dc.contributor.author	Gabr, Moustafa T.
dc.contributor.author	El-Gohary, Nadia S.
dc.contributor.author	El-Bendary, Eman R.
dc.contributor.author	El-Kerdawy, Mohamed M.
dc.contributor.author	Ni, Nanting
dc.date.accessioned	2017-12-05T07:30:03Z
dc.date.available	2017-12-05T07:30:03Z
dc.date.issued	2017-08-30
dc.description.abstract	A new series of thiazolylcoumarin derivatives was synthesized. The designed strategy embraced a molecular hybridization approach which involves the combination of the thiazole and coumarin pharmacophores together. The new hybrid compounds were tested for in vitro antitumor efficacy over cervical (Hela) and kidney fibroblast (COS-7) cancer cells. Compounds 5f, 5h, 5m and 5r displayed promising efficacy toward Hela cell line. In addition, 5h and 5r were found to be the most active candidates toward COS-7 cell line. The four active analogs, 5f, 5h, 5m and 5r were screened for in vivo antitumor activity over EAC cells in mice, as well as in vitro cytotoxicity toward W138 normal cells. Results illustrated that 5r has the highest in vivo activity, and that the four analogs are less cytotoxic than 5-FU toward W138 normal cells. In this study, 3D pharmacophore analysis was performed to investigate the matching pharmacophoric features of the synthesized compounds with trichostatin A. In silico studies showed that the investigated compounds meet the optimal needs for good oral absorption with no expected toxicity hazards.	en
dc.identifier.issn	1611-2156
dc.identifier.uri	http://hdl.handle.net/2003/36233
dc.identifier.uri	http://dx.doi.org/10.17877/DE290R-18247
dc.language.iso	en
dc.relation.ispartofseries	EXCLI Journal;Vol. 16 2017
dc.rights.uri	http://creativecommons.org/licenses/by/4.0/
dc.subject	Thiazolylcoumarins	en
dc.subject	Synthesis	en
dc.subject	Antitumor activity	en
dc.subject	Cytotoxic activity	en
dc.subject	3D pharmacophore elucidation	en
dc.subject	In silico studies	en
dc.subject.ddc	610
dc.title	Microwave-assisted synthesis and antitumor evaluation of a new series of thiazolylcoumarin derivatives	en
dc.type	Text
dc.type.publicationtype	article
dcterms.accessRights	open access
eldorado.dnb.zdberstkatid	2132560-1
eldorado.secondarypublication	true

Microwave-assisted synthesis and antitumor evaluation of a new series of thiazolylcoumarin derivatives

Files

Original bundle

License bundle

Collections