Synthesis of phenstatin/isocombretastatin-chalcone conjugates as potent tubulin polymerization inhibitors and mitochondrial apoptotic inducers.

@article{Kamal2015SynthesisOP,
  title={Synthesis of phenstatin/isocombretastatin-chalcone conjugates as potent tubulin polymerization inhibitors and mitochondrial apoptotic inducers.},
  author={Ahmed Kamal and Gajjela Bharath Kumar and M. Vishnuvardhan and Anver Basha Shaik and Vangala Santhosh Reddy and Rasala Mahesh and Ibrahim Bin Sayeeda and Jeevak Sopanrao Kapure},
  journal={Organic \& biomolecular chemistry},
  year={2015},
  volume={13 13},
  pages={
          3963-81
        }
}
A series of phenstatin/isocombretastatin–chalcones were synthesized and screened for their cytotoxic activity against various human cancer cell lines. Some representative compounds exhibited significant antiproliferative activity against a panel of sixty human cancer cell lines of the NCI, with GI50 values in the range of 0.11 to 19.0 μM. Three compounds (3b, 3c and 3e) showed a broad spectrum of antiproliferative efficacy on most of the cell lines in the sub-micromolar range. In addition, all… 
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TLDR
A series of pyrazoline derivatives and corresponding chalcone intermediates with substituents same as combretastatin‐A4(CA‐4) conjugated with triazole nucleus has been synthesized and evaluated for their anticancer potential, indicating their ability to trigger apoptosis.
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