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  3. Development of constrained tamoxifen mimics and their antiproliferative properties against breast cancer cells

Development of constrained tamoxifen mimics and their antiproliferative properties against breast cancer cells

  • Bioorg Med Chem Lett. 2015 Feb 1;25(3):680-4. doi: 10.1016/j.bmcl.2014.11.077.
Sivakumar Archana 1,  Ramasatyaveni Geesala 2,  Narasimha B Rao 1,  Suresh Satpati 3,  Giridhar Puroshottam 4,  Akhila Panasa 4,  Anshuman Dixit 3,  Amitava Das 2,  Ajay Kumar Srivastava 5
Affiliations

Affiliations

  • 1 Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India.
  • 2 Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India; Academy for Scientific Innovation and Research, New Delhi 110001, India.
  • 3 Institute of Life Sciences, Bhubaneswar 751023, India.
  • 4 Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India.
  • 5 Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India; Academy for Scientific Innovation and Research, New Delhi 110001, India. Electronic address: aksrivastava@iict.res.in.
PMID: 25529734 DOI: 10.1016/j.bmcl.2014.11.077
Abstract

An efficient synthesis of a new series of tamoxifen mimics is described by employing iodine catalyzed ipsocyclization strategy followed by Suzuki coupling. A molecular docking studies of the synthesized compounds 11a-n and 12 in Estrogen Receptor (ER-α) showed that the scaffolds are fitting well in the groove, thereby suggesting them as promising antiproliferative agents for estrogen dependent breast Cancer lines. All compounds were tested in vitro against breast Cancer cell lines-ER positive, MCF-7; ER negative, MDA-MB-231; and control mammary epithelial cells, MEpiC. The biological results showed that most of the compounds are active against MCF-7 with IC50 values less than 6.5μM which corroborate the results of molecular docking studies.

Keywords

Breast cancer; Ipsocyclization; Molecular docking; SERMs; Tamoxifen.

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