Programs
- M. Tech. in Automotive Engineering -
- Fellowship In Interventional Pulmonology and Pulmonary Critical care - Fellowship
Publication Type : Journal Article
Publisher : Bioorganic & Medicinal Chemistry Letters
Source : Bioorganic & Medicinal Chemistry Letters, Volume 26, Number 13, p.3024-3028 (2016)
Url : https://www.sciencedirect.com/science/article/pii/S0960894X16305054
Keywords : Cell cycle analysis, cytotoxicity, Indole, Indolyl-pyrimidine, Knoevenagel, Oxindole
Campus : Kochi
School : School of Pharmacy
Department : Pharmacology
Verified : Yes
Year : 2016
Abstract : In our endeavor towards the development of effective cytotoxic agents, a series of oxindole linked indolyl-pyrimidine derivatives were synthesized and characterized by IR, 1H NMR, 13C NMR and Mass spectral analysis. All the newly synthesized target compounds were assessed against PA-1 (ovarian), U-87MG (glioblastoma), LnCaP (prostate), and MCF-7 (Breast) cancer cell lines for their cytotoxic potential, with majority of them showing inhibitory activity at low micro-molar concentrations. Significantly, compound 8e was found to be most potent amongst all the tested compounds with an IC50 value of (2.43±0.29μM) on PA-1 cells. The influence of the most active cytotoxic compound 8e on the cell cycle distribution was assessed on the PA-1 cell line, exhibiting a cell cycle arrest at the G2/M phase. Moreover, acridine orange/ethidium bromide staining and annexin V binding assay confirmed that compound 8e can induce cell apoptosis in PA-1 cells. These preliminary results persuade further investigation on the synthesized compounds aiming to the development of potential cytotoxic agents.
Cite this Research Publication : S. Kumar Prajapti, Nagarsenkar, A., Guggilapu, S. Devi, Gupta, K. Kumar, Allakonda, L., Dr. Manish Kumar Jeengar, V.G.M. Naidu, and Babu, B. Nagendra, “Synthesis and Biological Evaluation of Oxindole linked indolyl-pyrimidine Derivatives as Potential Cytotoxic Agents”, Bioorganic & Medicinal Chemistry Letters, vol. 26, pp. 3024-3028, 2016.