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: narsaiah@iict.res.in.

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.

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