Synthesis of novel nicotinohydrazide and (1,3,4-oxadiazol-2-yl)-6-(trifluoromethyl)pyridine derivatives as potential anticancer agents

  • Bioorg Med Chem Lett. 2016 Oct 1;26(19):4829-4831. doi: 10.1016/j.bmcl.2016.08.020.
R Naresh Kumar  1 ,  Y Poornachandra  2 ,  P Nagender  1 ,  G Santhosh Kumar  3 ,  D Krishna Swaroop  1 ,  C Ganesh Kumar  2 ,  B Narsaiah  4
Affiliations
  • 1. Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India; Academy of Scientific and Innovative Research, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 2. Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India; Academy of Scientific and Innovative Research, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 3. Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 4. Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India; Academy of Scientific and Innovative Research, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India. Electronic address: [email protected].
PMID: 27561719 DOI: 10.1016/j.bmcl.2016.08.020
Abstract

A series of novel nicotinohydrazide derivatives 6a-g and 1,3,4-oxadiazole functionalized pyridine derivatives 7a-k and 8a-d were prepared in series of steps. All the compounds were screened for cytotoxicity against HeLa (cervical), DU145 (prostate), HepG2 (liver) and MBA-MB-231 (breast) human Cancer cell lines. Compounds 6h, 6i, 7d, 7h, 7i and 8b which showed promising cytotoxicity at <15μM concentration have been identified. Further optimization of the structure is underway to identify a lead compound.

Keywords
1,3,4-Oxadiazole; Anticancer agents; Cyclization; Human cancer cell lines; Nicotinohydrazide.