Synthesis and cytotoxicity of dibenzo[(γ-aryl)pyridino]aza-17-crown-5 ethers

For the development of new anticancer agents, dibenzo[(γ-aryl)pyridino]aza-17-crown-5 ethers containing 2,4,6-triarylpyridine were synthesized successfully by one-step domino-condensation of 1,8-bis(2-acetylphenoxy)-3,6-dioxaoctane, arylaldehydes and ammonium acetate according to the conditions of Hantzsch reactions. The synthesized γ-arylpyridine derivatives show high cytotoxic activity against human cancer cell lines: Hep-G2, RD, FL, Lu1. Compounds (3b,c) showed significant cytotoxicity against all four human cell lines whereas the similar synthesized compound (3d) possessed cytotoxicity against HepG2, Lu1 and RD cell lines. Meantime, both compounds (3f,g) containing γ-heteroaryl only exhibited cytotoxicity against RD and FL cell lines. Azacrown ethers (3b-d) exhibited low activity on the Vero cell line, meaning that they can be evaluated for their potential as promising anticancer agents. X-Ray structure study was performed to determine the structure of the representative compound 3a. © ISUCT Publishing

Novel podands containing N-arylthiosemicarbazide moiety

Six novel biological active podands based on N-arylthiosemicarbazide were synthesized from 1,5-bis(2-formylphenoxy)-3-oxapentane or 1,8-bis-(2-formylphenoxy)-3,6-dioxaoctane. All podands have tested cytotoxicity on human cancer cell lines RL, MCF7, RD, and HepG2 and antimicrobial activity. © ISUCT Publishing

Synthesis of tetrakisbenzo-31(34)-crown-7(8) ethers

Condensations of 1,5-bis(2-formylphenoxy)-3-oxapentane (1a) or 1,8-bis(2-formylphenoxy)-3,6-dioxanoctane (1b) podands and 1,8-bis(2-acetylphenoxy)-3,6-dioxanoctane (2) gave two novel crown ethers: tetrakis-(benzo)-31-crown-7 ether (5) and tetrakis(benzo)-34-crown-8 ether (6). Their molecular structures were established by IR, NMR and MS methods. © ISUCT Publishing

Synthesis and cytotoxicity of dibenzo[(γ-aryl)pyridino]aza-17-crown-5 ethers

For the development of new anticancer agents, dibenzo[(γ-aryl)pyridino]aza-17-crown-5 ethers containing 2,4,6-triarylpyridine were synthesized successfully by one-step domino-condensation of 1,8-bis(2-acetylphenoxy)-3,6-dioxaoctane, arylaldehydes and ammonium acetate according to the conditions of Hantzsch reactions. The synthesized γ-arylpyridine derivatives show high cytotoxic activity against human cancer cell lines: Hep-G2, RD, FL, Lu1. Compounds (3b,c) showed significant cytotoxicity against all four human cell lines whereas the similar synthesized compound (3d) possessed cytotoxicity against HepG2, Lu1 and RD cell lines. Meantime, both compounds (3f,g) containing γ-heteroaryl only exhibited cytotoxicity against RD and FL cell lines. Azacrown ethers (3b-d) exhibited low activity on the Vero cell line, meaning that they can be evaluated for their potential as promising anticancer agents. X-Ray structure study was performed to determine the structure of the representative compound 3a. © ISUCT Publishing

N-acylation and N-alkylation of bis(benzo)aza-14-crown-4 ethers. Novel hybrid compound - bis(furanyl)triazinethiolazacrown ether

Macroheterocycles containing aza-14-crown-4 ether subunit were synthesized by one-step domino reaction. They are interesting objects for study of physicochemical properties and types of transformation. The N-acylated and N-alkylated aza-14-crown-4 ethers were obtained in good yields. The new hybrid compound - bis(furanyl)triazinethiolazacrown ether - was formed by S-alkylation of N-chloroacyl derivative (3). According to the PASS program, these substances can be inhibitors of the permeability of cell membrane and act also as a CYP2H substrate. © ISUCT Publishing

Novel podands containing N-arylthiosemicarbazide moiety

Six novel biological active podands based on N-arylthiosemicarbazide were synthesized from 1,5-bis(2-formylphenoxy)-3-oxapentane or 1,8-bis-(2-formylphenoxy)-3,6-dioxaoctane. All podands have tested cytotoxicity on human cancer cell lines RL, MCF7, RD, and HepG2 and antimicrobial activity. © ISUCT Publishing

Synthesis of tetrakisbenzo-31(34)-crown-7(8) ethers

Condensations of 1,5-bis(2-formylphenoxy)-3-oxapentane (1a) or 1,8-bis(2-formylphenoxy)-3,6-dioxanoctane (1b) podands and 1,8-bis(2-acetylphenoxy)-3,6-dioxanoctane (2) gave two novel crown ethers: tetrakis-(benzo)-31-crown-7 ether (5) and tetrakis(benzo)-34-crown-8 ether (6). Their molecular structures were established by IR, NMR and MS methods. © ISUCT Publishing