2. Academic Validation
  3. Design, synthesis and anticancer activity of N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives

Design, synthesis and anticancer activity of N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives

  • Bioorg Med Chem Lett. 2017 Sep 1;27(17):4140-4145. doi: 10.1016/j.bmcl.2017.07.029.
Mura Reddy Gudisela 1,  N Srinivasu 1,  Chaitanya Mulakayala 2,  Praveen Bommu 3,  M V Basaveswara Rao 4,  Naveen Mulakayala 5
Affiliations

Affiliations

  • 1 Department of Chemistry, VFSTR, Vadlamudi, Guntur 522213, India.
  • 2 Department of Biosciences, Sri Satya Sai Institute of Higher Learning, Anantapuram 515001, India.
  • 3 PS3 Laboratories LLC, Hyderabad 500072, India.
  • 4 Department of Chemistry, Krishna University, Machilipatnam 521 00, India.
  • 5 Clearsynth Labs Ltd, IDA Mallapur, Nacharam, Hyderabad 500076, India. Electronic address: naveen071280@gmail.com.
PMID: 28756024 DOI: 10.1016/j.bmcl.2017.07.029
Abstract

Novel N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives were designed, synthesized and their chemical structures were confirmed by 1H NMR, 13C NMR and Mass spectra. The Anticancer activities of the newly synthesized compounds were evaluated in vitro against three human Cancer cell lines including K562, Colo-205 and MDA-MB 231 by MTT assay. The screening results showed that five compounds (16b, 16d, 16i, 16p and 16q) exhibited potent cytotoxic activities with IC50 values between 20 and 40μM. Further in vitro studies revealed that inhibition of sirtuins could be the possible mechanism of action of these molecules.

Keywords

Anticancer activity; Dibenzo[b,f][1,4]thiazepin; Sirtuins; Sunitinib; Synthesis.

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