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Molecules 2016, 21(11), 1581; doi:10.3390/molecules21111581

Semisynthetic and SAR Studies of Amide Derivatives of Neocrotocembraneic Acid as Potential Antitumor Agents

1
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China
2
School of Life Science and Engineering, Southwest University of Science and Technology, Mianyang 621010, China
*
Author to whom correspondence should be addressed.
Academic Editor: Maria Emília de Sousa
Received: 13 October 2016 / Revised: 9 November 2016 / Accepted: 17 November 2016 / Published: 19 November 2016
(This article belongs to the Section Medicinal Chemistry)
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Abstract

A series of novel amide derivatives of cembranoid neocrotocembraneic acid were designed and synthesized. The antiproliferative activities of these derivatives were evaluated against three human tumor cell lines (the human cervical cancer cell line HeLa, chronic myeloid leukemia cell line K562 and leukemia multidrug-resistant cell line K562/A02). Some of the synthesized compounds exhibited moderate to good activity against all three cancer cell lines. Particularly, compound 8a exhibited more potent antiproliferative activity than the reference drug etoposide against drug-resistant cell line K562/A02, indicating that it possessed a great potential for further development as a multidrug resistance modulator by structural modification. View Full-Text
Keywords: cembranoid type diterpene; neocrotocembraneic acid; structural modification; antitumor activity; anti-multidrug resistance cembranoid type diterpene; neocrotocembraneic acid; structural modification; antitumor activity; anti-multidrug resistance
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Shang, H.; Li, L.-Y.; Cheng, W.-H.; Luo, J.; Zhang, H.-W.; Zou, Z.-M. Semisynthetic and SAR Studies of Amide Derivatives of Neocrotocembraneic Acid as Potential Antitumor Agents. Molecules 2016, 21, 1581.

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