Design, synthesis and anti-proliferative activities of novel 7 '-O-substituted schisantherin A derivatives
- Authors
- Venkanna, A.; Kumar, Ch. Pavan; Poornima, B.; Siva, Bandi; Jain, Nishant; Babu, K. Suresh
- Issue Date
- 2016
- Publisher
- ROYAL SOC CHEMISTRY
- Citation
- MEDCHEMCOMM, v.7, no.6, pp.1159 - 1170
- Journal Title
- MEDCHEMCOMM
- Volume
- 7
- Number
- 6
- Start Page
- 1159
- End Page
- 1170
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/9730
- DOI
- 10.1039/c6md00097e
- ISSN
- 2040-2503
- Abstract
- A series of schisantherin A (1) derivatives were efficiently synthesized utilizing Yamaguchi esterification (2,4,6-trichlorobenzoyl chloride, Et3N, THF, DMAP, toluene) at the C-7'position of the schisantherin A core. The synthesized derivatives were evaluated for their anti-cancer activities against SIHA, PANC 1, MDA-MB-231, IMR-32, DU-145 and A549 cancer cell lines using sulforhodamine B assay. Within the new series tested, compound 29 displayed the most promising cytotoxic effect against the human cervical cancer cell line (SIHA) with a GI(50) value of < 0.01 mu M, which is comparable to that of the standard drug, doxorubicin. Mechanism of action studies validated that 29 functions as a microtubule inhibitor. Additionally, several of the other analogues exhibited potent activity against the tested cell lines. Based on the results obtained, structure-activity relationships (SARs) were established and a correlation between the activities was also observed and discussed.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - ETC > 1. Journal Articles
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.