Synthesis and biological evaluation of tetrahydro-beta-carline derivatives.
- Author:
Xiu-Qin RUAN
1
;
Qi-Dong YOU
;
Lei YANG
;
Wu-Tong WU
Author Information
1. Key Laboratory of Carcinogenesis and Intervention of Jiangsu Province, China Pharmaceutical University, Nanjing 210009, China.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Carbolines;
chemical synthesis;
chemistry;
pharmacology;
Kinesin;
antagonists & inhibitors;
metabolism;
Molecular Structure
- From:
Acta Pharmaceutica Sinica
2008;43(8):828-832
- CountryChina
- Language:Chinese
-
Abstract:
Kinesin spindle protein (KSP/Eg5) is essential for the formation and maintenance of bipolar spindles during mitosis. Inhibition of this protein leads to cell cycle arrest and apoptosis without interfering other microtubule-dependent processes. Therefore, it is a potential target in cancer therapy. Here, a series of tetrahydro-beta-carboline derivatives 5a - k were synthesized as kinesin spindle protein inhibitor. Their structures were confirmed with 1H NMR, ESI-MS and elemental analysis. The synthesized compounds were evaluated for their inhibition of KSP.
