Synthesis and antitumor activity of bis(arylsulfonyl)dihydroimidazolinone derivatives

Bioorg Med Chem Lett. 2020 Jan 1;30(1):126776. doi: 10.1016/j.bmcl.2019.126776.

Satapanawat Sittihan ¹, Watthanachai Jumpathong ², Pattarawut Sopha ³, Somsak Ruchirawat ⁴

Affiliations

1 Program on Chemical Biology, Chulabhorn Graduate Institute, Center of Excellence on Environmental Health and Toxicology (EHT), Ministry of Education, 906 Kamphaeng Phet 6, Laksi, Bangkok 10210, Thailand. Electronic address: satapanawat@cgi.ac.th.
2 Program on Chemical Biology, Chulabhorn Graduate Institute, Center of Excellence on Environmental Health and Toxicology (EHT), Ministry of Education, 906 Kamphaeng Phet 6, Laksi, Bangkok 10210, Thailand.
3 Program on Applied Biological Sciences, Chulabhorn Graduate Institute, Center of Excellence on Environmental Health and Toxicology (EHT), Ministry of Education, 906 Kamphaeng Phet 6, Laksi, Bangkok 10210, Thailand.
4 Program on Chemical Biology, Chulabhorn Graduate Institute, Center of Excellence on Environmental Health and Toxicology (EHT), Ministry of Education, 906 Kamphaeng Phet 6, Laksi, Bangkok 10210, Thailand; Laboratory of Medicinal Chemistry, Chulabhorn Research Institute, 54 Kamphaeng Phet 6, Laksi, Bangkok 10210, Thailand.

PMID: 31704206 DOI: 10.1016/j.bmcl.2019.126776

Abstract

A series of novel bis(arylsulfonyl)dihydroimidazolinones with different aryl substitution patterns were readily synthesized and evaluated for their antitumor activities. Some of the newly synthesized compounds exhibited cytotoxicity at micromolar range against multiple Cancer cell lines, including A549, HepG2, HuCCA-1, and MOLT-3. The most potent analogue contained pentafluorobenzenesulfonyl groups, which could be chemically elaborated to serve as a potential pharmacophore.

Keywords

Antitumor; Bis(arylsulfonyl)dihydroimidazolinones; Cytotoxicity.

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