Sytnhesis of Organoboron Amide-Ester Branched Derivatives of Poly(Itaconic Anhydride-alt-2-Vinyl-1,3-Dioxolane) and Cancer Cells Interaction Studies

Abstract

New organaboron amide-ester branched derivatives of poly(itaconic anhydridealt-2-vinyl-1,3-dioxolane) are synthesized by amidolysis and grafting reactions, respectively. The structure and composition of the synthesized compounds are characterized by FTIR-ATR (Fourier Transform-Infrared-Attenuated Total Reflection) and 1 H (13 C) NMR (Nuclear Magnetic Resonance) spectroscopy. These novel functionalized boron containing biopolymers are interacted with HeLa (human cervix carcinoma cell) cancer cells and L929 Fibroblast (normal) cells. Their anticancer properties are investigated using a combination of different biochemical analysis methods. It is found that both the values of the cytotoxicity and necrotic indexes are increased due to organoboron linkage but these indexes of organoboron amide-ester derivative are visibly decreased because of α-Hydroxy-ω-methoxypoly(ethylene oxide) (PEO) biocompatibilization. The results of these studies allow us to utilize PEO branched derivatives of synthesized organoboron copolymers (up to 200 µg mL-1) as therapeutic potential functional copolymer drugs in cancer chemotherapy and Boron-Neutron Capture Therapy (BNCT).

Biological evaluation the 2‐aryl‐2,3‐dihydrobenzodiazaborinin‐4(1H)‐ones as potential dual α‐glucosidase and α‐amylase inhibitors with antioxidant properties

“…Replacement of covalent carbon‐carbon bonds with boron‐nitrogen bonds has in many cases provided compounds with significantly improved biological and electronic properties. Moreover, the boron centre can be converted from neutral trigonal planar (sp 2 ) to tetrahedral (sp 3 ) hybridization under proper physiological conditions to form strong interactions with the receptor (Özçayan, 2019). Previous studies on the 2,1‐borazaronaphthalenes, for example, have demonstrated strong correlation of their biological properties in vitro as inhibitors of phosphodiesterase 10A (PDE10A; Vlasceanu et al., 2015) and β2 receptor (Rombouts et al., 2015) compared to the reference standards used for the assays.…”