Isolation of two cellular lines resistant to ribonucleotide reductase inhibitors to investigate the inhibitory activity of 2,2'-bipyridyl-6-carbothioamide.


:The mechanism of action of a synthetic compound--2,2'-bipyridyl-6-carbothioamide--was investigated by developing tumor lines resistant to it (P388-R1.5 and P388-R4). P388-R4 is resistant to inhibitors of ribonucleotide reductase (RR) while no resistance was observed to antitumor drugs having other targets (except to bleomycin). The resistance to inhibitors of the RR M2 subunit is higher than that to compounds active on the RR M1 subunit. Moreover, murine chromosome 12, in which the M2 structural gene was recently localized, was trisomic in the resistant lines. We conclude that it is possible to consider BPYTA a new inhibitor of the RR M2 subunit.


Anticancer Drugs


Anti-cancer drugs


Nocentini G,Federici F,Armellini R,Franchetti P,Barzi A




Has Abstract


1990-12-01 00:00:00












  • A clinical armamentarium of marine-derived anti-cancer compounds.

    abstract::The sea, covering 70% of the Earth's surface, offers a considerably broader spectrum of biological diversity than terra firma. Containing approximately 75% of all living organisms, the marine environment offers a rich source of natural products with potential therapeutic application. Marine organisms have evolved the ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审


    authors: Jimeno JM

    更新日期:2002-05-01 00:00:00

  • Neoadjuvant TPF in locally advanced head and neck cancer can be followed by radiotherapy combined with cisplatin or cetuximab: a study of 157 patients.

    abstract::Neoadjuvant TPF (docetaxel, cisplatin, 5-fluorouracil), followed by radiotherapy or chemoradiotherapy with weekly carboplatin, increases overall survival and organ preservation. We assessed whether TPF could be used in routine practice and whether radiotherapy potentiated with cisplatin or cetuximab was feasible and c...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,多中心研究


    authors: Fayette J,Bonnin N,Ferlay C,Lallemant B,Ramade A,Favrel V,Zrounba P,Chabaud S,Pommier P,Poupart M,Céruse P

    更新日期:2013-07-01 00:00:00

  • Chemosensitization and drug accumulation effects of VX-710, verapamil, cyclosporin A, MS-209 and GF120918 in multidrug resistant HL60/ADR cells expressing the multidrug resistance-associated protein MRP.

    abstract::Overexpression of the multidrug resistance MDR1 gene product P-glycoprotein and/or the multidrug resistance-associated protein MRP confers multidrug resistance to cancer cells. The pipecolinate derivative VX-710 has previously been demonstrated to reverse MDR1-mediated multidrug resistance at concentrations of 0.5-2.5...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Germann UA,Ford PJ,Shlyakhter D,Mason VS,Harding MW

    更新日期:1997-02-01 00:00:00

  • Potential antineoplastic activity of keto-C-glycosides--a new family of cytostatic agents.

    abstract::We have examined the biological activity of keto-C-glycosides (KCGs), a new family of drugs displaying antiproliferative and cytotoxic properties on tumor cells. KCG1, the most powerful drug tested on epithelial derived neoplastic cells, was 25-125 times more cytostatic on epithelial cells than on lymphoma. By contras...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Bennani-Baïti MI,Lafarge-Frayssinet C,Herscovici J,Monserret R,Antonakis K,Frayssinet C,Uriel J

    更新日期:1992-08-01 00:00:00

  • Malignant phenotype of renal cell carcinoma cells is switched by ukrain administration in vitro.

    abstract::We investigated whether Ukrain modulates the malignant phenotype of clear cell renal cell carcinoma (ccRCC) cells Caki-1, Caki-2, and ACHN treated with four doses (5, 10, 20, and 40 μmol/l) for 24 and 48 h. The epithelial-to-mesenchymal transition markers E-cadherin, β-catenin, and vimentin were analyzed by immunofluo...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Gagliano N,Pettinari L,Aureli M,Martinelli C,Colombo E,Costa F,Carminati R,Volpari T,Colombo G,Milzani A,Dalle-Donne I,Gioia M

    更新日期:2011-09-01 00:00:00

  • The marine alkaloid naamidine A promotes caspase-dependent apoptosis in tumor cells.

    abstract::Apoptosis is important for normal development and removal of damaged cells. Evasion of apoptosis by cancer cells is one of the key characteristics of many tumor types. Thus, discovering agents that promote apoptosis in tumor cells could have great therapeutic value. Marine natural products have demonstrated great pote...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: LaBarbera DV,Modzelewska K,Glazar AI,Gray PD,Kaur M,Liu T,Grossman D,Harper MK,Kuwada SK,Moghal N,Ireland CM

