title: Newly synthesized anticancer drug HUHS1015 is effective on malignant pleural mesothelioma.
abstract: The newly synthesized naftopidil analogue HUHS1015 reduced cell viability in malignant pleural mesothelioma cell lines MSTO-211H, NCI-H28, NCI-H2052, and NCI-H2452, with the potential greater than that for the anticancer drugs paclitaxel or cisplatin at concentrations higher than 30 μM. HUHS1015 induced both necrosis and apoptosis of MSTO-211H and NCI-H2052 cells. HUHS1015 upregulated expression of mRNAs for Puma, Hrk, and Noxa in MSTO-211H and NCI-H2052 cells, suggesting HUHS1015-induced mitochondrial apoptosis. HUHS1015 clearly suppressed tumor growth in mice inoculated with NCI-H2052 cells. Taken together, the results of the present study indicate that HUHS1015 could be developed as an effective anticancer drug for treatment of malignant pleural mesothelioma.
authors.affiliation: Division of Bioinformation, Department of Physiology, Hyogo College of Medicine, Nishinomiya, Japan.
authors.forename: Yoshiko
authors.initials: Y
authors.lastname: Kaku
authors.forename: Hisao
authors.initials: H
authors.lastname: Nagaya
authors.forename: Ayako
authors.initials: A
authors.lastname: Tsuchiya
authors.forename: Takeshi
authors.initials: T
authors.lastname: Kanno
authors.forename: Akinobu
authors.initials: A
authors.lastname: Gotoh
authors.forename: Akito
authors.initials: A
authors.lastname: Tanaka
authors.forename: Tadashi
authors.initials: T
authors.lastname: Shimizu
authors.forename: Syuhei
authors.initials: S
authors.lastname: Nakao
authors.forename: Chiharu
authors.initials: C
authors.lastname: Tabata
authors.forename: Takashi
authors.initials: T
authors.lastname: Nakano
authors.forename: Tomoyuki
authors.initials: T
authors.lastname: Nishizaki
mesh_terms: D000814:Aniline Compounds / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D051017:Apoptosis Regulatory Proteins / Q000235:genetics; D045744:Cell Line, Tumor / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D008297:Male; D008654:Mesothelioma / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D000086002:Mesothelioma, Malignant; D051379:Mice; D008807:Mice, Inbred BALB C; D010997:Pleural Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D011412:Propanolamines / Q000494:pharmacology*; D011518:Proto-Oncogene Proteins / Q000235:genetics; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000235:genetics; D015854:Up-Regulation / Q000187:drug effects
chemical_list: C586405:1-(2-(2-methoxyphenylamino)ethylamino)-3-(naphthalene-1-yloxy)propan-2-ol; D000814:Aniline Compounds; D000970:Antineoplastic Agents; D051017:Apoptosis Regulatory Proteins; C438378:BBC3 protein, human; C484586:HRK protein, human; C498702:PMAIP1 protein, human; D011412:Propanolamines; D011518:Proto-Oncogene Proteins; D019253:Proto-Oncogene Proteins c-bcl-2
keywords: Apoptosis; Bcl-2 family; HUHS1015; malignant pleural mesothelioma; synthetic anticancer compound
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