Design, synthesis and potent cytotoxic activity of novel 7-(N-[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives.
Design, synthesis and potent cytotoxic activity of novel 7-(N-[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives.
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新型7-(N-[(取代磺酰基)哌嗪基]-甲基)-喜树碱衍生物的设计、合成和有效细胞毒活性
DOI：
10.1016/j.bmcl.2017.02.066
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发表时间：
2017-04-15
影响因子：
2.7
通讯作者：
Lee KH
中科院分区：
文献类型：
--
作者：
Zhu GX;Cheng PL;Goto M;Zhang N;Morris-Natschke SL;Hsieh KY;Yang GZ;Yang QR;Liu YQ;Chen HL;Zhang XS;Lee KH
In an effort to discover potent camptothecin-derived antitumor agents, novel camptothecin analogues with sulfonylpiperazinyl motifs at position-7 were designed and synthesized. They were evaluated for in vitro cytotoxicity with the sulforhodamine-B (SRB) method in five types of human tumor cell lines, A-549, MDA-MB-231, KB, KB-VIN and MCF-7. With IC50 values in the low μM to nM level, most of the new analogues showed greater cytotoxicity activity than the reference compounds irinotecan and topotecan. Furthermore, compounds 12l (IC50, 1.2 nM) and 12k (IC50, 20.2 nM) displayed the highest cytotoxicity against the multidrug-resistant (MDR) KB-VIN cell line and merit further development as preclinical drug candidates for treating cancer, including MDR phenotype. Our study suggested that integration of sulfonylpiperazinyl motifs into position-7 of camptothecin is an effective strategy for discovering new potent cytotoxic camptothecin derivatives.
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DOI：
10.1073/pnas.242259599
发表时间：
2002-11-26
影响因子：
11.1
作者：
Staker, BL;Hjerrild, K;Stewart, L
通讯作者：
Stewart, L
影响因子：
7.3
作者：
Dallavalle, S;Ferrari, A;Zunino, F
通讯作者：
Zunino, F
影响因子：
2.7
作者：
Dallavalle, S;Ferrari, A;Zunino, F
通讯作者：
Zunino, F
影响因子：
7.3
作者：
Fan, Y;Weinstein, JN;Pommier, Y
通讯作者：
Pommier, Y
影响因子：
7.3
作者：
Dallavalle, S;Delsoldato, T;Zunino, F
通讯作者：
Zunino, F