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Design, synthesis and potent cytotoxic activity of novel 7-(N-[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives.

ABSTRACT: 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 ?M to nM level, most of the new analogues showed greater cytotoxicity activity than the reference compounds irinotecan and topotecan. Furthermore, compounds 12l (IC50, 1.2nM) and 12k (IC50, 20.2nM) 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.

SUBMITTER: Zhu GX 

PROVIDER: S-EPMC5512430 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature

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Design, synthesis and potent cytotoxic activity of novel 7-(N-[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives.

Zhu Gao-Xiang GX   Cheng Pi-Le PL   Goto Masuo M   Zhang Na N   Morris-Natschke Susan L SL   Hsieh Kan-Yen KY   Yang Guan-Zhou GZ   Yang Qian-Ru QR   Liu Ying-Qian YQ   Chen Hai-Le HL   Zhang Xiao-Shuai XS   Lee Kuo-Hsiung KH  

Bioorganic & medicinal chemistry letters 20170228 8

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 IC<sub>50</sub> values in the low μM to nM level, most of the new analogues showed greater cytotoxicity activity than the reference compounds irinoteca  ...[more]

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