Cytotoxicity of three new triazolo-pyrimidine derivatives against the plant trypanosomatid: Phytomonas sp. isolated from Euphorbia characias

Abstract

There is no effective chemotherapy against diseases caused by

Essramycin: A First Triazolopyrimidine Antibiotic Isolated from Nature†

“…Comparison of the 13 C-NMR data of essramycin with values of related synthetic compounds of type 1 delivered, however, a much better agreement with the experimental values than with compounds of type 2, confirming the skeleton of 1 [15,16]: A C-2 substituent affects the ipso C atom of 1,2,4-triazolo[1,5-a]pyrimidines, however, the influence on the 13 C shifts of the other ring atoms is negligible (Table 4). [1,2,4]Triazolo[1,5-a]pyrimidines have found a broad interest as fungicides [17], herbicide safener [18,19], kinase inhibitors [20,21], antiparasitic [22] and plant protecting agents [23]. Thousands of compounds of this type have been described, however, to the best of our knowledge, not a single natural product is amongst them [6,24,25].…”

Synthesis and anti-tumor activities of new [1,2,4]triazolo[1,5-a]pyrimidine derivatives

“…Synthesis of new [1,2,4]triazolo[1,5-a]pyrimidine derivatives was accomplished and structures were elucidated by means of various characterization techniques such as elemental analyses, spectral (IR, 1 H NMR, 13 C NMR, 2D NMR), and X-ray single crystal diffraction data. These derivatives were evaluate for in vitro anti-tumor using various human cancer cell lines…”

“…Navarro [1] found that 4,7-H-5-methyl-7-oxo [1,2,4]triazolo [1,5-a]pyrimidine have a moderate antitumor activity against breast carcinoma, MCF7 cell lines. (Figure 2 and 3).…”

“…Triazolopyrimidines represent a pharmaceutically important class of compounds because of their diverse range of biological activities, such as antitumor [1], cytotoxicity [2], therapeutic potentiality [3], potent and selective ATP site directed inhibition of the EGF-receptor protein tyrosine kinase [4] and cardiovascular [5] activities. In addition, they have been found in DNA-interactive drugs [6] and as useful building blocks in the synthesis of herbicidal drugs, e.g.…”

“…In view of these reports and in continuation of our interest in the synthesis of a variety of heterocyclic systems for biological evaluation [11][12][13][14][15][16][17], we describe herein a facile synthesis of some new 1,2,4-triazolo [5,1-a]pyrimidine derivatives and study the anti-carcinogenic effects of two newly synthesized derivatives, 7,8-dihydro-6H-cyclopenta[e] [1,2,4] triazolo [1,5-a]pyrimidine and 6,7,8,9,10,11-hexahydrocyclo octa[e] [1,2,4]triazolo [1,5-a]pyrimidine against human hepatocarcinoma (HepG2) and breast carcinoma (MCF7).…”