Synthesis and Cytotoxicity Assay of Aniline Substituted Thienopyrimidines for Anti-Colorectal Cancer Activity

Abstract

Colorectal cancer ranks third among all cancers worldwide. Colorectal cancer is treated using a variety of therapies and methods. Almost 1 million deaths are caused every year. The treatment is very ineffective against the cancer cells. Today, drug resistance is a major problem in the fight against cancer. In order to address this, new drugs must be developed. The focus of the article is the synthesis of small molecules of aniline-substituted thieno(2,3-d) pyrimidine derivatives and the evaluation of their anticancer activities. Based on the bioisosterism theory and results from earlier research, thienopyrimidine is substituted with aniline derivatives. Using the HCT116 cell line, the synthesized compounds were tested for cytotoxicity. When compared to standard 5-Fluorouracil (IC50 = 435.59 μg/ml), the compound MS4e has a lower IC50 value (357.12 μg/ml). When aniline was substituted with halogen (F, Cl) cytotoxic properties are observed. It seems to hold special potential for the treatment of colorectal cancer, as the compound MS4e has less IC50 value than the standard.