Abstract:
:Methoxymorpholinyl doxorubicin (PNU 152243) is a morpholinyl analog possessing a methoxymorpholinyl group at the 3' position of the sugar moiety, which, compared with doxorubicin, appears to be less cardiotoxic and more cytotoxic against multidrug-resistant tumor cells. In this study, we report the anticancer activity of PNU 152243 on human hepatocellular carcinoma (HCC) in vitro and in vivo. The average IC50 value of PNU was 0.08 microM. In contrast, the average IC50 values of adriamycin (ADM), 4'-epidoxorubicin (EDR), mitomycin C (MMC), cisplatin and vepesid (VP-16) were 0.96, 0.74, 2.81, 7.27 and 26.66 microM, respectively. PNU 152243 was 13.7, 10.6, 40.1, 103.8 and 380.8 times more potent than ADM, EDR, MMC, cisplatin and VP-16 against HCC in vitro. In nude mice, the T/C (%) were 43.8 at the dose of 25 microg/kg and 41.2 at the dose of 50 microg/kg on BEL-7402 xenograft, the T/C (%) were 41.7 at the dose of 25 microg/kg and 54.6 at the dose of 50 microg/kg on Zip-177 xenograft. The results showed that PNU 152243 had growth inhibition of HCC in vitro and in vivo and may be useful in HCC chemotherapy.
journal_name
Anticancer Drugsjournal_title
Anti-cancer drugsauthors
Yuan S,Zhang X,Lu L,Xu C,Yang W,Ding Jdoi
10.1097/01.cad.0000132238.23050.f5subject
Has Abstractpub_date
2004-07-01 00:00:00pages
641-6issue
6eissn
0959-4973issn
1473-5741pii
00001813-200407000-00016journal_volume
15pub_type
杂志文章abstract::The antitumor effect and tumor levels of 5-fluoro-2'-deoxyuridylate (FdUMP) following oral administration of tetradecyl 2'-deoxy-5-fluoro-5'-uridylate (TT-62) were compared with those attained following intravenous (i.v.) or intraperitoneal (i.p.) administration of 5-fluorouracil (5-FU) or 5-fluoro-2'-deoxyuridine (FU...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199206000-00013
更新日期:1992-06-01 00:00:00
abstract::Since 5-fluorouracil (5-FU) was synthesized in the late 1950s it has become an important component of many anticancer treatment regimens. The increasing volume of literature accumulating about this drug is evidence that the optimal administration schedule and its combination with modulators has yet to be determined. M...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/00001813-199406000-00002
更新日期:1994-06-01 00:00:00
abstract::Although 5-fluorouracil (5-FU) has been used to treat breast and colorectal cancers for several decades, bolus 5-FU has disappointing efficacy. Prolonged infusion schedules and biomodulation with leucovorin have resulted in improved response rates, but these have not translated into significant improvements in surviva...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/00001813-200109000-00001
更新日期:2001-09-01 00:00:00
abstract::5-Fluorouracil, usually in combination with folinic acid, is widely used in the treatment of both colorectal and head and neck squamous cell cancer patients. Since 5-fluorouracil plus folinic acid and the antifolate thymidylate synthase inhibitor; raltitrexed have distinct mechanisms of action and toxicity profiles, w...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32809ef9b7
更新日期:2007-08-01 00:00:00
abstract::High expression of vascular endothelial growth factor (VEGF) in patients with breast cancer has been associated with a poor prognosis, indicating that VEGF could be linked to the efficacy of chemotherapy and radiotherapy. It has also been suggested that radiation resistance is partly due to tumour cell production of a...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32834ea5b3
更新日期:2012-06-01 00:00:00
abstract::Caffeic acid phenethyl ester (CAPE) is a major propolis component that possesses a variety of pharmacological properties such as antioxidant and anticancer effects. Herein, we investigated the effectiveness of CAPE on cytotoxicity of clinically used anticancer drugs, doxorubicin (DXR) and cisplatin (CDDP), in parental...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000715
更新日期:2019-03-01 00:00:00
abstract::In a retrospective study, we calculated the treatment and follow-up costs of patients with newly diagnosed multiple myeloma. The total treatment programme consisted of eight phases: VAD or VAMP chemotherapy, follow-up I, high-dose melphalan followed by transplantation of whole blood, follow-up II, collection of periph...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199811000-00008
更新日期:1998-11-01 00:00:00
