2. Academic Validation
  3. Design, synthesis and docking studies of novel 1,2-dihydro-4-hydroxy-2-oxoquinoline-3-carboxamide derivatives as a potential anti-proliferative agents

Design, synthesis and docking studies of novel 1,2-dihydro-4-hydroxy-2-oxoquinoline-3-carboxamide derivatives as a potential anti-proliferative agents

  • Eur J Med Chem. 2017 Jan 5:125:400-410. doi: 10.1016/j.ejmech.2016.09.062.
Saleha Banu 1,  Rajitha Bollu 1,  Rajashaker Bantu 1,  Lingaiah Nagarapu 1,  Sowjanya Polepalli 2,  Nishant Jain 2,  Radhika Vangala 3,  Vijjulatha Manga 3
Affiliations

Affiliations

  • 1 Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad, 500007, India.
  • 2 Center for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad, 500007, India.
  • 3 Molecular Modeling and Medicinal Chemistry Group, Department of Chemistry, Osmania University, Tarnaka, Hyderabad, 500007, India.
PMID: 27688193 DOI: 10.1016/j.ejmech.2016.09.062
Abstract

A new series of 4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide hybrids 8a-l have been designed and synthesized using peptide coupling agents with substituted N-phenyl piperazines and piperidines with good to excellent yields. The synthesized compounds were evaluated for their in vitro anti-proliferative activity against PANC 1, HeLa and MDA-MB-231. The compounds 8d, 8e, 8f, 8g, 8h and 8k exhibited considerable anti-proliferative activity with GI50 values ranging from 0.15 to 1.4 μM. The structure and anti-proliferative activity relationship was further supported by in silico molecular docking study of the active compounds against tubulin protein.

Keywords

1,2-dihydro-4-hydroxy-2-oxoquinoline-3-carboxamides; Anti-proliferative; Cell lines and molecular modeling; Multiple sclerosis; Piperazines; Roquinimex.

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