Synthesis and anticancer activity of novel 2-substituted pyranopyridine derivatives

Abstract

A novel series of 2-aminopyranopyridine derivatives (3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19) were synthesized utilizing 2-chloro-4-(thiophen-2-yl)-7,8-dihydro-5H-pyrano[4,3-b]pyridine-3-carbonitrile (2) as a key starting compound. The structures of the newly synthesized compounds were confirmed on the basis of elemental analyses and infrared (IR), 1 H, 13 C-nuclear magnetic resonance (NMR) and mass spectra. Anticancer evaluation was carried out for the new derivatives against Hep-G2 (human liver carcinoma), MCF-7 (human breast carcinoma), Caco-2 (human colorectal adenocarcinoma) and HCT116 (human colorectal carcinoma) cell lines using doxorubicin as a reference drug. The biological results revealed that the compounds 12 and 14 exhibited more potent anticancer activity than the reference drug.

Electrical properties, cyclic voltammetry, and anticancer activities of N‐(4‐(2‐hydrazinyl‐2‐oxoethoxy)phenyl) acetamide complexes

“…The cytotoxicities of the prepared compounds against the MCF‐7 cell line was estimated using the 3‐[4,5‐dimethyl‐2‐thiazolyl)‐2,5‐diphenyl‐2H‐tetrazolium bromide (MTT) assay, which is based on the cleavage of the tetrazolium salt by mitochondrial dehydrogenases in viable cells . The cells were transferred to a 96‐well sterile microplate (5 × 10 4 cells/well) and incubated at 37°C with DMSO solutions of the test compounds or doxorubicin (positive control) for 48 hours in serum‐free medium prior to the MTT assay.…”

Synthesis and in vitro evaluation of novel tetralin‐pyrazolo[3,4‐b]pyridine hybrids as potential anticancer agents

“…The anticancer activities on HCT116 (colorectal carcinoma) and MCF‐7 (human breast adenocarcinoma) human cell lines were assessed using the 3‐[4,5‐dimethyl‐2‐thiazolyl)‐2,5‐diphenyl‐2 H ‐tetrazolium bromide (MTT) assay . These cancer cell lines were purchased from ATCC (Rockville, MD, USA).…”

Synthesis, In Vitro Cytotoxicity and Bleomycin‐Dependent DNA Damage Evaluation of Some Heterocyclic‐Fused Pyrimidinone Derivatives

“…The cytotoxic effect of the designed compounds have been assessed in vitro at the National Institute of Cancer, Cairo, Egypt against human liver hepatocellular carcinoma (HepG2) and normal lung fibroblasts (WI‐38) cell lines via the MTT colorimetric technique, using doxorubicin as a reference standard for comparison. As for activity against HepG2 cells, the investigated compounds 1 a‐12 b exhibited variable degrees of inhibitory activity ranging from potent to weak impacts compared to the results acquired by doxorubicin (Table , Figure ).…”