    更新日期:2009-07-01 00:00:00

  • Phase II study of miltefosine 6% solution as topical treatment of skin metastases in breast cancer patients.

    abstract::Topical treatment of skin metastases with a cytotoxic agent is attractive for its easy self-administration and absence of major systemic interference. Miltefosine exerts its cytotoxicity by acting on cell membrane phospholipids and can be administered topically. Twenty breast cancer patients with progression of skin m...

    journal_title:Anti-cancer drugs

    pub_type: 临床试验,杂志文章


    authors: Smorenburg CH,Seynaeve C,Bontenbal M,Planting AS,Sindermann H,Verweij J

    更新日期:2000-11-01 00:00:00

  • Ex vivo effects of the dual topoisomerase inhibitor tafluposide (F 11782) on cells isolated from fresh tumor samples taken from patients with cancer.

    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


    authors: Sargent JM,Elgie AW,Williamson CJ,Hill BT

    更新日期:2003-07-01 00:00:00

  • Phase II trial of infusional fluorouracil, leucovorin, oxaliplatin, and irinotecan (FOLFOXIRI) as first-line treatment for advanced gastric cancer.

    abstract::The efficacy of chemotherapy for advanced gastric cancer with palliative intent compared with supportive care alone is now widely accepted. However, the best choice of chemotherapy regimen for patients with advanced gastric cancer is still a matter of controversy and requires further investigation. This study is perfo...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Cao W,Yang W,Lou G,Jiang J,Geng M,Xi W,Li H,Ma T,Jin Y

    更新日期:2009-04-01 00:00:00

  • Sensitivity of gastric adenocarcinoma and normal cell lines against combined or conjugated antimetabolites.

    abstract::The in-vitro growth inhibition of cancer and normal cell lines caused by mixed or covalently linked antimetabolites should clarify whether the conjugation of antimetabolites influences cell sensitivity and growth inhibition in a manner that differs from an equimolar mixture of the same antimetabolites or not. Growth i...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Weinreich J,Struller F,Küper M,Hack A,Königsrainer A,Schott TC

    更新日期:2013-04-01 00:00:00

  • Paclitaxel-induced remission in docetaxel-refractory anthracycline-pretreated metastatic breast cancer.

    abstract::Paclitaxel and docetaxel are excellent agents with a high antitumor effect for the treatment of previously anthracycline-exposed metastatic breast cancer. There has been no standard treatment for patients who undergo therapy of a taxan-resistant metastatic breast cancer. Paclitaxel has partial non-cross-resistance in ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Suzuma T,Sakurai T,Yoshimura G,Umemura T,Tamaki T,Naito Y

    更新日期:2000-08-01 00:00:00

  • Complete pathologic response with combination oxaliplatin and 5-fluorouracil chemotherapy in an older patient with advanced gastric cancer.

    abstract::Management of gastric cancer in older adults is challenging. Perioperative treatment with epirubicin, cisplatin, and 5-fluorouracil combination chemotherapy and surgery is considered the standard treatment of locally advanced gastric adenocarcinoma. However, this chemotherapy regimen is not well tolerated in older adu...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Amini A,Sanati H

    更新日期:2011-11-01 00:00:00

  • Phase II evaluation of interleukin-4 in patients with non-Hodgkin's lymphoma: a Southwest Oncology Group trial.

    abstract::We performed a phase II, Southwest Oncology Group (SWOG) clinical trial of recombinant human interleukin-4 (rhuIL-4) in patients with previously treated non-Hodgkin's lymphoma (NHL). We studied 18 eligible patients with low-grade and 21 patients with intermediate- or high-grade NHL. All patients had received prior che...

    journal_title:Anti-cancer drugs

    pub_type: 临床试验,杂志文章,多中心研究


    authors: Taylor CW,LeBlanc M,Fisher RI,Moore DF Sr,Roach RW,Elias L,Miller TP

    更新日期:2000-10-01 00:00:00

  • Preclinical toxicologic evaluation of DENSPM (N1,N11-diethylnorspermine) in rats and dogs.

    abstract::A toxicology study of DENSPM was carried out in rats by multiple (once daily for 5 days) intravenous injection. Doses of 12.5, 25 and 50 mg DENSPM/kg were well tolerated. Infusion of 100 mg DENSPM resulted in distressing physical signs, including labored breathing, convulsive movements and acute death. There were no e...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Kanter PM,Bullard GA,King JM

    更新日期:1994-08-01 00:00:00

  • RITA induces apoptosis in p53-null K562 leukemia cells by inhibiting STAT5, Akt, and NF-κB signaling pathways.

    abstract::Targeting oncogenic signaling pathways by small molecules has emerged as a potential treatment strategy for cancer. reactivation of p53 and induction of tumor cell apoptosis (RITA) is a promising anticancer small molecule that reactivates p53 and induces exclusive apoptosis in tumor cells. Less well appreciated was th...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Mobaraki RN,Karimi M,Alikarami F,Farhadi E,Amini A,Bashash D,Paridar M,Kokhaei P,Rezvani MR,Kazemi A,Safa M

    更新日期:2018-10-01 00:00:00

  • Cytotoxicity of cantharidin analogues targeting protein phosphatase 2A.

    abstract::Cantharidin is a natural toxin that possesses potent anti-tumor properties. Its clinical application, however, is limited due to severe side-effects. Its cytotoxicity is believed to be mediated by the inhibition of serine/threonine protein phosphatase 2A. In order to identify new compounds with potential clinical ther...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Shan HB,Cai YC,Liu Y,Zeng WN,Chen HX,Fan BT,Liu XH,Xu ZL,Wang B,Xian LJ

    更新日期:2006-09-01 00:00:00

  • Antitumor activity, optimum administration method and pharmacokinetics of 13,14-dihydro-15-deoxy-deoxy-Delta7 -prostaglandin A1 methyl ester (TEI-9826) integrated in lipid microspheres (Lipo TEI-9826).

    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


    authors: Fukushima S,Takeuchi Y,Kishimoto S,Yamashita S,Uetsuki K,Shirakawa S,Suzuki M,Furuta K,Noyori R,Sasaki H,Kikuchi Y,Kita T,Yamori T,Sawada J,Kojima M,Hazato A,Kurozumi S,Fukushima M

    更新日期:2001-03-01 00:00:00

  • Efficient induction of apoptosis by ONYX-015 adenovirus in human colon cancer cell lines regardless of p53 status.

    abstract::The ONYX-015 virus is a mutated adenovirus that in theory selectively replicates and induces cytolysis in tumor cells lacking functional p53. The present study investigated whether ONYX-015 viral infection alone or in combination with conventional chemotherapeutic agents could significantly increase apoptosis in human...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Petit T,Davidson KK,Cerna C,Lawrence RA,Von Hoff DD,Heise C,Kirn D,Izbicka E

    更新日期:2002-01-01 00:00:00

  • Control of nausea and vomiting by Navoban (tropisetron) in 131 children receiving cytotoxic chemotherapy.

    abstract::One hundred and thirty-one children with a median age of 5 years were administered Navoban (tropisetron), a selective antagonist of the serotonin receptor (5-HT3), dosed once daily at 0.2 mg/kg (with a maximum of 5 mg daily) in a study aimed at evaluating the prevention of nausea and vomiting induced by anti-cancer ch...

    journal_title:Anti-cancer drugs

    pub_type: 临床试验,杂志文章,多中心研究


    authors: Benoit Y,Hulstaert F,Vermylen C,Sariban E,Hoyoux C,Uyttebroeck A,Otten J,Laureys G,De Kerpel I,Nortier D

    更新日期:1995-02-01 00:00:00

  • Clinical significance of a prostate-specific antigen flare phenomenon in patients with hormone-refractory prostate cancer receiving docetaxel.

    abstract::Docetaxel has shown promise for the treatment of hormone-refractory prostate cancer and has become the standard of care. The flare phenomenon is a known entity in androgen-deprivation therapy of advanced prostate cancer and it has also been described in palliative chemotherapy of hormone-refractory prostate cancer. Th...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Olbert PJ,Hegele A,Kraeuter P,Heidenreich A,Hofmann R,Schrader AJ

    更新日期:2006-09-01 00:00:00

  • Phase 1 study of escalating-dose OncoGel (ReGel/paclitaxel) depot injection, a controlled-release formulation of paclitaxel, for local management of superficial solid tumor lesions.

    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


    authors: Vukelja SJ,Anthony SP,Arseneau JC,Berman BS,Cunningham CC,Nemunaitis JJ,Samlowski WE,Fowers KD

    更新日期:2007-03-01 00:00:00

  • Trastuzumab and vinorelbine as first-line therapy for HER2-overexpressing metastatic breast cancer: multicenter phase II and pharmacokinetic study in Japan.

    abstract::Tolerability and response rate to weekly combination chemotherapy with trastuzumab and vinorelbine in Japanese women with HER2-overexpressing breast cancer not previously receiving either therapy were assessed. Tumor response was evaluated every 4 weeks and adverse events were graded. A total of 23 patients from six p...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,多中心研究


    authors: Tokudome N,Ito Y,Hatake K,Toi M,Sano M,Iwata H,Sato Y,Saeki T,Aogi K,Takashima S

