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Your search keyword '"Chahrour, Osama"' showing total 3 results
Start Over Author "Chahrour, Osama" Topic sulfones
3 results on '"Chahrour, Osama"'

1. Discovery of (E)-3-((styrylsulfonyl)methyl)pyridine and (E)-2-((styrylsulfonyl)methyl)pyridine derivatives as anticancer agents: synthesis, structure-activity relationships, and biological activities.

Author

Lu T, Goh AW, Yu M, Adams J, Lam F, Teo T, Li P, Noll B, Zhong L, Diab S, Chahrour O, Hu A, Abbas AY, Liu X, Huang S, Sumby CJ, Milne R, Midgley C, and Wang S

Subjects
Animals, Annexin A5, Antineoplastic Agents pharmacokinetics, Apoptosis drug effects, Area Under Curve, Biological Availability, Cell Cycle drug effects, Cell Line, Tumor, Cell Proliferation drug effects, Crystallography, X-Ray, Drug Design, Drug Discovery, Glycine pharmacology, Half-Life, Indicators and Reagents, Kaplan-Meier Estimate, Magnetic Resonance Spectroscopy, Mass Spectrometry, Mice, Microsomes, Liver metabolism, Models, Molecular, Rats, Structure-Activity Relationship, Xenograft Model Antitumor Assays, Aminopyridines chemical synthesis, Aminopyridines pharmacology, Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Glycine analogs & derivatives, Styrenes chemical synthesis, Styrenes pharmacology, Sulfonamides chemical synthesis, Sulfonamides pharmacology, Sulfones pharmacology
Abstract

ON01910.Na is a highly effective anticancer agent that induces mitotic arrest and apoptosis. Clinical studies with ON01910 in cancer patients have shown efficacy along with an impressive safety profile. While ON01910 is highly active against cancer cells, it has a low oral availability and requires continuous intravenous infusion or multiple gram doses to ensure sufficient drug exposure for biological activity in patients. We have identified two novel series of styrylsulfonyl-methylpyridines. Lead compounds 8, 9a, 18 and 19a are highly potent mitotic inhibitors and selectively cytotoxic to cancer cells. Impressively, these compounds possess excellent pharmaceutical properties and two lead drug candidates 9a and 18 demonstrated antitumor activities in animal models.

Published
2014
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2. Synthesis and biological evaluation of benzyl styrylsulfonyl derivatives as potent anticancer mitotic inhibitors

Author

Chahrour, Osama, Abdalla, Ashraf, Lam, Frankie, Midgley, Carol, and Wang, Shudong

Subjects
*ORGANIC synthesis, *SULFONES, *ANTINEOPLASTIC agents, *ENZYME inhibitors, *APOPTOSIS, *CANCER treatment, *PROTEIN-tyrosine kinases
Abstract

Abstract: We herein report the synthesis, biological activity and structure activity relationship of derivatives of benzylstyrylsulfone, benzylstyrylsulfine and benzylsulfonyl-N-phenylacetamide. A lead compound 7 represents a new class of mitotic inhibitors that demonstrates potent anti-proliferative activity and selectively induces cancer cell apoptosis while sparing non-transformed lung fibroblast. [Copyright &y& Elsevier]

Published
2011
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3. Discovery of (E)-3-((Styrylsulfonyl)methyl)pyridine and (E)-2-((Styrylsulfonyl)methyl)pyridine Derivatives as Anticancer Agents: Synthesis, Structure–Activity Relationships, and Biological Activities

Author

Osama Chahrour, Xiangrui Liu, Ben Noll, Theodosia Teo, Aik Wye Goh, Mingfeng Yu, Abdullahi Y. Abbas, Robert W. Milne, Longjin Zhong, Christopher J. Sumby, Shiliang Huang, Anran Hu, Frankie Lam, Julian Adams, Peng Li, Carol Midgley, Sarah Diab, Tiangong Lu, Shudong Wang, Lu, Tiangong, Goh, Aik Wye, Yu, Mingfeng, Adams, Julian, Lam, Frankie, Teo, Theodosia, Li, Peng, Noll, Ben, Zhong, Longjin, Diab, Sarah, Chahrour, Osama, Hu, Anran, Abbas, Abdullahi Y, Liu, Xiangrui, Huang, Shiliang, Sumby, Christopher J, Milne, Robert, Midgley, Carol, and Wang, Shudong

Subjects
Models, Molecular, Drug, Magnetic Resonance Spectroscopy, media_common.quotation_subject, Glycine, Aminopyridines, Biological Availability, Antineoplastic Agents, Apoptosis, Kaplan-Meier Estimate, Pharmacology, Crystallography, X-Ray, Mass Spectrometry, Styrenes, Mice, Structure-Activity Relationship, Cell Line, Tumor, Drug Discovery, medicine, cancer, Animals, Cytotoxic T cell, Structure–activity relationship, Sulfones, Annexin A5, genes, Cell Proliferation, media_common, Sulfonamides, Drug discovery, Chemistry, Cell Cycle, Cancer, protein kinase, Biological activity, cell, Cell cycle, medicine.disease, Xenograft Model Antitumor Assays, drug therapy, Rats, Biochemistry, Area Under Curve, Drug Design, Cancer cell, Microsomes, Liver, Molecular Medicine, Indicators and Reagents, Half-Life
Abstract

ON01910.Na is a highly effective anticancer agent that induces mitotic arrest and apoptosis. Clinical studies with ON01910 in cancer patients have shown efficacy along with an impressive safety profile. While ON01910 is highly active against cancer cells, it has a low oral availability and requires continuous intravenous infusion or multiple gram doses to ensure sufficient drug exposure for biological activity in patients. We have identified two novel series of styrylsulfonyl-methylpyridines. Lead compounds 8, 9a, 18 and 19a are highly potent mitotic inhibitors and selectively cytotoxic to cancer cells. Impressively, these compounds possess excellent pharmaceutical properties and two lead drug candidates 9a and 18 demonstrated antitumor activities in animal models. Refereed/Peer-reviewed

Published
2014
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