2. Academic Validation
  3. Novel benzothiazine-piperazine derivatives by peptide-coupling as potential anti-proliferative agents

Novel benzothiazine-piperazine derivatives by peptide-coupling as potential anti-proliferative agents

  • Bioorg Med Chem Lett. 2017 Jan 15;27(2):354-359. doi: 10.1016/j.bmcl.2016.10.071.
Ramineni Venkatesh 1,  Suresh Kasaboina 1,  Deepthi Bidayat 1,  U Nikhil Kumar 1,  Nishant Jain 2,  Saritha Jostna Tangeda 3,  Rajashaker Bantu 1,  Sridhara Janardhan 4,  Lingaiah Nagarapu 5
Affiliations

Affiliations

  • 1 Organic Chemistry Division-II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 2 Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 3 Medicinal Chemistry Division, S. N. V. Pharmacy Maha Vidyalay, Tarnaka, Hyderabad 500017, India.
  • 4 Centre for Molecular Modeling, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 5 Organic Chemistry Division-II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India. Electronic address: lnagarapuiict@yahoo.com.
PMID: 27964883 DOI: 10.1016/j.bmcl.2016.10.071
Abstract

In an attempt to develop potential and selective anti-proliferative agents, a series of novel benzothiazine-piperazine derivatives 8a-i and 10a-g were synthesized by coupling of 2H-1,4-benzothiazin-3(4H)-one with various amines 7a-i and 9a-g in excellent yields and evaluated for their in vitro anti-proliferative activity against four Cancer cell lines, HeLa (cervical), MIAPACA (pancreatic), MDA-MB-231 (breast) and IMR32 (neuroblastoma). In vitro inhibitory activity indicated that compounds 8a, 8d, 8g, 10a, 10b, 10e, 10f were found to be good anti-proliferative agents. Among them the derivatives 8g, 10e and 10f were found to be the most active members exhibiting remarkable growth inhibitory activity. Molecular docking was undertaken to investigate the probable binding mode and key active site interactions in HDAC8 and EHMT2 proteins. The docking results are complementary to the experimental results.

Keywords

Anti-proliferative activity; Benzothiazine-piperazine; EHMT2; HDAC8; Molecular docking; Peptide-coupling.

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