Design, Synthesis, and Evaluation of the Antiproliferative Activity of a Series of Novel Fused Xanthenone Aminoderivatives in Human Breast Cancer Cells

Abstract

Derivatives of two novel, structurally related heterocyclic ring systems, xantheno[3,4-d]imidazole and chromeno[4,3,2-c,d]imidazo[4,5-f]indazole, bearing aminoalkyl side chains, have been synthesized, and their antiproliferative activity has been studied against the aggressive human breast MDA-MB-231 cell line. The pyrazole-fused analogue 27a possesses a pronounced antiproliferative effect on the tested cell line, evident at 1 muM, and achieves an IC50 of 6.5 microM.

Cobalt(II) complexes with disubstituted 3-aminopyrazole derivative: Mononuclear Co(II) complex with in situ prepared formamidine ligand

“…With an idea of producing an adenino-mimetic pharmacophore, we accepted a challenging task to explore what would happen in an anhydrous solution, in the presence of CH(OEt) 3 excess which is a known dehydrating and in the same time a CH-group supplying agent [29] for insertion purposes. Under this reaction condition the formation Scheme 1. of a formamidine group becomes very probable.…”

Synthesis, Biological Evaluation and Stability Studies of Some Novel Aza-Acridine Aminoderivatives

“…Although considerable progress has been made in this field, more work is needed to further improve the potency and selectivity of these compounds. In the course of our involvement in this area, we had previously studied several amino-substituted acridine derivatives with interesting anticancer properties [ 15 , 21 , 22 , 23 ]. These compounds share common structural features with the compounds described above, bearing a basic side chain and a nitro group, and exhibit substantial cytotoxic activities against a panel of cancer cell lines, presumably due to DNA binding and intercalation.…”

Ultrasound promoted synthesis of chromeno[2,3-b]pyridines and their evaluation as lipid peroxidation inhibitors

“…Both fragments display a wide range of biological activities; they are present in many drugs and have been extensively studied. Chromenes form a group of either naturally or synthetically obtained compounds possessing a broad diversity of biological activities with an impact in the treatment of inflammation and ulcers, 9 schizophrenia, 10 cancer, 11 etc.…”