Synthesis and Cytotoxicity Assay of Aniline Substituted Thienopyrimidines for Anti-Colorectal Cancer Activity
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...
| Main Authors: | , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2023-01-01
|
| Series: | Results in Chemistry |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211715623001650 |
| _version_ | 1797799001534234624 |
|---|---|
| author | Mahalakshmi Suresha Biradar Shachindra L. Nargund Shankar Thapa |
| author_facet | Mahalakshmi Suresha Biradar Shachindra L. Nargund Shankar Thapa |
| author_sort | Mahalakshmi Suresha Biradar |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-13T04:13:23Z |
| format | Article |
| id | doaj.art-42a87b14cae343d1a6a55b295018de8a |
| institution | Directory Open Access Journal |
| issn | 2211-7156 |
| language | English |
| last_indexed | 2024-03-13T04:13:23Z |
| publishDate | 2023-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Results in Chemistry |
| spelling | doaj.art-42a87b14cae343d1a6a55b295018de8a2023-06-21T06:52:36ZengElsevierResults in Chemistry2211-71562023-01-015100926Synthesis and Cytotoxicity Assay of Aniline Substituted Thienopyrimidines for Anti-Colorectal Cancer ActivityMahalakshmi Suresha Biradar0Shachindra L. Nargund1Shankar Thapa2Department of Pharmaceutical Chemistry, Nargund College of Pharmacy, Rajiv Gandhi University of Health Science, Bengaluru, India; Corresponding author at: Department of Pharmaceutical Chemistry, Nargund College of Pharmacy, Dattatreya Nagar, Bengaluru 560085, India.Department of Pharmaceutical Chemistry, Nargund College of Pharmacy, Rajiv Gandhi University of Health Science, Bengaluru, IndiaDepartment of Pharmaceutical Chemistry, Nargund College of Pharmacy, Rajiv Gandhi University of Health Science, Bengaluru, India; Department of Pharmacy, Universal College of Medical Sciences, Bhairahawa, NepalColorectal 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.http://www.sciencedirect.com/science/article/pii/S2211715623001650ThienopyrimidineAnilineGewald ReactionColorectal cancerMTT Assay |
| spellingShingle | Mahalakshmi Suresha Biradar Shachindra L. Nargund Shankar Thapa Synthesis and Cytotoxicity Assay of Aniline Substituted Thienopyrimidines for Anti-Colorectal Cancer Activity Results in Chemistry Thienopyrimidine Aniline Gewald Reaction Colorectal cancer MTT Assay |
| title | Synthesis and Cytotoxicity Assay of Aniline Substituted Thienopyrimidines for Anti-Colorectal Cancer Activity |
| title_full | Synthesis and Cytotoxicity Assay of Aniline Substituted Thienopyrimidines for Anti-Colorectal Cancer Activity |
| title_fullStr | Synthesis and Cytotoxicity Assay of Aniline Substituted Thienopyrimidines for Anti-Colorectal Cancer Activity |
| title_full_unstemmed | Synthesis and Cytotoxicity Assay of Aniline Substituted Thienopyrimidines for Anti-Colorectal Cancer Activity |
| title_short | Synthesis and Cytotoxicity Assay of Aniline Substituted Thienopyrimidines for Anti-Colorectal Cancer Activity |
| title_sort | synthesis and cytotoxicity assay of aniline substituted thienopyrimidines for anti colorectal cancer activity |
| topic | Thienopyrimidine Aniline Gewald Reaction Colorectal cancer MTT Assay |
| url | http://www.sciencedirect.com/science/article/pii/S2211715623001650 |
| work_keys_str_mv | AT mahalakshmisureshabiradar synthesisandcytotoxicityassayofanilinesubstitutedthienopyrimidinesforanticolorectalcanceractivity AT shachindralnargund synthesisandcytotoxicityassayofanilinesubstitutedthienopyrimidinesforanticolorectalcanceractivity AT shankarthapa synthesisandcytotoxicityassayofanilinesubstitutedthienopyrimidinesforanticolorectalcanceractivity |