2. Academic Validation
  3. Synthesis and evaluation of benzosuberone embedded with 1,3,4-oxadiazole, 1,3,4-thiadiazole and 1,2,4-triazole moieties as new potential anti proliferative agents

Synthesis and evaluation of benzosuberone embedded with 1,3,4-oxadiazole, 1,3,4-thiadiazole and 1,2,4-triazole moieties as new potential anti proliferative agents

  • Bioorg Med Chem Lett. 2015;25(10):2220-4. doi: 10.1016/j.bmcl.2015.03.032.
Bandi Yadagiri 1,  Srikanth Gurrala 1,  Rajashaker Bantu 1,  Lingaiah Nagarapu 2,  Sowjanya Polepalli 3,  Garimella Srujana 3,  Nishant 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: 25827522 DOI: 10.1016/j.bmcl.2015.03.032
Abstract

As an aspect of our ongoing research in search of new anti proliferative agents, a series of novel analogs of benzosuberone embedded with 1,3,4-oxadiazole, 1,3,4-thiadiazole and 1,2,4-triazole moieties were synthesized in excellent yields (82-93%). All the newly synthesized compounds were characterized by (1)H NMR, (13)C NMR, ESI/LC-MS, HRMS and evaluated for their in vitro anti proliferative activity against four human Cancer cell lines (cervical, breast, pancreatic and alveolar). Among the synthesized compounds, 4b, 6a, 7d and 7l showed potent anti proliferative activity with GI50 values range of 0.079-0.957μM against four human Cancer cell lines. However, it was revealed that the compound 7d have shown very close GI50 value 0.079μM as compared with positive control of colchicine against cervical Cancer cell line.

Keywords

1,2,4-Triazole; 1,3,4-Oxadiazole; 1,3,4-Thiadiazole; Anti-proliferative; Benzosuberone; Cell lines.

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