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关键词:'C0621'
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Incorporating targeted treatments into standard regimens: whither the role of established doses?
Don S Dizon
Cancer investigation, 22(6), 954-954 (2005-01-12)
Mickaël Thomas et al.
Bioorganic & medicinal chemistry, 16(17), 8109-8116 (2008-08-12)
Two glucuronide prodrugs of the histone deacetylase inhibitor CI-994 were synthesized. These compounds were found to be soluble in aqueous media and stable under physiological conditions. The carbamoyl derivatisation of CI-994 significantly decreased its toxicity towards NCI-H661 lung cancer cells.
B J Foster et al.
Investigational new drugs, 15(3), 187-194 (1997-01-01)
CI-994, a substituted benzamide derivative, is a compound that showed solid tumor selectivity for a variety of solid tumor models compared to L1210 leukemia. Due to its lack of aqueous solubility, it requires oral administration. Female B6D2F1 mice were treated
Michael S Werner et al.
Nature communications, 14(1), 2095-2095 (2023-04-14)
Development can be altered to match phenotypes with the environment, and the genetic mechanisms that direct such alternative phenotypes are beginning to be elucidated. Yet, the rules that govern environmental sensitivity vs. invariant development, and potential epigenetic memory, remain unknown.
M H Seelig et al.
European journal of cancer (Oxford, England : 1990), 32A(11), 1968-1976 (1996-10-01)
Dinaline [4-amino-N-(2'-aminophenyl)-benzamide, Din], p-N-methyldinaline (Me-Din) and p-N-acetyldinaline (Ac-Din) were evaluated for their antineoplastic efficacy in acetoxymethylmethylnitrosamine-induced colorectal carcinomas in Sprague-Dawley rats and in two human colon cancer cell lines. Din was very effective at all dosages (10, 7.7 and 5.9
Qinglei Zhan et al.
PloS one, 8(8), e71663-e71663 (2013-08-27)
Neuroblastoma is the second most common solid tumor diagnosed during infancy. The survival rate among children with high-risk neuroblastoma is less than 40%, highlighting the urgent needs for new treatment strategies. PCI-24781 is a novel hydroxamic acid-based histone deacetylase (HDAC)
D A Richards et al.
Annals of oncology : official journal of the European Society for Medical Oncology, 17(7), 1096-1102 (2006-04-28)
CI-994, an oral histone deacetylase inhibitor, has antineoplastic activity and synergism with gemcitabine preclinically. This randomized phase II trial explored whether CI-994 plus gemcitabine improves overall survival, objective response, duration of response, time to treatment failure and change in quality
Shilpa Thakur et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 27(5), 1399-1409 (2020-12-24)
The goal of this study was to analyze the role of somatostatin receptor type 2 (SSTR2) as a molecular target for the imaging and treatment of thyroid cancer through analysis of SSTR2 expression and its epigenetic modulation and testing tumor
S A Rummel et al.
International journal of cancer, 62(5), 636-642 (1995-09-04)
The mechanism of action of the novel anti-cancer compound CI-994 was studied in C26 murine colon tumor and HCT-8 human colon adenocarcinoma cells. Treatment of either cell line resulted in the specific loss of a 16-kDa phosphoprotein in a time-
In vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines.
Maura Loprevite et al.
Oncology research, 15(1), 39-48 (2005-04-21)
CI-994 (N-acetyldinaline) is a novel oral compound with a wide spectrum of antitumor activity in preclinical models, in vitro and in vivo. The mechanism of action may involve inhibition of histone deacetylation and cell cycle arrest. We studied the action
CoREST Complex-Selective Histone Deacetylase Inhibitors Show Prosynaptic Effects and an Improved Safety Profile To Enable Treatment of Synaptopathies
Fuller NO, et al.
ACS Chemical Neuroscience (2019)
Yasaman KalantarMotamedi et al.
iScience, 24(9), 103080-103080 (2021-09-30)
Resistance to current therapies is common for pancreatic cancer and hence novel treatment options are urgently needed. In this work, we developed and validated a computational method to select synergistic compound combinations based on transcriptomic profiles from both the disease
L Riva et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 6(3), 994-997 (2000-03-31)
CI-994 is a substituted benzamide derivative that has demonstrated significant antitumor activity in vitro and in vivo against a broad spectrum of murine and human tumor models. Its mechanism of action is still unknown but seems to be novel compared
Naoki Sada et al.
Cell death & disease, 11(8), 655-655 (2020-08-20)
Brain injury causes serious motor, sensory, and cognitive disabilities. Accumulating evidence has demonstrated that histone deacetylase (HDAC) inhibitors exert neuroprotective effects against various insults to the central nervous system (CNS). In this study, we investigated the effects of the HDAC
K A Keyes et al.
Experimental hematology, 29(3), 286-294 (2001-03-29)
The protracted administration of near-conventional daily doses of chemotherapeutic agents is a strategy to increase dose intensity and, potentially, efficacy as well. However, protracted therapy carries the risk of damage to stem cells in proliferative tissues that are not targeted
Zhenchuan Liu et al.
