TY - JOUR
T1 - Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents
AU - Kaur, Gurleen
AU - Mahajan, Mohinder P.
AU - Pandey, Manoj K.
AU - Singh, Parvesh
AU - Ramisetti, Srinivasa R.
AU - Sharma, Arun K.
N1 - Funding Information:
Gurleen Kaur is grateful to Department of Science & Technology (DST), New Delhi, India for financial assistance under Inspire Program and Parvesh Singh acknowledges the Centre for High Performance Computing, an initiative supported by the Department of Science and Technology, Republic of South Africa . The investigations were supported, in part, by the Department of Pharmacology, Penn State College of Medicine .
PY - 2014/10/30
Y1 - 2014/10/30
N2 - The synthesis of some novel Ospemifene derived analogs and their evaluation as anti-breast cancer agents against MCF-7 (ER-positive) and MDA-MB-231 (ER-negative) human breast cancer cell lines are described. Few of these analogs for instance, compounds 6, 7 and 8 are shown to be more effective than recent Selective Estrogen Receptor Modulators (SERMs) i.e. Ospemifene and Tamoxifen, against these cell lines. Compound 8 was relatively more cytotoxic to MCF-7 cells similar to Ospemifene and Tamoxifen, while most potent compounds 6 and 7 were equally effective in inhibiting growth of both ER-positive and ER-negative cell lines. The observed activity profiles were further supported by the docking studies performed against estrogen receptors (ERα and ERβ). Compounds 6, 7 and 8 exhibited stronger binding affinities with both ERα and ERβ compared to Ospemifene and Tamoxifen.
AB - The synthesis of some novel Ospemifene derived analogs and their evaluation as anti-breast cancer agents against MCF-7 (ER-positive) and MDA-MB-231 (ER-negative) human breast cancer cell lines are described. Few of these analogs for instance, compounds 6, 7 and 8 are shown to be more effective than recent Selective Estrogen Receptor Modulators (SERMs) i.e. Ospemifene and Tamoxifen, against these cell lines. Compound 8 was relatively more cytotoxic to MCF-7 cells similar to Ospemifene and Tamoxifen, while most potent compounds 6 and 7 were equally effective in inhibiting growth of both ER-positive and ER-negative cell lines. The observed activity profiles were further supported by the docking studies performed against estrogen receptors (ERα and ERβ). Compounds 6, 7 and 8 exhibited stronger binding affinities with both ERα and ERβ compared to Ospemifene and Tamoxifen.
UR - http://www.scopus.com/inward/record.url?scp=84906538667&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84906538667&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2014.08.050
DO - 10.1016/j.ejmech.2014.08.050
M3 - Article
C2 - 25164760
AN - SCOPUS:84906538667
SN - 0223-5234
VL - 86
SP - 211
EP - 218
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -