硒吩并吡唑衍生物及其作為抗癌劑的用途

專利類型

發明

專利國別 (專利申請國家)

中華民國

專利申請案號

099121902

專利證號

I 408141

專利獲證名稱

硒吩并吡唑衍生物及其作為抗癌劑的用途

專利所屬機關 (申請機關)

中國醫藥大學

獲證日期

2013/09/11

技術說明

設計並合成兩系列1,3-disubstituted selenolo[3,2-c]pyrazole和1,3-disubstituted selenolo[2,3-c]pyrazole衍生物。將這些新合成的selenolopyrazole衍生物以A498腎癌細胞篩選結果發現，在受試的化合物中，hydroxymethyl衍生物包括化合物2, 33, 36和37都具有顯著的抑制活性。我們選擇其中活性最強的化合物2提供美國NCI做60種人類腫瘤細胞的評估結果發現，化合物2對NCI-H226非小細胞肺癌及A498腎癌具有選擇抑制活性。其作用模式與NCI的標準database中所儲存的175種抗癌藥都不相同，因此我們認為在所有合成的化合物中hydroxymethyl derivatives (2, 33, 36和37)值得進一步的開發成為新穎的抗腎癌及抗非小細胞肺癌的新藥候選物質。 Two series of 1,3-disubstituted selenolo[3,2-c]pyrazole and 1,3-disubstituted selenolo[2,3-c]pyrazole derivatives were designed and synthesized. The newly synthesized selenolopyrazoles were evaluated for their cytotoxicity against A-498 renal cancer cell line. Hydroxymethyl derivatives of the synthesized selenolopyrazoles including compounds 2, 33, 36 and 37, exhibited significanct inhibitory activity. As one of the most potent hydromethyl derivative, compound 2, was submitted to NCI for evaluation against its 60 human tumor cell panel. The results demonstrated that compound 2 selectively inhibited NCI-H226 non-small cell lung cancer cell line and A-498 renal cancer cell line. The mode of action of compound 2 seems to differ from those of the 175 anticancer agent listed in NCI’s standard database. Thus, we recommend that hydroxymethyl derivatives of the synthesized compounds should be developed further as new drug candidate for treatment of non-small cell lung cancer and renal cancer.

備註

106-02研發成果審查會同意終止維護專利

連絡單位 (專責單位/部門名稱)

產學合作處生物科技發展育成中心

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(04)2205-3366轉1581

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