Synthesis in the phenothiazine series

1-Bromophenothiazine (I) and 1,3-dibromophenothiazine (II) have been synthesized by the intramolecular rearrangement of 2-acetylaminophenyl 2-bromo-6-nitrophenyl sulfide (III) and 2-acetylaminophenyl 2,4-dibromo-6-nitrophenyl sulfide (VIII) and the subsequent cyclization of resulting N-acetyl-2-bromo-2-mercapto-6-nitrodiphenylamine (IV) and N-acetyl-2,4-dibromo-2-mercapto-2-nitrodiphenylamine (IX), followed by saponification of the acetyl groups of the latter, respectively.For Communication XXIV see [6].Translated from Khimiya Geterotsiklicheskikh Soedinenii, Vol. 6, No. 8, pp. 1041–1044, August, 1970.     

1-Vinyl-1,2,4-triazole in copolymerization reaction with 1-vinyl-4,5,6,7-tetrahydroindole: synthesis and properties of copolymers

A radical copolymerization of 1-vinyl-1,2,4-triazole (VTA) with 1-vinyl-4,5,6,7-tetrahy-droindole (VTHI) was studied. New thermally stable functional copolymers of different composition, well soluble in organic solvents were synthesized. It was found that VTA has higher reactivity as compared to VTHI. A new soluble polymeric nanocomposite with metallic silver nanoparticles encapsulated into the matrix of synthesized copolymer was obtained.     

Synthesis and characterization of silver polymer nanocomposites of 1-vinyl-1,2,4-triazole with acrylonitrile

Novel organic-inorganic nanocomposites were synthesized by chemical reduction of silver ions from silver acetate in DMSO and DMF solutions in the presence of the stabilizing copolymer of 1-vinyl-1,2,4-triazole-acrylonitrile. The solvents DMSO and DMF can act as efficient reducing agents for silver ions, which makes it possible to carry out the reaction under mild conditions and simplify procedures of nanocomposite isolation. The structure and properties of the starting copolymer and related nanocomposites were characterized by UV, IR, and ¹H and ¹³C NMR spectroscopy, as well as transmission electron microscopy and thermogravimetry. The prepared polymer nanocomposites contain 6.8–7.2% silver in the form of nanoparticles with a size of 2–20 nm uniformly dispersed in the polymer matrix. The nanocomposites are readily soluble in DMSO and DMF and do not decompose on heating to 260 °C.     

Sea Anemone Heteractis crispa Actinoporin Demonstrates In Vitro Anticancer Activities and Prevents HT-29 Colorectal Cancer Cell Migration

Actinoporins are the most abundant group of sea anemone cytolytic toxins. Their membranolytic activity is of high interest for the development of novel anticancer drugs. However, to date the activity of actinoporins in malignant cells has been poorly studied. Here, we report on recombinant analog of Hct-S3 (rHct-S3), belonging to the combinatory library of Heteractis crispa actinoporins. rHct-S3 exhibited cytotoxic activity against breast MDA-MB-231 (IC₅₀ = 7.3 µM), colorectal HT-29 (IC₅₀ = 6.8 µM), and melanoma SK-MEL-28 (IC₅₀ = 8.3 µM) cancer cells. The actinoporin effectively prevented epidermal growth factor -induced neoplastic transformation of JB6 Cl41 cells by 34% ± 0.2 and decreased colony formation of HT-29 cells by 47% ± 0.9, MDA-MB-231 cells by 37% ± 1.2, and SK-MEL-28 cells by 34% ± 3.6. Moreover, rHct-S3 decreased proliferation and suppressed migration of colorectal carcinoma cells by 31% ± 5.0 and 99% ± 6.4, respectively. The potent anti-migratory activity was proposed to mediate by decreased matrix metalloproteinases-2 and -9 expression. In addition, rHct-S3 induced programmed cell death by cleavage of caspase-3 and poly (ADP-ribose) polymerase, as well as regulation of Bax and Bcl-2. Our results indicate rHct-S3 to be a promising anticancer drug with a high anti-migratory potential.