Synthesis of new derivatives of 3‐aryl‐1,5‐dimethyl‐1H‐[1,2,4]triazolo[4′,3′:1,2]pyrimido[4,5‐e][1,3,4]oxadiazines as potential antiproliferative agents

Abstract

(5b), as examples, were tested on different cancer cell lines including HeLa, MCF-7, and HepG2. Malignant cells were cultured in DMEM medium and incubated with different concentrations of the titled compounds. Cell viability was quantitated by MTT assay.

Synthesis and Anticancer Evaluation of New Derivatives of 3-Phenyl-1,5-Dimethyl-1H-[1,2,4]Triazolo[4′,3′:1,2]Pyrimido[4,5-e][1,3,4]Oxadiazine

“…29 Treatment of compound (1) with benzoyl chloride in the presence of K 2 CO 3 in boiling dry CH 3 CN afforded 7-chloro-1,5-dimethyl-3-phenyl-1H-pyrimido [4,5-e] [1,3,4]oxadiazine (2). 27 Subsequent reaction of this compound with hydrazine hydrate led to the replacement of * Correspondent: E-mail: mbakavoli@yahoo.com the chorine atom with hydrazine and gave quantitatively the hydrazino derivative (3) which was utilised as the precursor for the synthesis of new tricyclic compounds 5a-e and 7a-e. Thus, heating under stirring of the compound (3) with various aromatic aldehydes in the presence of a few drops of acetic acid in ethanol resulted in the formation of corresponding hydrazones 4a-e.…”

Synthesis and evaluation of cytotoxicity of 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitriles

“…They are also identified as potential antimicrobial and antican cer [11][12][13][14][15][16][17][18], as well as anti inflammatory agents [19]. Prompted by these reports and in continuation of our endeavor on potential anticancer agents [20,21], we have now focused our attention on preparing a series of 6 amino 4 phenyl 2 thioxo 1,2,3,4 tetrahydro pyrimidine 5 carbonitriles (I)-(X) and screened them for antiproliferative activity against human breast cancer (MCF 7), human colon carcinoma (HT29), and non malignant mouse fibroblast (L929) cell lines. The MCF 7 and HT29 cell lines are known as widely used model systems for the study of breast [22] and colorectal [23] cancers.…”

Synthesis of Oxazolo[5,4‐d][1,2,4]triazolo[4,3‐a]pyrimidines as a New Class of Heterocyclic Compounds

“…Regarding these points and as part of our ongoing studies dealing with the synthesis of various fused pyrimidines [28][29][30][31][32][33][34], herein, we wish to report on the synthesize of oxazolo [5,4-d] [1,2,4]triazolo [4,3-a]pyrimidine (5a-p) as members of a novel heterocyclic system that may be of use in designing new, potent and effective pharmacologically active compounds.…”