abstract::We examined the anti-tumor activity and structure-activity requirements of omega-hydroxy fatty acids (omega-HFAs) on the human melanoma cell line G361. The omega-hydroxystearic acid (omega-HSA) had strong growth-inhibiting and cytotoxic activity. Although omega-hydroxypalmitic acid (omega-HPA) also had growth-inhibiti...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200506000-00010
更新日期:2005-06-01 00:00:00
abstract::Extrachromosomal DNA is the predominant form of gene amplification in human tumors. Hydroxyurea (HU) concentrations of 100-150 microM have been promising in vitro for extrachromosomal DNA elimination. The study objective was to determine the HU dose-concentration relationship in nude mice with HU doses from 0 to 200 m...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199410000-00009
更新日期:1994-10-01 00:00:00
abstract::Treatment of mammalian cells with chemotherapeutic drugs can result in perturbations of nucleotide pools. Monitoring these perturbations in cultured tumor cells from human sources is useful for assessment of the effect of drug therapy and a better understanding of the mechanism of action of these drugs. In this study,...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000096
更新日期:2014-07-01 00:00:00
abstract::Trichostatin A and helixor A increased thrombospondin-1 expression by ECV304 cells at both mRNA and protein levels by transcriptional activation through the enhancement of tsp-1 promoter activity. The induction of thrombospondin-1 by these agents potently reduced ECV 304 cell migration and capillary-like tube formatio...
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
abstract::This study examined the growth inhibitory effects of combining 1,25-dihydroxyvitamin D3 (calcitriol) with retinoic acid or dexamethasone against cultured breast and ovarian carcinoma cells. Retinoic acid (12.5-50 nM) increased the effectiveness of calcitriol (12.5-50 nM) against MCF-7 and NIH:OVCAR3 cells, with synerg...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199508000-00009
更新日期:1995-08-01 00:00:00
abstract::The sap of Euphorbia peplus, commonly know as 'petty spurge', 'radium weed' or 'milkweed' has been used for centuries as a traditional treatment for skin conditions, including warts, corns and cancers of the skin. Documentation of its use by medical professionals to treat basal cell carcinoma (BCC) dates from the earl...
journal_title:Anti-cancer drugs
pub_type:
doi:10.1097/CAD.0b013e3280149ec5
更新日期:2007-03-01 00:00:00
abstract::Organotypic cultures of human A549 cells were used as a tumor model to investigate sequence effects for combination treatments with adriamycin (ADR) and X-irradiation. Initial drug exposure led to the greatest cytotoxic effect especially when X-rays were delivered 24 h later and this subsequent irradiation did not sig...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199204000-00010
更新日期:1992-04-01 00:00:00
abstract::Silibinin, with a strong antioxidant activity and a weak cytotoxic property, is considered a candidate for cancer prevention. As there is no information on its effect on breast cancer tumor-initiating cells [cancer stem cells (CSCs)] in a 3D culture model, which more closely mimic natural tissues, we carried out this ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000205
更新日期:2015-06-01 00:00:00
abstract::In a previous study, we showed that a combination of an oral fluoropyrimidine anticancer agent (S-1) and gemcitabine (GEM) had synergistic effects on cell growth and cell cycle arrest in the pancreatic cancer cell line MIA PaCa-2. Therefore, we conducted further mechanistic studies using the pancreatic cancer cell lin...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e328350e8c7
更新日期:2012-06-01 00:00:00
abstract::CHS 828, a pyridyl cyanoguanidine, is a new drug candidate now in phase I/II trials, that has shown promising anticancer activity in experimental tumor models and primary cultures of cancer cells from patients. In this study the fluorometric microculture cytotoxicity assay was used for evaluation of CHS 828 in primary...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200208000-00008
更新日期:2002-08-01 00:00:00
abstract::We have previously reported the cytotoxic effects of chalcone A1, derived from 1-naphthaldehyde, in leukemia cell lines. On the basis of these findings, the main aim of this study was to elucidate some of the molecular mechanisms involved in apoptosis induced by chalcone A1 toward K562 and Jurkat cells. In both cell l...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000384
更新日期:2016-09-01 00:00:00
