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

^*此作品的通讯作者

化学与分子工程学院

科研成果: 期刊稿件 › 文章 › 同行评审

20 引用（Scopus）

摘要

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.

源语言	英语
页（从-至）	281-286
页数	6
期刊	European Journal of Medicinal Chemistry
卷	54
DOI	https://doi.org/10.1016/j.ejmech.2012.05.002
出版状态	已出版 - 8月 2012

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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",

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}

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

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