Series of novel triterpenoid hybrids were designed and synthesized by introducing 2-aminobenzamide moiety at C28 position of triterpenoid derivatives. Thirteen new conjugates were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity in KB and HepG2 cancer cell lines.
Betulin was converted to the corresponding alkyne-functionalized esters and amides and subsequently deployed as substrates for a 'click' chemistry-mediated coupling with 3'-azido-3'-deoxythydimine (AZT) to furnish a novel betulin-triazole-AZT hybrid compounds. Eleven new hybrids were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity in KB and HepG2 cancer cell lines.
A series of new hydroxamate derivatives of lupane triterpenoids has been designed and successfully synthesized. The synthesized compounds were evaluated for their in vitro antitumor activity using the 3-[4,5-dimethylthiazol-2-yl]−2,5-diphenyltetrazolium bromide-based assay against the human cancer cell lines KB and HepG2. Most of these derivatives possess at least moderate cytotoxic activity and the hydroxamate derivative compounds 3c, 3e, 7a, and 15b could be lead compounds for further optimization to develop novel anticancer agents.
Hợp chất lai của 2-aminobenzothiazole có chứa nhóm 2-aminobenzamide qua cầu nối amide đã được thiết kế, tổng hợp thành công và cấu trúc được xác định bằng các phương pháp phổ cộng hưởng từ hạt nhân (NMR), phổ khối lượng phân giải cao (HRMS). Hợp chất (3) tổng hợp cũng đã được thử hoạt tính kháng tế bào ung thư người in vitro trên hai dòng tế bào A549 và SW480. Kết quả thu được cho thấy, hợp chất (3) không thể hiện hoạt tính đối với dòng tế bào SW480 nhưng lại thể hiện độc tính đối với dòng tế bào A549 với giá trị IC50 là 29.49 µM.
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