A novel temozolomide analog, NEO212, with enhanced activity against MGMT-positive melanoma in vitro and in vivo

Highlights • Temozolomide was modified by conjugation to perillyl alcohol. • The resulting novel analog, NEO212, exerted superior activity against melanoma. • NEO212 was also active against drug-resistant tumors in vivo. • NEO212 should be developed for clinical use.

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Bibliographic Details
Published in:Cancer letters 2015-03, Vol.358 (2), p.144-151
Main Authors: Chen, Thomas C, Cho, Hee-Yeon, Wang, Weijun, Nguyen, Jenny, Jhaveri, Niyati, Rosenstein-Sisson, Rachel, Hofman, Florence M, Schönthal, Axel H
Format: Article
Language:English
Subjects:
Alcohol
Alcohols
Alkylation
Animals
Antineoplastic Agents, Alkylating - administration & dosage
Antineoplastic Agents, Alkylating - pharmacology
Antineoplastic Agents, Alkylating - toxicity
Antitumor activity
Apoptosis
Apoptosis - drug effects
Brain cancer
Cancer therapies
Cell culture
Cell death
Cell Line, Tumor
Cell Survival - drug effects
Chemoresistance
Cytotoxicity
Dacarbazine - administration & dosage
Dacarbazine - analogs & derivatives
Dacarbazine - pharmacology
Dacarbazine - toxicity
Deoxyribonucleic acid
Disease Models, Animal
DNA
DNA damage
DNA Damage - drug effects
DNA Methylation - drug effects
DNA methyltransferase
Dose-Response Relationship, Drug
Guanine
Hematology, Oncology and Palliative Medicine
Humans
Inhibitory Concentration 50
Investigations
Kinases
Laboratories
Melanoma
Melanoma - drug therapy
Melanoma - metabolism
Melanoma - pathology
Metastasis
MGMT
Mice
O-Methylguanine-DNA Methyltransferase - metabolism
O6-methylguanine-DNA methyltransferase
Perillyl alcohol
Proteins
Temozolomide
Tumor Burden - drug effects
Tumor cells
Tumors
Xenograft Model Antitumor Assays
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Description
Summary:Highlights • Temozolomide was modified by conjugation to perillyl alcohol. • The resulting novel analog, NEO212, exerted superior activity against melanoma. • NEO212 was also active against drug-resistant tumors in vivo. • NEO212 should be developed for clinical use.
ISSN:0304-3835
1872-7980
DOI:10.1016/j.canlet.2014.12.021