Abstract
To explore the anticancer activity of 2, 4, 5, 6-substituted pyrimidines, several ethyl 2-(1-aminocyclobutyl)-5-(benzoyloxy)-6-hydroxy-pyrimidine-4-carboxylate derivatives associated with the different substituted aromatic/aliphatic carboxamides and sulfonamides were synthesized. Different groups and position on phenyl ring attached to the carboxamide and sulfonamide of the pyrimidine led to two set of compounds. Their chemical structures were confirmed by IR,1H NMR and LC/MS analysis. Cytotoxicity of all the synthesized compounds were examined on human leukemia celllines (K562 and CEM). The preliminary results showed most of the derivatives exhibited good antitumor activity. Compound with para chloro substitution among carboxamides and compound with meta dichloro substitution among sulphonamidesexhibited significant antitumor activity with IC50 value of 14.0 μM and 15.0 μM respectively against K562cell line. For comparison among electron donating groups between carboxamides and sulfonamides, compounds with para tert-butyl substitution were chosen for further studies. Cell cycle analysis suggests that both tert-butyl substituted compounds are able to induce apoptosis.
Highlights
Cancer is a terrible disease which is the leading death of the human population in some areas of the world
Cytotoxicity of all the synthesized compounds were examined on human leukemia cell lines (K562 and CEM)
Pyrimidine ring was derivatized by substituting electron withdrawing and electron releasing groups along with cyclobutyl carboxamide 2(a-i) and sulfonamide 3(a-i) moiety at position 2 of the pyrimidine ring
Summary
Cancer is a terrible disease which is the leading death of the human population in some areas of the world. It is the second leading cause of death, behind cardiovascular disease, in the United States [1]. Cancer may affect people at all ages, even fetuses, but the risk for most varieties increases with age. Leukemia is a cancer of the blood-forming cells. Leukemia is the most common childhood cancer, affecting more than 3,500 children in the United States every year. There are three main methods of cancer treatment: surgery, radiation therapy, and chemotherapy. With the development of molecular biology, chemotherapy is becoming a more important therapeutic method. Designing new anticancer drugs with high-efficiency and broad-spectrum activity is a significant study area today
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
