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AuthorMalki, Ahmed
AuthorLaha, Rumita
AuthorBergmeier, Stephen C.
Available date2016-03-30T08:22:56Z
Publication Date2014-02
Publication NameBioorganic and Medicinal Chemistry Letters
ResourceScopus
Identifierhttp://dx.doi.org/10.1016/j.bmcl.2013.12.103
CitationMalki, A., Laha, R., Bergmeier, S.C. "Synthesis and cytotoxic activity of MOM-ether analogs of isosteviol" (2014) Bioorganic and Medicinal Chemistry Letters, 24 (4), pp. 1184-1187.
ISSN0960-894X
URIhttp://hdl.handle.net/10576/4282
AbstractLung cancer is one of the most common malignancies worldwide. In this Letter, novel MOM-ether analogs of isosteviol were designed and synthesized to be tested for anticancer activities against H1299 lung cancer cell lines. The effects of these derivatives were studied in H1299 human large cell lung carcinoma cells that are null for p53 and compared to normal counterparts NL-20 normal lung epithelial cells. The initial screening of twelve MOM-ether analogs of isosteviol derivatives on H1299 lung cancer cells by MTT assay revealed that two derivatives (an ester and a carbamate) were the most potent in reducing cell viability. The IC50 values for these derivatives were determined to be 14 and 21 ?M respectively. We compared the cytotoxicity of the best derivatives in H1299 lung cancer cells and NL-20 normal lung epithelial cells. Both derivatives showed lower cytotoxic effects on NL-20 normal lung epithelial cells. Moreover, both derivatives induced apoptosis in H1299 lung cancer cells more than NL-20 normal lung epithelial cells.
SponsorU.S.-Egypt Joint Board on Scientific and Technological Cooperation and Science and Technology Development Fund (STDF) grant ID 3684
Languageen
PublisherElsevier Ltd.
SubjectAnticancer
Diterpene
Isosteviol
Lung cancer
Antineoplastic Agents
Cell Line, Tumor
Cell Proliferation
Cell Survival
Diterpenes, Kaurane
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Ethers
Humans
Molecular Conformation
Structure-Activity Relationship
TitleSynthesis and cytotoxic activity of MOM-ether analogs of isosteviol
TypeArticle
Pagination1184-1187
Issue Number4
Volume Number24


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