Kaur G., Mahajan M.P., Pandey M.K., Singh P., Ramisetti S.R., Sharma A.K.
School of Pharmaceutical Sciences, Apeejay Stya University, Institutional Area, Gurgaon 122001, India; Apeejay Stya Research Foundation, Institutional Area, Gurgaon 122001, India; Department of Pharmacology, Penn State Hershey Cancer Institute, CH72 Penn State College of Medicine, 500 University Drive, Hershey, PA 17033, United States; School of Chemistry and Physics, University of Kwa-Zulu Natal (UKZN), Westville Campus, Durban 4000, South Africa
Kaur, G., School of Pharmaceutical Sciences, Apeejay Stya University, Institutional Area, Gurgaon 122001, India; Mahajan, M.P., School of Pharmaceutical Sciences, Apeejay Stya University, Institutional Area, Gurgaon 122001, India, Apeejay Stya Research Foundation, Institutional Area, Gurgaon 122001, India; Pandey, M.K., Department of Pharmacology, Penn State Hershey Cancer Institute, CH72 Penn State College of Medicine, 500 University Drive, Hershey, PA 17033, United States; Singh, P., School of Chemistry and Physics, University of Kwa-Zulu Natal (UKZN), Westville Campus, Durban 4000, South Africa; Ramisetti, S.R., Department of Pharmacology, Penn State Hershey Cancer Institute, CH72 Penn State College of Medicine, 500 University Drive, Hershey, PA 17033, United States; Sharma, A.K., Department of Pharmacology, Penn State Hershey Cancer Institute, CH72 Penn State College of Medicine, 500 University Drive, Hershey, PA 17033, United States
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. © 2014 Elsevier Masson SAS. All rights reserved.
2 [ 4 ( 4 amino 1,2 diphenylbut 1 enyl)phenoxy]ethanol; 2 [ 4 ( 4 azido 1,2 diphenylbut 1 enyl)phenoxy]ethanol; 4 [ 4 ( 2 aminoethoxy)phenyl] 3,4 diphenylbut 3 en 1 amine; antineoplastic agent; estrogen receptor; estrogen receptor alpha; estrogen receptor beta; hormone receptor stimulating agent; ospemifene; ospemifene derivative; phenyl 4 [ 4 ( 2 hydroxyethoxy)phenyl] 3,4 diphenylbut 3 enylcarbamic acid; selective estrogen receptor modulator; tamoxifen; unclassified drug; 2 [4 (4 amino1,2 diphenylbut 1 enyl) phenoxy]ethanol; 2 [4 (4 azido 1,2 diphenylbut 1 enyl)phenoxy]ethanol; 2 [4 (4 chloro 1,2 diphenylbut 1 enyl) phenoxy]ethanol; 2 [4 (4 chloro 1,2 diphenylbut 1 enyl)phenoxy]ethyl methanesulfonate; 4 [4 (2 aminoethoxy)phenyl] 3,4 diphenylbut 3 en 1 amine; antineoplastic agent; ospemifene; ospemifene derivative; phenyl 4 [4 (2 hydroxyethoxy)phenyl] 3,4 diphenylbut 3 enylcarbamate; selective estrogen receptor modulator; tamoxifen; [1 [4 (2 azidoethoxy) phenyl] 4 chlorobut 1 ene 1,2 diyl]dibenzene; [4 azido 1 [4 (2 azidoethoxy)phenyl]but 1 ene 1,2 diyl]dibenzene; antineoplastic agent; ospemifene; antineoplastic activity; article; binding affinity; breast cancer cell line; cell viability; controlled study; cytotoxicity; drug design; drug potency; drug protein binding; drug synthesis; growth inhibition; human; human cell; IC 50; MCF 7 cell line; molecular docking; animal cell; antineoplastic activity; Article; breast cancer; cancer inhibition; concentration response; drug cytotoxicity; drug screening; drug selectivity; embryo; IC50; mouse; nonhuman; analogs and derivatives; Breast Neoplasms; cell proliferation; cell survival; chemical structure; chemistry; dose response; drug effects; drug screening; pathology; structure activity relation; synthesis; tumor cell culture; Antineoplastic Agents; Breast Neoplasms; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Humans; MCF-7 Cells; Models, Molecular; Molecular Structure; Structure-Activity Relationship; Tamoxifen; Tumor Cells, Cultured