Antimitotic Agent

2020 ◽  
Author(s):  
Keyword(s):  
Antimitotic Agent

scholarly journals Synthesis of New Simplified and Racemic Hemiasterlin Derivatives with Extremely High Cytotoxicity

2018 ◽  
Vol 13 (12) ◽  
pp. 1934578X1801301
Author(s):  
Pham The Chinh ◽  
Đang Thi Tuyet Anh ◽  
Duong Huong Quynh ◽  
Le Nhat Thuy Giang ◽  
Nguyen Ha Thanh ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Human Cancer ◽  
Microtubule Depolymerization ◽  
Antimitotic Agent ◽  
Human Cancer Cell Lines ◽  
Weak Activity ◽  
High Cytotoxicity ◽  
Chemistry Community

Hemiasterlin is a potent antimitotic agent acting through inhibition of microtubule depolymerization. For this reason, the synthesis of new hemiasterlin derivatives has attracted a lot of interest in the organic chemistry community recently. In this paper, the synthesis and evaluation of the cytotoxicity of new simplified and racemic hemiasterlin derivatives were reported. All of the synthesized analogues were evaluated in vitro for cytotoxic activity against four human cell lines (KB, Hep-G2, LU and MCF7). Most of these analogues possess a strong cytotoxic activity on two human cancer cell lines (KB and Hep-G2) and very weak activity on LU and MCF7 cell lines.

scholarly journals Sodium cacodylate as antimitotic agent

2014 ◽  
Vol 57 (3) ◽  
pp. 329-340
Author(s):  
Jadwiga A. Tarkowska
Keyword(s):  
Allium Cepa ◽  
Mitotic Spindle ◽  
Sodium Cacodylate ◽  
Antimitotic Agent ◽  
Ultrastructural Studies ◽  
Meristematic Cells ◽  
Cacodylate Buffer ◽  
Root Meristematic Cells ◽  
Dividing Cells

The effect of pure sodium cacodylate on dividing cells was studied. The root meristematic cells of <em>Allium cepa</em> L. (the roots were squashed in acetoorcein) and endosperm cells of <em>Haemanthus katherinae</em> Bak. (<em>in vitro</em> observations) were used. Serious disturbances in karyokinesis and cytokinesis were found that led most often to the formation of polyploid or multinucleate (<em>A. cepa</em>) cells. These results point to damage of the mitotic spindle and phragmoplast. Careful use of cacodylate buffer in ultrastructural studies of microtubules is advised.

The influence of aminopterin on limb regeneration in Ambystoma mexicanum

Development ◽  
1966 ◽  
Vol 16 (1) ◽  
pp. 143-158
Author(s):  
D. O. E. Gebhardt ◽  
J. Faber
Keyword(s):  
Toluidine Blue ◽  
Growth Retardation ◽  
Limb Regeneration ◽  
Ambystoma Mexicanum ◽  
Ontogenetic Development ◽  
Antimitotic Agent ◽  
Chemical Substances ◽  
Histamine Formation ◽  
Number Of Authors

During the last twenty-five years a number of authors have studied the influence of chemical substances on limb regeneration in amphibians. Examples of compounds which have been tested so far are: (1) the antimitotic agent, colchicine (Thornton, 1943); (2) the salt, beryllium nitrate (Thornton, 1949, 1950, 1951); (3) the carcinogens, dibenzanthracene and methylcholanthrene (Karczmar & Berg, 1952; Ruben & Balls, 1964); (4) the lathyrus factor, β- aminopropionitrile (Chang, Witschi & Ponseti, 1955); (5) the hormone, thyroxine (Hay, 1956); (6) atropine and other neuropharmacological drugs (Singer, Davis & Scheuing, 1960); (7) the metachromatic dye, toluidine blue (Csaba, Bierbauer & Törö, 1961); and (8) semicarbazide, an inhibitor of histamine formation (Deck & Shapiro, 1963). Most of these substances caused growth retardation as well as malformations of the limb regenerates. A number of other investigators have studied the effects of chemicals on the ontogenetic development of the amphibian limb.

Synthesis, X-Ray Crystal Structure and Tubulin- Binding Properties of a Benzofuran Analogue of the Potent Cytotoxic Agent Combretastatin A4

1999 ◽  
Vol 52 (8) ◽  
pp. 767 ◽  
Author(s):  
Martin G. Banwell ◽  
Bernard L. Flynn ◽  
Ernest Hamel ◽  
Anthony C. Willis
Keyword(s):  
Crystal Structure ◽  
Cytotoxic Agent ◽  
Binding Agent ◽  
Binding Properties ◽  
Antimitotic Agent ◽  
X Ray ◽  
Combretastatin A4 ◽  
Tubulin Binding

The benzofuran (4), a ring-fused analogue of the potent antimitotic agent combretastatin A4 (1), has been prepared by a convergent route involving 5-endo-dig iodocyclization of o-hydroxytolan (5) as the key step. Compound (4), which has been characterized crystallographically as well as spectroscopically, is inactive as a tubulin-binding agent.

