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Start Over Author "Qian Shi" Topic adenocarcinoma Journal journal of medicinal chemistry

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1. Antitumor Agents 288: Design, Synthesis, SAR, and Biological Studies of Novel Heteroatom-Incorporated Antofine and Cryptopleurine Analogues as Potent and Selective Antitumor Agents.

Author

Xiaoming Yang, Qian Shi, Shuenn-Chen Yang, Chi-Yuan Chen, Sung-Liang Yu, Kenneth F. Bastow, Susan L. Morris-Natschke, Pei-Chi Wu, Chin-Yu Lai, Tian-Shung Wu, Shiow-Lin Pan, Che-Ming Teng, Jau-Chen Lin, Pan-Chyr Yang, and Kuo-Hsiung Lee

Subjects
*ANTINEOPLASTIC agents, *DRUG design, *STRUCTURE-activity relationship in pharmacology, *CANCER treatment, *BIOCHEMICAL mechanism of action, *CANCER cell growth, *LABORATORY mice, *ADENOCARCINOMA, *PREVENTION
Abstract

Novel heteroatom-incorporated antofine and cryptopleurine analogues were designed, synthesized, and tested against a panel of five cancer cell lines. Two new S-13-oxo analogues (11and 16) exhibited potent cell growth inhibition in vitro(GI50: 9 nM and 20 nM). Interestingly, both compounds displayed improved selectivity among different cancer cell lines, in contrast to the natural products antofine and cryptopleurine. Mechanism of action (MOA) studies suggested that R-antofine promotes dysregulation of DNA replication during early S phase, while no similar effects were observed for 11and 15on corresponding replication initiation complexes. Compound 11also showed greatly reduced cytotoxicity against normal cells and moderate antitumor activity against HT-29 human colorectal adenocarcinoma xenograft in mice without overt toxicity. [ABSTRACT FROM AUTHOR]

Published
2011
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