Abstract:
:BPR0C305 is a novel N-substituted indolyl glyoxylamide previously reported with in-vitro cytotoxic activity against a panel of human cancer cells including P-gp-expressing multiple drug-resistant cell sublines. The present study further examined the underlying molecular mechanism of anticancer action and evaluated the in-vivo antitumor activities of BPR0C305. BPR0C305 is a novel synthetic small indole derivative that demonstrates in-vitro activities against human cancer cell growth by inhibiting tubulin polymerization, disrupting cellular microtubule assembly, and causing cell cycle arrest at the G2/M phase. It is also orally active against leukemia and solid tumor growths in mouse models. Findings of these pharmacological and pharmacokinetic studies suggest that BPR0C305 is a promising lead compound for further preclinical developments.
journal_name
Anticancer Drugsjournal_title
Anti-cancer drugsauthors
Li WT,Yeh TK,Song JS,Yang YN,Chen TW,Lin CH,Chen CP,Shen CC,Hsieh CC,Lin HL,Chao YS,Chen CTdoi
10.1097/CAD.0000000000000014subject
Has Abstractpub_date
2013-11-01 00:00:00pages
1047-57issue
10eissn
0959-4973issn
1473-5741journal_volume
24pub_type
杂志文章abstract::Long noncoding RNA (lncRNA) KTN1 antisense RNA 1 (KTN1-AS1) is a novel promoter in the progression of some cancers. However, the knowledge of its role in lung adenocarcinoma is still limited. The current study aimed to examine the biological functions of KTN1-AS1 and its coexpressed protein in lung adenocarcinoma. The...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000001035
更新日期:2021-01-22 00:00:00
abstract::1,4-Anthraquinone (AQ) was synthesized and shown to prevent L1210 leukemic cells from synthesizing macromolecules and growing in vitro. In contrast, its dihydroxy-9,10anthraquinone precursor, quinizarin, was inactive. The antitumor activity of AQ was compared to that of daunorubicin (DAU), which is structurally differ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200006000-00004
更新日期:2000-06-01 00:00:00
abstract::The primary objective was to determine the optimal doses for gemcitabine (prolonged infusion), liposomal doxorubicin (Myocet) and docetaxel as primary (neoadjuvant) chemotherapy for locally advanced breast cancer. Secondary objectives included evaluation of the safety and efficacy of the regimen. Patients (n=19) with ...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章,多中心研究
doi:10.1097/00001813-200501000-00003
更新日期:2005-01-01 00:00:00
abstract::The cytotoxic activity of bendamustine hydrochloride was evaluated against human ovarian and breast carcinoma cell lines including cell lines resistant to cisplatin and doxorubicin in vitro. The relative degree of resistance to bendamustine hydrochloride was lower in all cell lines compared with cyclophosphamide, melp...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199606000-00007
更新日期:1996-06-01 00:00:00
abstract::A functionalized poly(amidoamine) (PAMAM) nanocarrier was designed and prepared to deliver anticancer drugs. The nanocarrier is a copolymer with a core-shell structure with 3.0 G PAMAM as the core and sequentially conjugated poly(2-(N,N-diethylamino)ethyl methacrylate) (pDEA) and methoxy-poly(ethylene glycol) 2000 (mP...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32835920fa
更新日期:2013-02-01 00:00:00
abstract::Anti-tubulin couplets have activity in hormone-resistant prostate cancer. This study was designed to define the dose-limiting toxicity (DLT) and recommended phase II dose (RPTD) of the unique triplet combination of paclitaxel, estramustine phosphate (EMP) and vinorelbine (Pacl-E-Vin). Patients with advanced malignanci...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/00001813-200301000-00009
更新日期:2003-01-01 00:00:00
abstract::Mantle cell lymphoma (MCL) remains incurable for most patients, and proteasome inhibitors like bortezomib induce responses in a minority of patients with relapsed disease. Fenretinide is a retinoid that has shown preclinical activity in B-cell lymphomas. We hypothesized that these agents could yield augmented antitumo...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000274
更新日期:2015-10-01 00:00:00
abstract::The goal of our study was to determine whether an apoptosis assay used after short-term drug exposure could predict selective toxicity to cancer cells. To this end we compared the effect of eight anticancer drugs and 10 toxic compounds without known antitumor activity in cultures of human breast cancer cells and norma...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200308000-00008
更新日期:2003-08-01 00:00:00
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journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:10.1097/00001813-200309000-00003
更新日期:2003-09-01 00:00:00
abstract::A cost-utility analysis has been performed comparing taxanes, vinorelbine and standard therapy for metastatic breast cancer considering clinical efficacy, quality-adjusted-life-years (QALYs) and costs. A decision model has been built. Clinical efficacy data were collected by literature review. Utility data and cost da...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200107000-00007
更新日期:2001-07-01 00:00:00
abstract::The effect of association of hyperthermia with the anti-inflammatory drug rhein (RH), 4,5-dihydroxyanthraquinone-2-carboxylic acid, on the clonogenic activity of human glioma cells has been examined. RH inhibits neoplastic growth mainly through an ATP depletion, but thermal cell killing is not mediated by the drug-ind...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199208000-00015
更新日期:1992-08-01 00:00:00
abstract::Zoledronic acid has been the standard of care for the prevention of skeletal-related events in patients with bone metastases from prostate cancer for the past 10 years. However, its potent antitumor activity has been questioned. We report the occurrence of a complete clinical and biological response to zoledronic acid...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32834bede5
更新日期:2012-01-01 00:00:00
abstract::beta-Lapachone is a naturally occurring quinone obtained from the bark of the lapacho tree (Tabebuia avellanedae) with cancer chemopreventive properties. The objective of the present study was to investigate the effect of beta-lapachone on the cell growth and apoptosis in human colon carcinoma tumor cell line HCT-116....
