F. G. Arsenyan

Antitumor activity of imidazole derivatives: dacarbazine and the new alkylating agent imidazene (Review)

The physicochemical properties and antitumor activity of dacarbazine, its analogs, and the new alkylating agent imidazene are reviewed. It is shown that the activity of dacarbazine is superior to most of its analogs. Imidazene exhibits an advantage over dacarbazine with respect to both stability and activity and can be used for the treatment of malignant melanoma and sarcoma of soft tissues and in combined chemotherapy.

Synthesis and antitumor activity of new furyl-2-substituted 1,3,4-thiadiazoles and 1,2,4-triazoles

A series of new furyl-2-substituted derivatives of 1,3,4-thiadiazole and 1,2,4-triaozle have been synthesized. The S-alkylation and aminomethylation of the latter leading to their 3-mercapto- and 2-aminomethylene-substituted derivatives have been studied. Results of antitumor activity testing of the synthesized compounds are presented and discussed.

Synthesis and antitumor activity of pyrano[4′,3′:4,5]pyrido[2,3-b]thieno[3,2-d]-1,2,3-triazine and l,2,3-triazino[4′,5′:4,5¦thieno-[2,3-c]isoquinoline derivatives

Methods for the synthesis of new heterosystems of condensed thieno[3,2-d]-1,2,3-triazines on the basis of pyrido[2,3-b]thiophenes have been developed. The antitumor activity of the synthesized compounds was studied and several compounds possessing low toxicity and moderate antitumor activity were found.

Imidazole derivatives and their antitumor activity (review)

Bis(2-chloroethyl)amino derivatives of imidazole, 4(5)-aminoimidazol-5(4)-carboxamide, 4-nitro-5-thioimidazole, benzimidazole, and imidazolylpeptides are reviewed. Data are presented for active compounds, some of which have passed the preclinical testing stage. Structures under consideration are interesting with respect to both the search for new antitumor drugs and the synthesis of compounds with different biological properties.

Synthesis and antitumor activity of 3,4,5-substituted 1,2,4-triazoles

Conditions for effective alkylation of new 3,4-substituted-5-mercapto-1,2,4-triazoles with various alkylating agents are established. Several compounds possessing pronounced antitumor activity have been found in experiments using two xenograft tumor models.

Imidazole Derivatives. XXX. Synthesis and Antitumor Activity of 4-amyloxy-3-nitroacetophenone 2-imidazolinyl-2-hydrazone and Related Compounds

The antitumor properties of 2-imidazolinyl-2-hydrazones of acetophenones with various substituents in the benzene ring have been studied. High activity is found for 4-amyloxy-3-nitroacetophenone 2-imidazolinyl-2-hydrazone, which points to the expediency of its further investigation.

Antitumor activity of substituted methylglyoxal bisthiosemicarbazones and their copper(II) chelates

A series of new bisthiosemicarbazones of methylglyoxal and their copper(II) complexes were synthesized. Evidence of antitumor properties of some products combined with low toxicity shows that further searching for antitumor agents in this group of compounds may be promising.

Synthesis, Transformations, and Study of Some Biological Properties of New 3,4,5-Substituted 1,2,4-Triazoles

A series of new 3,4,5-substituted 1,2,4-triazoles were synthesized. Their SH-alkylation by various alkylating compounds and aminomethylation leading to the formation of Mannich bases were studied. The influence of the synthesized compounds on the level of DNA methylation and their antitumor and antibacterial properties were investigated. Several compounds with pronounced demethylation and weak antitumor and antibacterial activities were identified. Correlations among the investigated biological properties were not found.

Synthesis and antitumor activity of a series of benzofuryl-substituted 1,2,4-triazoles and triazolin-5-thiones

3-Benzofuryl-4-benzyl(cyclohexyl)-5-mercapto-1,2,4-triazoles were synthesized by cyclization of the corresponding substituted thiosemicarbazides. 5-Mercaptotriazoles were S-alkylated with various alkenyl-substituted benzylhalogenides, chloracetamide, chloroacetic, and α-bromopropionic and α-bromocaproic acids. The aminomethylation and hydroxymethylation reactions of 3-benzofuryl-4-benzyl(cyclohexyl)-5-mercapto-1,2,4-triazoles were studied. The antitumor activity of the resulting compounds was investigated.

Imidazole derivatives XVIII. Synthesis and antitumor activity of some bis[2-chloroethyl]amino imidazole derivatives

T h e 1 b e n z y l s u b s t i t u t e d i m i d a z o l e s ( I V g a n d h ) w e r e o b t a i n e d b y t h e a l k y l a t i o n o f t h e i s o d i u m s a l t o f 4 ( 5 ) ( 4 a c e t y l a m i n o p h e n y l ) i m i d a z o l e w i t h b e n z y l c h l o r i d e w i t h s u b s e q u e n t d e a c e t y l a t i o n o f t h e 1 b e n z y l 4 ( 4 a c e t y l a m i n o p h e n y l ) i m i d a z o l e s .