No abstract

1,2,4-Thiadiazol-5(2H)-imines

No abstract

Synthesis of a series of 2-(dichloromethyl)pyrazolo [1,5-a][1,3,5]triazines and evaluation in vitro of their anticancer activity against a panel of 60 cell lines derived from nine cancer types, namely leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, breast cancer. Methods. Organic synthesis; biological tests; spectral methods; statistical methods. Results. In vitro screening of the anticancer activity showed that 5 of 26 tested compounds can effectively inhibit the growth of certain cancer cell lines. Conclusions. New type of N-(2,2-dichloro-1-cyanoethenyl)carboxamides heterocyclization with 1H-pyrazol-5-amines led to the formation of 2-(dichloromethyl)pyrazolo [1,5-a][1,3,5]triazines. Some of these compounds inhibit growth of certain cancer cell lines.

N-(2,2-Dichloro-1-cyanoethenyl)carboxamides 1 are known to be highly reactive electrophilic reagents suitable for the synthesis of heterocyclic compounds. Two research groups headed by K. Matsumura and B. Drach began independently in the 1970s studying the cyclocondensation of these reagents with N-nucleophiles. It was found that the reaction of 1 with ammonia, high basicity amines, and hydrazine leads to the oxazole ring formation that has become a common method for the production of 5-amino-4-cyanooxazoles 2 (Scheme 1) [1-3]. A quite unusual cycloaddition of benzamidine to compounds 1 reported by Drach and co-workers was featured by the