    更新日期:2008-08-01 00:00:00

  • Mutational profile in circulating tumor DNA in a patient affected by low-risk endometrial cancer: predictable tool of relapse?

    abstract::Endometrial cancer is the commonest gynecological cancer, the majority is endometrioid type, diagnosed at an early stage with 69-88% 5-year survival. Low-grade endometrial cancers have low recurrence rates and often do not receive adjuvant therapy; however, a subset of these patients will have poor outcomes and would ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Malentacchi F,Turrini I,Zepponi F,Fantappiè G,Sorbi F,Antonuzzo L,Fambrini M,Noci I,Pillozzi S

    更新日期:2020-11-01 00:00:00

  • Effect of gastric pH on erlotinib pharmacokinetics in healthy individuals: omeprazole and ranitidine.

    abstract::The aim of this study was to evaluate the effect of coadministration of acid-reducing agents on the pharmacokinetic exposure of orally administered epidermal growth factor receptor inhibitor erlotinib, a drug that displays pH-dependent solubility. Two studies were conducted, the first with the proton pump inhibitor om...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,随机对照试验


    authors: Kletzl H,Giraudon M,Ducray PS,Abt M,Hamilton M,Lum BL

    更新日期:2015-06-01 00:00:00

  • Antiproliferative and apoptotic effects of paeonol on human hepatocellular carcinoma cells.

    abstract::Paeonol, a major phenolic component of Moutan Cortex, is known to have antitumor effects through an unknown mechanism. In this study, we tried to elucidate the anticancer effects of paeonol on human hepatocellular carcinoma (HCC) cell lines BEL-7404, SMMC-7721, and MHCC97-H in vitro. Using the 3-[4,5-dimethylthiazol-2...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Chunhu Z,Suiyu H,Meiqun C,Guilin X,Yunhui L

    更新日期:2008-04-01 00:00:00

  • Advanced breast cancer: chemotherapy phase III trials that change a standard.

    abstract::At the present time, there is not a standard regimen in upfront metastatic setting for breast cancer. A wide variety of regimens which includes anthracyclines, taxanes, gemcitabine or capecitabine are currently used, however, there is evidence to support the use of many of these drugs in early breast cancer and conseq...

    journal_title:Anti-cancer drugs



    authors: Estevez LG,Tusquets I,Muñoz M,Adrover E,Rovira PS,Seguí MA,Rodríguez CA,Lescure AR,Ruiz M,Alvarez I,Mata JG

    更新日期:2007-08-01 00:00:00

  • Phase I/II study of irinotecan (CPT-11) and S-1 in the treatment of advanced gastric cancer.

    abstract::A phase I/II study to determine the recommended dose for combination therapy with CPT-11 (irinotecan hydrochloride) and S-1 (tegafur, gimestat and otastat potassium) for advanced or recurrent gastric cancer, and to assess the safety and efficacy of this therapy. In the phase I portion of the study, S-1 was administere...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Katsube T,Ogawa K,Ichikawa W,Fujii M,Tokunaga A,Takagi Y,Kochi M,Hayashi K,Kubota T,Aiba K,Arai K,Terashima M,Kitajima M

    更新日期:2007-06-01 00:00:00

  • In-vivo antitumour effect of daunorubicin-GnRH-III derivative conjugates on colon carcinoma-bearing mice.

    abstract::Targeted cancer chemotherapy is a novel approach developed for the specific delivery of anticancer drugs. Tumour targeting can be achieved by combining a chemotherapeutic agent with a targeting moiety that recognizes tumour-specific or highly expressed receptors on cancer cells. We used the gonadotropin-releasing horm...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Manea M,Tóvári J,Tejeda M,Schulcz A,Kapuvári B,Vincze B,Mezo G

    更新日期:2012-01-01 00:00:00

  • A suramin derivative induces enterocyte-like differentiation of human colon cancer cells without lysosomal storage disorder.

    abstract::Suramin is a polysulfonated naphthylurea currently investigated for the treatment of advanced malignancy. We have previously reported that suramin was a potent inducer of the differentiation of the human colic adenocarcinoma cell clone HT29-D4 (Fantini et al., J Biol Chem, 1989; 264: 10282-10286). In this report, we s...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章


    authors: Baghdiguian S,Nickel P,Marvaldi J,Fantini J

    更新日期:1990-10-01 00:00:00

  • The clinical rationale for developing docetaxel (Taxotere).

    abstract::Clinical empiricism has recognized resistant breast cancer as a privileged target for docetaxel (Taxotere). This worldwide registration will offer medical oncologists the opportunity to develop new indications for docetaxel. Pharmacokinetics, preclinical optimal combination and clinical practice will constitute the ra...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审


    authors: Armand JP

    更新日期:1996-08-01 00:00:00