2. Academic Validation
  3. Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells

Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells

  • Bioorg Med Chem Lett. 2017 Nov 15;27(22):5040-5045. doi: 10.1016/j.bmcl.2017.09.060.
Mohammad Imran Ahmad 1,  Shivani Dixit 2,  Rituraj Konwar 2,  Prema G Vasdev 3,  Akhilesh Kumar Yadav 4,  Shubhandra Tripathi 5,  Madan Mohan Gupta 4,  Ashok Sharma 5,  Atul Gupta 6
Affiliations

Affiliations

  • 1 Medicinal Chemistry Department, CSIR-Central Institute of Medicinal and Aromatic Plants, PO CIMAP, Kukrail Road, Lucknow 226015, India.
  • 2 Division of Endocrinology, CSIR-Central Drug Research Institute, Sector-10, Jankipuram Extension, Lucknow 226031, India.
  • 3 Metabolic and Structural Biology Department, CSIR-Central Institute of Medicinal and aromatic Plants, PO CIMAP, Kukrail Road, Lucknow 226015, India.
  • 4 Analytical Chemistry Department, CSIR-Central Institute of Medicinal and aromatic Plants, PO CIMAP, Kukrail Road, Lucknow 226015, India.
  • 5 Biotechnology Department, CSIR-Central Institute of Medicinal and aromatic Plants, PO CIMAP, Kukrail Road, Lucknow 226015, India.
  • 6 Medicinal Chemistry Department, CSIR-Central Institute of Medicinal and Aromatic Plants, PO CIMAP, Kukrail Road, Lucknow 226015, India. Electronic address: atisky2001@yahoo.co.in.
PMID: 29054359 DOI: 10.1016/j.bmcl.2017.09.060
Abstract

A series of conformationally restricted benzopyran based triarylethylenes has been synthesized and characterized as potential growth inhibitors of breast carcinoma cells. The synthesized compounds (14a-b, 15a and 16a-e) presented significant growth inhibition of ER+ and ER- breast Cancer cells within the range of IC50 0.55-9.96µM. Amongst Other, 16c showed potent Anticancer activity at IC50 0.95µM in MCF-7 cells with good selectivity (Selectivity Index 4.47) towards healthy cells. The mechanistic studies for 16c were performed to elucidate possible mode of action which showed 16c elicited Anticancer activity through Necroptosis process.

Keywords

Anticancer; Benzopyran; Chromanone; Estrogen; Triarylethylene.

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