2. Academic Validation
  3. Synthesis and anticancer evaluation of novel triazole linked N-(pyrimidin-2-yl)benzo[d]thiazol-2-amine derivatives as inhibitors of cell survival proteins and inducers of apoptosis in MCF-7 breast cancer cells

Synthesis and anticancer evaluation of novel triazole linked N-(pyrimidin-2-yl)benzo[d]thiazol-2-amine derivatives as inhibitors of cell survival proteins and inducers of apoptosis in MCF-7 breast cancer cells

  • Bioorg Med Chem Lett. 2015 Feb 1;25(3):654-8. doi: 10.1016/j.bmcl.2014.11.083.
Ravindra M Kumbhare 1,  Tulshiram L Dadmal 2,  M Janaki Ramaiah 3,  K S V Kishore 2,  S N C V L Pushpa Valli 4,  Sudheer Kumar Tiwari 4,  K Appalanaidu 2,  Y Khageswar Rao 2,  Manika Pal Bhadra 5
Affiliations

Affiliations

  • 1 Fluoroorganics Division, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500607, India. Electronic address: kumbhare@iict.res.in.
  • 2 Fluoroorganics Division, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500607, India.
  • 3 School of Chemical and Biotechnology, SASTRA University, Tirumalaisamudram, Thanjavur 613401, Tamil Nadu, India.
  • 4 Chemical Biology Laboratory, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500607, India.
  • 5 Chemical Biology Laboratory, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500607, India. Electronic address: manika@iict.res.in.
PMID: 25563891 DOI: 10.1016/j.bmcl.2014.11.083
Abstract

A series of novel triazole linked N-(pyrimidin-2yl)benzo[d]thiazol-2-amine 5a-k were synthesized and evaluated for Anticancer activity against breast (MCF-7), lung (A549) and skin (A375) Cancer cell lines and their cytotoxic effects were compared against normal breast epithelial cells. The effect of compounds on cell cycle of MCF-7 breast Cancer cell line was investigated by FACS. Result indicated G2/M cell cycle arrest of MCF-7 cells. Further promising compounds 5b, 5g, 5h and 5i were tested for their Apoptosis inducing ability as well as inhibitory activity against key proteins NF-kB, Survivin, CYP1A1, and ERK1/2 which help in Cancer cell survival and proliferation. The apoptotic aspect of these compounds is further evidenced by increase in the activity of caspase-9 in MCF-7 cells. Hence these small molecules have the potential to control both the cell proliferation as well as the invasion process in highly malignant breast cancers and can be selected for further biological studies.

Keywords

Breast cancer cells; Cytotoxicity; N-(Pyrimidin-2yl)benzo[d]thiazol-2-amine; Sharpless conditions; Triazole.

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