Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents
| Autor: | John Drewe, Ben Tseng, William Kemnitzer, Shailaja Kasibhatla, Sui Xiong Cai, Han-Zhong Zhang, Jared Kuemmerle |
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| Rok vydání: | 2009 |
| Předmět: |
Stereochemistry
Chemistry Pharmaceutical Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Antineoplastic Agents Apoptosis Primary alcohol Biochemistry Chemical synthesis Mice Structure-Activity Relationship chemistry.chemical_compound In vivo Cell Line Tumor Furan Drug Discovery Animals Combinatorial Chemistry Techniques Humans Hydroxymethyl Infusions Intravenous Cytotoxicity Molecular Biology Oxadiazoles Molecular Structure Aryl Organic Chemistry Water In vitro Models Chemical Solubility chemistry Drug Design Molecular Medicine Neoplasm Transplantation |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 19:4410-4415 |
| ISSN: | 0960-894X |
| Popis: | As a continuation of our efforts to discover and develop the 3-aryl-5-aryl-1,2,4-oxadiazole series of apoptosis inducers as potential anticancer agents, we explored substitutions at the 2- and 3-positions of the 3-aryl group to improve the aqueous solubility properties and identify development candidates. A small substitution such as methyl or hydroxymethyl at the 2-position was well tolerated. This modification, in combination with a 3-substituted furan ring as the 5-aryl group, resulted in 4g and 4h, which have improved solubility properties. Compound 4g was found to have good in vivo efficacy in animal studies via intravenous administration. |
| Databáze: | OpenAIRE |
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