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Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Jun2016, Vol. 26 Issue 11, p2713-2718. 6p. - Publication Year :
- 2016
-
Abstract
- p53-independent malignant cancer is still severe health problem of human beings. HIF-1 pathway is believed to play an important role in the survival and developing progress of such cancers. In the present study, with the aim to inhibit the proliferation of p53-independent malignant cells, we disclose the optimization of 6a , the starting compound which is discovered in the screening of in-house compound collection. The structure–activity relationship (SAR) is summarized. The most potent derivative 8d , inhibits the proliferation of both p53-null and p53-mutated cells through inhibition of HIF-1 pathway. Our findings here provide a new chemotype in designing potent anticancer agent especially against those p53-independent malignant tumors. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 26
- Issue :
- 11
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 114991013
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.03.112