Design and synthesis of novel 5-aminosalicylate (5-ASA)-4-thiazolinone hybrid derivatives with promising antiproliferative activity

Bioorg Med Chem Lett. 2016 Apr 1;26(7):1647-50. doi: 10.1016/j.bmcl.2016.02.073.

Hajjaj H M Abdu-Allah ¹, Samia G Abdel-Moty ², Raafat El-Awady ³, Abdel-Nasser A El-Shorbagi ⁴

Affiliations

1 Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt. Electronic address: hagag.abdallah@pharm.au.edu.eg.
2 Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.
3 Cancer Biology Department, National Cancer Institute, Cairo University, Cairo, Egypt; Sharjah Institute for Medical Research and College of Pharmacy, University of Sharjah, Sharjah 27272, United Arab Emirates.
4 Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt; Sharjah Institute for Medical Research and College of Pharmacy, University of Sharjah, Sharjah 27272, United Arab Emirates.

PMID: 26947606 DOI: 10.1016/j.bmcl.2016.02.073

Abstract

Two privileged pharmacophores were assembled in one molecular frame involving 5-aminosalicylate and 4-thiazolinones that can be found in different stereochemical features. The compounds were fully characterized and evaluated for antiproliferative activity against four human Cancer cell lines and some are equipotent to doxorubicin with lower cytotoxicity to normal cells. The most interesting finding relates to compound 10, which shows an IC50 value of 70nM against MCF-7 cells, while the IC50 against human fibroblasts is 10μM. The results of this study indicate that the new compounds are optimal anti-cancer leading compounds and merit further studies to optimize their structure, detect their biotargets and in vivo activity.

Keywords

4-Thiazolidinone; 4-Thiazolinone; 5-Aminosalicylic; Antiproliferative; Hybrid; Stereochemistry.

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