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200311000-00011
更新日期:2003-11-01 00:00:00
abstract::This review focuses on the recent advances in chemotherapy of malignant gliomas, with special emphasis on the most common primary brain tumor in adults, glioblastoma. The demonstration of the superiority of concomitant and adjuvant temozolomide with standard radiotherapy over radiotherapy alone in patients with newly ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/CAD.0b013e32801476fd
更新日期:2007-07-01 00:00:00
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000070
更新日期:2014-04-01 00:00:00
abstract::The in vitro antitumor activity of navelbine (NVB, KW-2307), a newly synthesized vinca alkaloid, was compared with that of adriamycin (ADM) against human breast carcinomas inoculated into nude mice at the maximum tolerated dose (MTD) and clinically equivalent dose (CED). The plasma levels of NVB after intravenous inje...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199412000-00004
更新日期:1994-12-01 00:00:00
abstract::13,14-Dihydro-15-deoxy-Delta7-prostaglandin A1 methyl ester (TEI-9826), an antitumor prostaglandin analog, is a candidate for clinical trial. In the present study, we examined its biological stability in vitro, antitumor activity in vitro and in vivo, and pharmacokinetics. Although TEI-9826 was rapidly hydrolyzed to t...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200103000-00008
更新日期:2001-03-01 00:00:00
abstract::The current reference treatment of hormone-refractory prostate cancer consists mainly of chemotherapy with docetaxel. To improve the management of advanced prostate cancer, one should examine the benefits of adding other agents to docetaxel. We examined the growth inhibitory effects of a triple combination, including ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/01.cad.0000224444.23953.90
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e3281e4429d
更新日期:2007-10-01 00:00:00
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200203000-00008
更新日期:2002-03-01 00:00:00
abstract::Twelve patients received intrapleural instilments of the cytostatic agent mitoxantrone in a total dosage of 30 mg for locoregional palliative therapy of malignant pleural effusion. Effusion could be stopped for a mean period of 3.2 months in 11 patients. ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199202000-00003
更新日期:1992-02-01 00:00:00
abstract::Patients with advanced gastric cancer unresponsive or progressing after PELF chemotherapy (5-fluorouracil, leucovorin, cisplatin and epidoxorubicin) received paclitaxel at the dose of 225 mg/m2 every 3 weeks, over 3 h infusion. Thirty-six patients entered the study, and all of them were evaluable for response and toxi...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/00001813-199804000-00003
更新日期:1998-04-01 00:00:00
abstract::OncoGel is a novel depot formulation of paclitaxel designed for intralesional injection with a sustained paclitaxel delivery over approximately 6 weeks from a single administration. This phase 1 study was designed to characterize the toxicity, pharmacokinetics and preliminary antitumor activity associated with OncoGel...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e328011a51d
更新日期:2007-03-01 00:00:00
abstract::Gossypol [(2,2'-binaphthalene)-8,8'-dicarboxaldehyde-1,1',6,6',7,7'-hexahydroxy-5,5'-diisopropyl-3,3'-dimethyl] 1a is a naturally occurring compound extracted from the cotton plant and has been extensively studied as an oral male contraceptive. Its favorable toxicity profile, and the more recent demonstration of anti-...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200003000-00009
更新日期:2000-03-01 00:00:00
abstract::A lack of cross-resistance between the aromatase inhibitors (AIs) provides evidence to suggest that there are clinical differences between these agents. Available data from clinical trials indicate that patients exposed to nonsteroidal AIs may benefit from a steroidal compound of similar biochemical potency, and durab...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
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更新日期:2008-03-01 00:00:00
abstract::Apalutamide (ARN-509) is an antiandrogen that binds selectively to androgen receptors (AR) and does not show antagonist-to-agonist switch like bicalutamide. We compared the activity of ARN versus bicalutamide on prostate cancer cell lines. The 22Rv1, PC3, and DU145 cell lines were used to study the effect of ARN and b...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000592
更新日期:2018-04-01 00:00:00
abstract::Fibroblast growth factor-inducible 14 (Fn14) has been reported to play an oncogene role in many types of cancer. However, its biological functions in small-cell lung cancer (SCLC) remain unknown. The aim of this study is to investigate the roles of Fn14 in the cell growth and chemoresistance of SCLC and its possible m...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000153
更新日期:2014-11-01 00:00:00
abstract::The aim of this study was to establish xenograft models of tumor in mice bladder and evaluate the antitumor efficacy of ampelopsin sodium (Amp-Na). A total of 2×10 human bladder carcinoma EJ cells and murine sarcoma 180 cells were instilled into the bladder of BALB/c nu/nu mice and Swiss mice after preconditioning to ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32835019f9
更新日期:2012-07-01 00:00:00