Cytotoxic activities of new jadomycin derivatives

Jian Ting Zheng; Uwe Rix; Lixia Zhao; Cynthia Mattingly; Val Adams; Quan Chen; Jürgen Rohr; Ke Qian Yang

doi:10.1038/ja.2005.51

Cytotoxic activities of new jadomycin derivatives

Jian Ting Zheng, Uwe Rix, Lixia Zhao, Cynthia Mattingly, Val Adams, Quan Chen, Jürgen Rohr, Ke Qian Yang

Research output: Contribution to journal › Article › peer-review

46 Scopus citations

Abstract

Cytotoxic activities of jadomycin B and five new jadomycin derivatives against four cancer cell lines (HepG2, IM-9, IM-9/Bcl-2 and H460) were evaluated. Jadomycin S was most potent against HepG2, IM-9 and IM-9/Bcl-2 while jadomycin F was most potent against H460. Their potencies correlated with the degrees of apoptosis induced. Structure-activity-relationship analyses clearly demonstrate that the side chains of the oxazolone ring derived from the incorporated amino acids make a significant impact on biological activity. Therefore, jadomycin offers an ideal scaffold to manipulate structure and could be exploited to make many novel bioactive compounds with altered activities.

Original language	English
Pages (from-to)	405-408
Number of pages	4
Journal	Journal of Antibiotics
Volume	58
Issue number	6
DOIs	https://doi.org/10.1038/ja.2005.51
State	Published - Jul 2005

Bibliographical note

Funding Information:
Acknowledgments We wish to thank Professor Xiu-Fen Kou for her assistance with purification methods, Mr. Li Xiao-Ming for his assistance with LC-MS analyses and Mrs. Wang Jing for her assistance operating flow cytometry. This work was supported by start-up funding from Institute of Microbiology and Chinese Academy of Sciences to KQY, and by the NIH and the Kentucky Lung Cancer Research Foundation to JR.

Keywords

Cytotoxic
Derivative
Jadomycin
Streptomyces venezuelae

ASJC Scopus subject areas

Pharmacology
Drug Discovery

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1038/ja.2005.51

Cite this

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title = "Cytotoxic activities of new jadomycin derivatives",

abstract = "Cytotoxic activities of jadomycin B and five new jadomycin derivatives against four cancer cell lines (HepG2, IM-9, IM-9/Bcl-2 and H460) were evaluated. Jadomycin S was most potent against HepG2, IM-9 and IM-9/Bcl-2 while jadomycin F was most potent against H460. Their potencies correlated with the degrees of apoptosis induced. Structure-activity-relationship analyses clearly demonstrate that the side chains of the oxazolone ring derived from the incorporated amino acids make a significant impact on biological activity. Therefore, jadomycin offers an ideal scaffold to manipulate structure and could be exploited to make many novel bioactive compounds with altered activities.",

keywords = "Cytotoxic, Derivative, Jadomycin, Streptomyces venezuelae",

author = "Zheng, {Jian Ting} and Uwe Rix and Lixia Zhao and Cynthia Mattingly and Val Adams and Quan Chen and J{\"u}rgen Rohr and Yang, {Ke Qian}",

note = "Funding Information: Acknowledgments We wish to thank Professor Xiu-Fen Kou for her assistance with purification methods, Mr. Li Xiao-Ming for his assistance with LC-MS analyses and Mrs. Wang Jing for her assistance operating flow cytometry. This work was supported by start-up funding from Institute of Microbiology and Chinese Academy of Sciences to KQY, and by the NIH and the Kentucky Lung Cancer Research Foundation to JR.",

year = "2005",

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doi = "10.1038/ja.2005.51",

language = "English",

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pages = "405--408",

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T1 - Cytotoxic activities of new jadomycin derivatives

AU - Zheng, Jian Ting

AU - Rix, Uwe

AU - Zhao, Lixia

AU - Mattingly, Cynthia

AU - Adams, Val

AU - Chen, Quan

AU - Rohr, Jürgen

AU - Yang, Ke Qian

N1 - Funding Information: Acknowledgments We wish to thank Professor Xiu-Fen Kou for her assistance with purification methods, Mr. Li Xiao-Ming for his assistance with LC-MS analyses and Mrs. Wang Jing for her assistance operating flow cytometry. This work was supported by start-up funding from Institute of Microbiology and Chinese Academy of Sciences to KQY, and by the NIH and the Kentucky Lung Cancer Research Foundation to JR.

PY - 2005/7

Y1 - 2005/7

N2 - Cytotoxic activities of jadomycin B and five new jadomycin derivatives against four cancer cell lines (HepG2, IM-9, IM-9/Bcl-2 and H460) were evaluated. Jadomycin S was most potent against HepG2, IM-9 and IM-9/Bcl-2 while jadomycin F was most potent against H460. Their potencies correlated with the degrees of apoptosis induced. Structure-activity-relationship analyses clearly demonstrate that the side chains of the oxazolone ring derived from the incorporated amino acids make a significant impact on biological activity. Therefore, jadomycin offers an ideal scaffold to manipulate structure and could be exploited to make many novel bioactive compounds with altered activities.

AB - Cytotoxic activities of jadomycin B and five new jadomycin derivatives against four cancer cell lines (HepG2, IM-9, IM-9/Bcl-2 and H460) were evaluated. Jadomycin S was most potent against HepG2, IM-9 and IM-9/Bcl-2 while jadomycin F was most potent against H460. Their potencies correlated with the degrees of apoptosis induced. Structure-activity-relationship analyses clearly demonstrate that the side chains of the oxazolone ring derived from the incorporated amino acids make a significant impact on biological activity. Therefore, jadomycin offers an ideal scaffold to manipulate structure and could be exploited to make many novel bioactive compounds with altered activities.

KW - Cytotoxic

KW - Derivative

KW - Jadomycin

KW - Streptomyces venezuelae

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SN - 0021-8820

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EP - 408

JO - Journal of Antibiotics

JF - Journal of Antibiotics

IS - 6

ER -

Cytotoxic activities of new jadomycin derivatives

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

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