2. Academic Validation
  3. Rational design, synthesis and anti-proliferative evaluation of novel benzosuberone tethered with hydrazide-hydrazones

Rational design, synthesis and anti-proliferative evaluation of novel benzosuberone tethered with hydrazide-hydrazones

  • Bioorg Med Chem Lett. 2014 Nov 1;24(21):5041-4. doi: 10.1016/j.bmcl.2014.09.018.
Bandi Yadagiri 1,  Uma Devi Holagunda 1,  Rajashaker Bantu 1,  Lingaiah Nagarapu 2,  Vijayacharan Guguloth 1,  Sowjanya Polepally 3,  Nishanth Jain 3
Affiliations

Affiliations

  • 1 Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 2 Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India. Electronic address: lnagarapuiict@yahoo.com.
  • 3 Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
PMID: 25264072 DOI: 10.1016/j.bmcl.2014.09.018
Abstract

Two different series of novel analogues of benzosuberones (5a-m and 9a-w) tethered with hydrazone-hydrazides (functional group alterations: Head group to Tail group and vice versa) have been synthesized by the reaction of appropriate aldehydes with substituted hydrazides in excellent yields (87-94%) and their structures were confirmed by (1)H NMR, (13)C NMR, ESI-MS and HRMS. The newly synthesized compounds were evaluated for anti-proliferative activity against different human Cancer cell lines (HeLa, MDA MB 231, MIAPACA and IMR32). Among the synthesized compounds, six compounds 5 a, 5 b, 5 d, 5 e, 5 f and 9 v exhibited potent anti-proliferative activity with GI50 values less than 0.01 μM against MIAPACA, MDA-MB-231 and IMR32 human Cancer cell lines.

Keywords

Anti-proliferative; Benzosuberone; Cell lines; Hydrazide–hydrazones.

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