alexa Z-GP Modification to CI-994, a Histone Deacetylase Inhibitor and the Application in Targeting Carcinoma Chemotherapy | OMICS International | Abstract
ISSN: 2161-0444

Medicinal Chemistry
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Research Article

Z-GP Modification to CI-994, a Histone Deacetylase Inhibitor and the Application in Targeting Carcinoma Chemotherapy

Yuanyuan Deng1, Peipei Gao2, Cuiping Guo2, Long Wu1, Jun Xu4, Heru Chen2,3* and Shao-hui Cai1*

1Department of Clinical Pharmacology, College of Pharmacy, Jinan University, Guangzhou 510632, P. R. China

2Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, P. R. China

3Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Guangzhou 510632, P. R. China

4College of Medicine, Jinan University, Guangzhou 510632, P. R. China

*Corresponding Author:
Shao-hui Cai
Department of Clinical Pharmacology
College of Pharmacy, Jinan University
Guangzhou 510632, P. R. China
E-mail: [email protected]

Heru Chen
Institute of Traditional Chinese Medicine and Natural Products
College of Pharmacy, Jinan University
Guangzhou 510632, P. R. China
E-mail: [email protected]

Received date: April 25, 2013; Accepted date: May 24, 2013; Published date: May 27, 2013

Citation: Deng Y, Gao P, Guo C, Wu L, Xu J, et al. (2013) Z-GP Modification to CI- 994, a Histone Deacetylase Inhibitor and the Application in Targeting Carcinoma Chemotherapy. Med chem 3:199-205. doi:10.4172/2161-0444.1000139

Copyright: © 2013 Deng Y, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Abstract

An adduct, namely (S)-4-acetamido-N-(2-(N-benzyloxycarbonyl- glycylprolyl)aminophenyl)benzamide (Z-GPCI- 994) has been designed and synthesized. All the evidences disclose that Z-GP-CI-994 is not the substrate of fibroblast activation protein-α (FAPα). However, the adduct is the substrate of another unknown enzyme which is ubiquitous in tumor tissue. The cytotoxicity of the adduct against HepG2, A549 and NIH3T3 cell lines is apparently decreased when compared to that of the parent compound (CI-994). Additionally, the inhibition rate of Z-GP-CI-994 on histone deacetylase is significantly lower than that of CI-994. All the results suggest preliminarily that Z-GP-CI-994 is promising to achieve enzyme-targeting delivery and to reduce systemic toxicity.

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