Anticancer and radio-sensitizing evaluation of some new thiazolopyrane and thiazolopyranopyrimidine derivatives bearing a sulfonamide moiety

Citation:
Ghorab, M. M., F. A. Ragab, H. I.Heba, and R. M.El-Hazek, "Anticancer and radio-sensitizing evaluation of some new thiazolopyrane and thiazolopyranopyrimidine derivatives bearing a sulfonamide moiety", European Journal of Medicinal Chemistry, vol. 46, issue 10, pp. 5120–5126, 2011.

Abstract:

Recently, it has been reported that compounds bearing a sulfonamide moiety posses many types of biological activities, including anticancer activity. There a variety of mechanisms for their anticancer activity, and the most prominent mechanism is the inhibition of carbonic anhydrase (CA) isozymes. The present work reports the synthesis of some new thiazolo[4,5-b]pyran and thiazolo[4,5-b] pyrano[2,3-d] pyrimidine derivatives bearing a sulfonamide moiety. The design of the structures of these compounds complies with the general pharmacophoric requirements for CA inhibiting anticancer drugs. The newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line ( MCF7) . Most of the screened compounds showed interesting cytoxic activity compared to doxorubicin as a reference drug. Three compounds showed higher cytotoxic activities than doxorubicin. These three compounds were evaluated again for their ability to enhance the cell killing effect of gamma radiation.

Notes:

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