Synthesis and biological evaluation of new homocamptothecin analogs

Yu Luo; Shanbao Yu; Linjiang Tong; Qingqing Huang; Wei Lu; Yi Chen

doi:10.1016/j.ejmech.2012.05.002

Synthesis and biological evaluation of new homocamptothecin analogs

Yu Luo, Shanbao Yu, Linjiang Tong, Qingqing Huang, Wei Lu, Yi Chen

School of Chemistry and Molecular Engineering

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

20 Scopus citations

Abstract

In order to increase the stability of E-ring of homocamptothecins, the electron-withdrawing group -OH or -OAc was induced to α position of ring-E lactone. Ten new homocamptothecin analogs were synthesized. Most compounds showed potent in vitro anticancer activity and potent Topo I inhibition, which was equal or superior to that of CPT, SN-38 and 10-HCPT. The stability studies of this series also displayed significant improvement of the stability.

Original language	English
Pages (from-to)	281-286
Number of pages	6
Journal	European Journal of Medicinal Chemistry
Volume	54
DOIs	https://doi.org/10.1016/j.ejmech.2012.05.002
State	Published - Aug 2012

Keywords

Anticancer drugs
Camptothecin
Electron-withdrawing group
Homocamptothecin

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10.1016/j.ejmech.2012.05.002

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title = "Synthesis and biological evaluation of new homocamptothecin analogs",

abstract = "In order to increase the stability of E-ring of homocamptothecins, the electron-withdrawing group -OH or -OAc was induced to α position of ring-E lactone. Ten new homocamptothecin analogs were synthesized. Most compounds showed potent in vitro anticancer activity and potent Topo I inhibition, which was equal or superior to that of CPT, SN-38 and 10-HCPT. The stability studies of this series also displayed significant improvement of the stability.",

keywords = "Anticancer drugs, Camptothecin, Electron-withdrawing group, Homocamptothecin",

author = "Yu Luo and Shanbao Yu and Linjiang Tong and Qingqing Huang and Wei Lu and Yi Chen",

year = "2012",

month = aug,

doi = "10.1016/j.ejmech.2012.05.002",

language = "英语",

volume = "54",

pages = "281--286",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

}

TY - JOUR

T1 - Synthesis and biological evaluation of new homocamptothecin analogs

AU - Luo, Yu

AU - Yu, Shanbao

AU - Tong, Linjiang

AU - Huang, Qingqing

AU - Lu, Wei

AU - Chen, Yi

PY - 2012/8

Y1 - 2012/8

N2 - In order to increase the stability of E-ring of homocamptothecins, the electron-withdrawing group -OH or -OAc was induced to α position of ring-E lactone. Ten new homocamptothecin analogs were synthesized. Most compounds showed potent in vitro anticancer activity and potent Topo I inhibition, which was equal or superior to that of CPT, SN-38 and 10-HCPT. The stability studies of this series also displayed significant improvement of the stability.

AB - In order to increase the stability of E-ring of homocamptothecins, the electron-withdrawing group -OH or -OAc was induced to α position of ring-E lactone. Ten new homocamptothecin analogs were synthesized. Most compounds showed potent in vitro anticancer activity and potent Topo I inhibition, which was equal or superior to that of CPT, SN-38 and 10-HCPT. The stability studies of this series also displayed significant improvement of the stability.

KW - Anticancer drugs

KW - Camptothecin

KW - Electron-withdrawing group

KW - Homocamptothecin

UR - https://www.scopus.com/pages/publications/84864415641

U2 - 10.1016/j.ejmech.2012.05.002

DO - 10.1016/j.ejmech.2012.05.002

M3 - 文章

C2 - 22647222

AN - SCOPUS:84864415641

SN - 0223-5234

VL - 54

SP - 281

EP - 286

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Synthesis and biological evaluation of new homocamptothecin analogs

Abstract

Keywords

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