Synthesis and characterization of a new retinoic acid ECPIRM as potential chemotherapeutic agent for human cutaneous squamous carcinoma

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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Synthesis and characterization of a new retinoic acid ECPIRM as potential chemotherapeutic agent for human cutaneous squamous carcinoma



Anti-Cancer Agents in Medicinal Chemistry, 15(9): 1204-1212.

Author(s): Mengli Zhang, Yue Tao, Pengcheng Ma, Dechuan Wang, Chundi He, Yuping Cao, Jun Wei, Lingjun Li and Lei Tao.

Affiliation: Institute of Dermatology, Chinese Academy of Medical Sciences, Peking Union Medical College, 12 jiang-wang-miao street, Nanjing 210042, China.

Abstract

Cutaneous squamous cell carcinoma (CSCC) is one of the most common cancers worldwide, requiring effective therapeutic interventions. Retinoids are important chemopreventive and therapeutic agents for a variety of human cancers including CSCC. In this study we synthesized a novel retinoic derivative N-(4-ethoxycarbonylphenyl) isoretinamide (ECPIRM) and evaluated its biological activities and possible mechanisms in human cutaneous squamous cell lines. ECPIRM had better inhibitory effect on the proliferation of squamous carcinoma cells SCL-1 and colo-16, compared with All-trans retinoic acid and 13-cis retinoic acid. ECPIRM had less toxicity to normal keratinocyte cell line HaCaT. Mechanistically, ECPIRM induced G1 cell cycle arrest in SCL-1 cells, via the downregulation of CDK2, CDK4, cycling D1 and cyclin E expression and upregulation of p21. In addition, these effects were at least partially due to the inhibition of JNK/ ERK-AP-1 signaling pathway by ECPIRM. Importantly, these effects of ECPIRM are independent of the classical retinoid receptor pathway, suggesting that the novel compound will have less side-effects in chemotherapy. These findings demonstrate that ECPIRM is a potential inhibitor of MPAK-AP-1 pathway, and is a potential therapeutic agent against CSCC.




Keywords:

AP-1, cell cycle arrest, cutaneous squamous cell carcinoma, ECPIRM, MAPK, N-(4-ethoxycarbonylphenyl) isoretinamide.



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Article Details

Volume: 15
Issue Number: 9
First Page: 1204
Last Page: 1212
Page Count: 9
DOI: 10.2174/1871520615666150520142719
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