Clinical and translational medicine, 11(9), e545-e545 (2021-09-30)
Esophageal squamous cell carcinoma (ESCC) is a highly aggressive and treatment-resistant tumor. The biological implications and molecular mechanism of cancer stem-like cells (CSCs) in ESCC, which contribute to therapeutic resistance such as radioresistance, remain elusive. Quantitative real-time polymerase chain reaction
Kanto Shozu et al.
Clinical epigenetics, 14(1), 147-147 (2022-11-13)
Proline/arginine-rich end leucine-rich repeat protein (PRELP) is a member of the small leucine-rich proteoglycan family of extracellular matrix proteins, which is markedly suppressed in the majority of early-stage epithelial cancers and plays a role in regulating the epithelial-mesenchymal transition by
Transcriptional repression of ER through hMAPK dependent histone deacetylation by class I HDACs.
Plotkin A, Volmar CH, Wahlestedt C, et al.
Breast Cancer Research and Treatment, 147(2), 249-263 (2014)
Establishing and characterizing a new primary effusion lymphoma cell line harboring Kaposi?s sarcoma-associated herpesvirus
Osawa M, et al.
Infectious Agents and Cancer, 11(1), 37-37 (2016)
Suxiang Zhang et al.
Cell death & disease, 9(5), 460-460 (2018-04-28)
Spinal cord injury (SCI) induces severe and long-lasting neurological disability. Accumulating evidence has suggested that histone deacetylase (HDAC) inhibitors exert neuroprotective effects against various insults and deficits in the central nervous system. In the present study, we assessed the effect
S Prakash et al.
Investigational new drugs, 19(1), 1-11 (2001-04-09)
CI-994 (N-acetyl dinaline, PD 123654) is a novel oral agent active in a broad variety of murine and human tumor xenografts. While cytotoxic in the Brown Norway (BN) rat leukemia model, growth inhibition in other murine and human tumor xenografts
Donna A Volpe et al.
Cancer chemotherapy and pharmacology, 54(1), 89-94 (2004-03-12)
Acetyldinaline (CI-994) has shown preclinical efficacy in vitro and in vivo against solid tumor and leukemia cell lines. Since myelosuppression was the dose-limiting toxicity for acetyldinaline in preclinical and clinical studies, experiments were conducted to examine the in vitro and
Ekaterina P Mochalova et al.
Scientific reports, 9(1), 10263-10263 (2019-07-18)
It is known that MuRF-1 and atrogin-1/MAFbx mRNA expression is increased in rat soleus muscle under unloading conditions. We aimed to determine the role of histone deacetylase 1 (HDAC1) in the activation of MuRF-1 and MAFbx expression in rat soleus
S D Undevia et al.
Annals of oncology : official journal of the European Society for Medical Oncology, 15(11), 1705-1711 (2004-11-03)
This study was conducted to determine the toxicity profile, maximum tolerated dose (MTD) and pharmacokinetics of the putative histone deacetylase inhibitor CI-994 in combination with capecitabine. Fifty-four patients were treated according to three different dosing schemes in which the capecitabine
M J Graziano et al.
Archives of toxicology, 73(3), 168-174 (1999-07-13)
CI-994 (acetyldinaline) is an investigative oral anticancer drug currently in clinical trials. To characterize the effects of CI-994 on lymphoid tissue, male rats were administered single oral doses at 0 (vehicle control), 10, 23, and 45 mg/kg and killed up
P M LoRusso et al.
Investigational new drugs, 14(4), 349-356 (1996-01-01)
CI-994 [aka: acetyldinaline; PD 123654; 4-acetylamino-N-(2'aminophenyl)-benzamide] (Figure 1) is a novel antitumor agent with a unique mechanism of action. It is the acetylated metabolite of dinaline, a compound previously identified as having cytotoxic and cytostatic activity against several murine and
M J Graziano et al.
Investigational new drugs, 15(4), 295-310 (1997-01-01)
CI-994 (acetyldinaline) is an orally active anticancer drug currently in Phase 1 clinical trials. To assess its preclinical toxicity, CI-994 was administered orally as suspensions to Wistar rats (10/sex/dose) and in capsules to beagle dogs (3/sex/dose) once daily for two
John J Nemunaitis et al.
Cancer journal (Sudbury, Mass.), 9(1), 58-66 (2003-02-27)
The purpose of this study was to determine the maximum tolerated dose, pharmacokinetic profile, and evidence of antitumor activity of CI-994 used in combination with gemcitabine. This was a dose escalation trial in which gemcitabine (1,000 mg/m2) was given as
Alan J Kraker et al.
Molecular cancer therapeutics, 2(4), 401-408 (2003-04-18)
CI-994 or N-acetyldinaline [4-(acetylamino)-N-(2-amino-phenyl) benzamide] is an antitumor cytostatic agent currently undergoing clinical trial. Although several changes in cellular metabolism induced by the drug have been characterized, the primary molecular mechanism of its antitumor activity has been previously unknown. Here
K A Keyes et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 6(6), 2474-2481 (2000-06-29)
Dose intensity, defined as dose administered per unit time, has emerged as a potentially important measurement of anticancer drug exposure and determinant of efficacy. There are several strategies for increasing dose intensity, one being a protracted daily dosing strategy without
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