Spiral Migration Theory of Organ of Corti Development

1976 ◽  
Vol 85 (5_suppl4) ◽  
pp. 1-19 ◽  
Author(s):  
William F. Marovitz ◽  
Joel M. A. Shugar ◽  
Khalid M. Khan
Keyword(s):  
Organ Of Corti ◽  
Anterior Wall ◽  
S Phase ◽  
Migration Pattern ◽  
Cellular Migration ◽  
Antimitotic Agent ◽  
Cellular Division ◽  
Cochlear Duct ◽  
Strategic Location ◽  
Endolymphatic Duct

A mitotic zone has previously been demonstrated on the luminal surface of the posteromedial wall of the otocyst in the plane of the endolymphatic duct and at the junction of cochlea with primitive saccule. In this experiment the application of fluorodeoxyuridine (FudR) (an antimitotic agent) demonstrates the existence of a discrete synthetic zone for the otocyst which lies nearby to the otic zone of mitosis. Cells labeled by FudR and, therefore, in the mitotic synthetic (S) phase are always found away from the lumen (antiluminal surface) when the animals are sacrificed soon after injection. Cellular migration from synthetic zone through the luminal mitotic area and beyond is hypothesized. Once cellular division is completed the cells appear to follow a spiral course (from medial to lateral) over the anterior wall of the otocyst. The cells continue their spiral course entering the thin side of the cochlear base. From this strategic location the cells migrate around the sides of the cochlea to reach and to form the pseudostratified wall and complete the thin side of the cochlear duct. The pitch of this migration pattern is similar to the helical pitch of the mature cochlear duct and may be responsible for the adult configuration.

scholarly journals Effects of Electrical Stimulation on Peripheral Nerve Regeneration in a Silicone Rubber Conduit in Taxol-Treated Rats

Materials ◽  
2020 ◽  
Vol 13 (5) ◽  
pp. 1063
Author(s):  
Chien-Fu Liao ◽  
Shih-Tien Hsu ◽  
Chung-Chia Chen ◽  
Chun-Hsu Yao ◽  
Jia-Horng Lin ◽  
...  
Keyword(s):  
Electrical Stimulation ◽  
Peripheral Nerve ◽  
Silicone Rubber ◽  
Motor Coordination ◽  
Neuronal Connectivity ◽  
Medium Frequency ◽  
Antimitotic Agent ◽  
Inflammatory Conditions ◽  
Macrophage Density

Taxol, a type of antimitotic agent, could modulate local inflammatory conditions in peripheral nerves, which may impair their regeneration and recovery when injured. This study provided in vivo trials of silicone rubber chambers to bridge a long 10 mm sciatic nerve defect in taxol-treated rats. It was aimed to determine the effects of electrical stimulation at various frequencies on regeneration of the sciatic nerves in the bridging conduits. Taxol-treated rats were divided into four groups (n = 10/group): sham control (no current delivered from the stimulator); and electrical stimulation (3 times/week for 3 weeks at 2, 20, and 200 Hz with 1 mA current intensity). Neuronal electrophysiology, animal behavior, neuronal connectivity, macrophage infiltration, calcitonin gene-related peptide (CGRP) expression levels, and morphological observations were evaluated. At the end of 4 weeks, animals in the low- (2 Hz) and medium-frequency (20 Hz) groups had dramatic higher rates of successful regeneration (90% and 80%) across the wide gap as compared to the groups of sham and high-frequency (200 Hz) (60% and 50%). In addition, the 2 Hz group had significantly larger amplitudes and evoked muscle action potentials compared to the sham and the 200 Hz group, respectively (P < 0.05). Heat, cold plate licking latencies, motor coordination, and neuronal connectivity were unaffected by the electrical stimulation. Macrophage density, CGRP expression level, and axon number were all significantly increased in the 20 Hz group compared to the sham group (P < 0.05). This study suggested that low- (2 Hz) to medium-frequency (20 Hz) electrical stimulation could ameliorate local inflammatory conditions to augment recovery of regenerating nerves by accelerating their regrowth and improving electrophysiological function in taxol-treated peripheral nerve injury repaired with the silicone rubber conduit.

scholarly journals Antimitotic agent alters MIP levels In breast cancer cells

2009 ◽  
Vol 96 (3) ◽  
pp. 505a
Author(s):  
Sharon Lobert ◽  
Holland Alday ◽  
Katherine Andersen ◽  
John J. Correia
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Antimitotic Agent

ChemInform Abstract: Synthetic Study on Curacin A: A Novel Antimitotic Agent from the Cyanobacterium Lyngbya majuscula.