abstract::Verapamil, cyclosporin A (CsA), the cyclosporin derivative SDZ PSC 833 and the novel cyclopeptolide SDZ 280-446 were tested for their capacity to chemosensitize a P-glycoprotein (Pgp)-expressing multi-drug resistant (MDR) variant of the CEM human T lymphoblastoid cell subline (CCRF ACTD 400+). That MDR-CEM cell sublin...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:
更新日期:1993-12-01 00:00:00
abstract::The antitumor effect of etoposide (ETO) may be related to duration of exposure to a relatively low serum level while myelosuppression may be dependent on peak ETO serum levels. With regard to such therapeutic ranges, duration of exposure to predefined plasma ETO concentration ranges and the related AUC (expressed as p...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/00001813-199910000-00003
更新日期:1999-10-01 00:00:00
abstract::Tafluposide (F 11782), a novel epipodophylloid with a unique mechanism of interaction with both topoisomerase I and II, has shown outstanding antitumor activity in vivo against a panel of experimental human tumor xenografts. The aim of this study was to evaluate its cytotoxicity against fresh tumor cells taken from pa...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200307000-00013
更新日期:2003-07-01 00:00:00
abstract::Human colon cancer SW480 cells express the c-myc gene. On the other hand, SW480DDP cell lines resistant to cisplatin exhibited decreased c-myc gene expression, but their cell growth rates remained similar to those of their parental cells. Antisense oligonucleotides to c-myc inhibited c-myc expression and induced incre...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200111000-00006
更新日期:2001-11-01 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::In melanoma, the RAS/RAF/MEK/ERK pathway is frequently activated by mutations in BRAF and NRAS. Selumetinib (AZD6244) is an oral, selective, non-ATP-competitive inhibitor of MEK1/2. Here, we describe a patient with metastatic melanoma (T1N2cM1a) with a BRAF V600E mutation. She is currently being treated with selumetin...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e328350737d
更新日期:2012-08-01 00:00:00
abstract::The antitumor action of bestatin is considered to be an indirect action mediated by T-cells. Therefore, we investigated the effects of bestatin on the differentiation and proliferation of human precursor T-cells using a colony formation technique. Bestatin did not increase the overall number of T-cell colonies, but it...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199102000-00005
更新日期:1991-02-01 00:00:00
abstract::Tumor-to-tumor metastasis is a rare phenomenon, with around 150 cases being reported in the literature. Breast cancer is the second most commonly reported donor tumor after lung cancer, but thymic epithelial tumors have never been reported as recipient tumors. Furthermore, the thymus is rarely affected by metastases. ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e328362a68b
更新日期:2013-08-01 00:00:00
abstract::The aim of this study was to evaluate whether radiolabeled iodoerythronitroimidazole (IETNIM) could predict the radiosensitization effect on tumors. Tumor-bearing mice were irradiated at a dose of 25, 31 and 37 Gy after the injection of IETNIM. They were also exposed to 37 Gy radiation at 35, 70, 140 and 240 min after...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199611000-00007
更新日期:1996-11-01 00:00:00
abstract::Taxanes have had a profound impact on the management of genitourinary tumors. In the perioperative and metastatic setting in bladder cancer, taxanes such as paclitaxel have an established role in combination chemotherapy strategies to improve survival. In metastatic prostate cancer, docetaxel was the only treatment, u...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/CAD.0000000000000088
更新日期:2014-05-01 00:00:00
abstract::Cancer cell resistance to chemotherapy is associated with a poor prognosis. The compound 2-deoxy-D-glucose (2-DG) enhances the effect of chemotherapy against cancer cells lines in vitro and in vivo. However, its effect on the epithelial to mesenchymal transition (EMT) in drug-resistant cancer cells has not been fully ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000472
更新日期:2017-04-01 00:00:00
abstract::Colchicine, the main alkaloid of the poisonous plant meadow saffron (Colchicum autumnale L.), is a classical drug used for the treatment of gout and familial Mediterranean fever. Although colchicine is not clinically used to treat cancer because of toxicity, it exerts antiproliferative effects through the inhibition o...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/CAD.0000000000000464
更新日期:2017-03-01 00:00:00