Synthesis and antitumor activity of 1,3,4-oxadiazole substituted 2-(5-ylidene-2,4-dioxothiazolidin-3-yl)-acetamides

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Abstract

A series of novel 1,3,4-oxadiazole substituted 2-(5-aryl/heterylidene-2,4-dioxothiazolidine-3-ylidene)-acetamides and their 5-unsubstituted analogues have been synthesized following N-alkylation reaction of 2-chloro-N-(5-aryl-[1,3,4]oxadiazol-2-yl)-acetamides with thiazolidinedione and potassium salts of its arylidene derivatives. The structures of target compounds were confirmed by using 1H NMR spectroscopy and elemental analysis. Evaluation of anticancer activity in vitro for the synthesized compounds was performed in accordance with the National Cancer Institute protocol. A selective influence of some tested compounds against leukaemia MOLT-4 (3e, GP = 76.85%) and K-562 (3e, GP = 79.84%), colon cancer HCT-15 (3d, GP = 76.86%), renal cancer A498 (4a, GP = 74.37%), CAKI-1 (3d, GP = 68.49%) and UO-31 (3b-e, 4a-b, GP = 66.67 ÷ 86.30%) cell lines was established. Grafical abstract:

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The NCI60 human tumour cell line anticancer drug screen.

Robert Shoemaker (2006)

The US National Cancer Institute (NCI) 60 human tumour cell line anticancer drug screen (NCI60) was developed in the late 1980s as an in vitro drug-discovery tool intended to supplant the use of transplantable animal tumours in anticancer drug screening. This screening model was rapidly recognized as a rich source of information about the mechanisms of growth inhibition and tumour-cell kill. Recently, its role has changed to that of a service screen supporting the cancer research community. Here I review the development, use and productivity of the screen, highlighting several outcomes that have contributed to advances in cancer chemotherapy.

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Feasibility of a high-flux anticancer drug screen using a diverse panel of cultured human tumor cell lines.

A. Monks, D Scudiero, P Skehan … (1991)

We describe here the development and implementation of a pilot-scale, in vitro, anticancer drug screen utilizing a panel of 60 human tumor cell lines organized into subpanels representing leukemia, melanoma, and cancers of the lung, colon, kidney, ovary, and central nervous system. The ultimate goal of this disease-oriented screen is to facilitate the discovery of new compounds with potential cell line-specific and/or subpanel-specific antitumor activity. In the current screening protocol, each cell line is inoculated onto microtiter plates, then preincubated for 24-28 hours. Subsequently, test agents are added in five 10-fold dilutions and the culture is incubated for an additional 48 hours. For each test agent, a dose-response profile is generated. End-point determinations of the cell viability or cell growth are performed by in situ fixation of cells, followed by staining with a protein-binding dye, sulforhodamine B (SRB). The SRB binds to the basic amino acids of cellular macromolecules; the solubilized stain is measured spectrophotometrically to determine relative cell growth or viability in treated and untreated cells. Following the pilot screening studies, a screening rate of 400 compounds per week has been consistently achieved.