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一些含有生物活性磺酰胺部分的新型吡喃并噻唑-Schiff 碱的抗癌和放射增敏作用评价。

Anticancer and radiosensitizing evaluation of some new pyranothiazole-Schiff bases bearing the biologically active sulfonamide moiety.

机构信息

Medicinal, Aromatic and Poisonous Plants Research Center, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia.

出版信息

Eur J Med Chem. 2012 Jul;53:403-7. doi: 10.1016/j.ejmech.2012.04.009. Epub 2012 Apr 26.

Abstract

The present work reports the synthesis of some new Schiff bases, 5-(substituted benzylideneamino)-6-cyano-7H-7-(4-methoxyphenyl)-2-(4-sulphamoylphenylamino) pyrano[2,3-d]thiazole (5-15). 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 cytotoxic activities compared to doxorubicin as a reference drug. Compounds 4, 6-8 and 11 (IC(50): 27.51, 10.25, 9.55, 9.39 and 9.70 μM, respectively) exhibited higher cytotoxic activities than the reference drug doxorubicin (IC(50): 32.00 μM). Additionally, the previously mentioned compounds were evaluated again for their ability to enhance the cell killing effect of γ-radiation.

摘要

本工作报道了一些新的席夫碱的合成,5-(取代苄叉基氨基)-6-氰基-7H-7-(4-甲氧基苯基)-2-(4-磺酰胺基苯基氨基)吡喃并[2,3-d]噻唑(5-15)。这些化合物的结构设计符合 CA 抑制抗癌药物的一般药效学要求。新合成的化合物被评估了对人乳腺癌细胞系(MCF7)的体外抗癌活性。与阿霉素作为参考药物相比,大多数筛选出的化合物显示出有趣的细胞毒性活性。化合物 4、6-8 和 11(IC(50):27.51、10.25、9.55、9.39 和 9.70 μM)表现出比参考药物阿霉素(IC(50):32.00 μM)更高的细胞毒性活性。此外,上述化合物再次被评估了它们增强γ辐射细胞杀伤效应的能力。

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