Nair, Daniel R. Nicponski, and Pravin D. Gagare

Subjects
endocrine system diseases, Stereochemistry, Cell Survival, Clinical Biochemistry, Pharmaceutical Science, Antineoplastic Agents, Biochemistry, chemistry.chemical_compound, Structure-Activity Relationship, 4-Butyrolactone, Pancreatic cancer, Cell Line, Tumor, Drug Discovery, medicine, Humans, Parthenolide, Molecular Biology, Amination, Chemistry, Organic Chemistry, Biological activity, Stereoisomerism, medicine.disease, digestive system diseases, Pancreatic Neoplasms, Pancreatic cancer cell, Molecular Medicine, Amine gas treating, Sesquiterpenes
Abstract

Aminated α-methylene-γ-butyrolactones, which are readily synthesized with facile control of the diastereoisomerism, provide an economical and commercially-viable alternative to the use of aminated natural products. These aminoloactones, which exhibit excellent activity against three pancreatic cancer cell lines when measured at 10 μM-Panc-1, MIA PaCa-2, and BxPC-3-and are comparable to or better than parthenolide and dimethylaminoparthenolide (DMAPT, LC-1). It has also been shown that there is an effect on the biological activity depending on the identity of the amine.

Published
2013

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