ChemInform ◽  
2010 ◽  
Vol 28 (12) ◽  
pp. no-no
Author(s):  
T. ONODA ◽  
R. SHIRAI ◽  
Y. KOISO ◽  
S. IWASAKI
Keyword(s):  
Antimitotic Agent ◽  
Lyngbya Majuscula ◽  
Curacin A

ChemInform Abstract: Absolute Configuration of Curacin A, a Novel Antimitotic Agent from the Tropical Marine Cyanobacterium Lyngbya majuscula.

ChemInform ◽  
2010 ◽  
Vol 26 (26) ◽  
pp. no-no
Author(s):  
D. G. NAGLE ◽  
R. S. GERALDS ◽  
H.-D. YOO ◽  
W. H. GERWICK ◽  
T.-S. KIM ◽  
...  
Keyword(s):  
Absolute Configuration ◽  
Marine Cyanobacterium ◽  
Antimitotic Agent ◽  
Lyngbya Majuscula ◽  
Curacin A

Anti CD-30 Antibody-Drug Conjugate Brentuximab Vedotin (ADCETRIS®) May Be a Promising Treatment Option for Systemic Mastocytosis (SM).

Blood ◽  
2012 ◽  
Vol 120 (21) ◽  
pp. 2857-2857 ◽  
Author(s):  
Amitkumar Mehta ◽  
Vishnu V B Reddy ◽  
Uma Borate
Keyword(s):  
Mast Cell ◽  
Mast Cells ◽  
Systemic Mastocytosis ◽  
White Male ◽  
Brentuximab Vedotin ◽  
Antibody Drug Conjugate ◽  
Antimitotic Agent ◽  
Drug Conjugate ◽  
Tryptase Level ◽  
Antibody Drug

Abstract Abstract 2857 Mastocytosis is a clonal proliferation of abnormal mast cells in single or multiple organs leading to clinical syndromes ranging from a benign self-resolving cutaneous disease to the highly aggressive malignancy, mast cell leukemia (MCL). Mastocytosis is categorized under myeloproliferative neoplasms in the 2008 World Health Organization (WHO) classification of hematopoietic and lymphoid diseases. In almost all cases of SM, the bone marrow (BM) is involved by atypical mast cells. The characteristic Asp816Val (D816V) mutation in the KIT gene present in most cases gives the atypical mast cells a survival advantage that leads to treatment resistance with tyrosine kinase inhibitor (TKIs) like imatinib. According to the 2008 WHO classification, 1 major and 1 minor or 3 minor criterion are required for the diagnosis of systemic mastocytosis (Fig. 1a). Systemic Mastocytosis (SM) is subcategorized into four distinct categories in order of indolent to highly aggressive disease: Indolent Systemic Mastocytosis (ISM), SM with an associated hematologic non-MC-lineage disease (SM-AHNMD), aggressive SM (ASM) and MCL. SM with C findings categorized as ASM (Fig. 1b) is treated with cytoreductive chemotherapy such as interferon 2α or 2-chlorodeoxyadenosine (2-CdA). The overall response rate (ORR) with these agents is 40–50% with significant chemotherapy-related toxicity and short durable responses. The majority of patients with ASM and MCL relapse within a year with a very poor prognosis. The CD30 (Ki-1) antigen is expressed in the majority of ASM cases. Thus, CD30 can serve as a potential therapeutic target as well as a reliable tumor marker to follow disease status. Brentuximab vedotin is an antibody-drug conjugate compound consisting of a chimeric monoclonal antibody against CD30 linked to the antimitotic agent monomethyl auristatin E (MMAE). Here we report evidence of anti-tumor activity in two patients with CD30-positive ASM treated with brentuximab vedotin. Case #1: A 62 year old white male with significant medical history of rheumatoid arthritis, diabetes mellitus and coronary artery disease was evaluated for pancytopenia and hepatomegaly. His initial BM aspiration and biopsy revealed multifocal dense mast cell infiltrate (30–40% involvement with tryptase and CD117 positivity). His initial serum tryptase level was 276 ng/ml. He was treated with 2-CdA continuous infusion for three cycles with no significant response and substantial toxicities. He was subsequently enrolled in a clinical trial with brentuximab vedotin given every 3 weeks at 1.8 mg/kg after confirmation of CD30 positivity on BM aspirate and biopsy (Fig. 2). His peripheral blood counts started to improve after the 5thcycle and he had a durable partial response as assessed by his peripheral blood counts and BM biopsies (Fig 2). Importantly, his sequential bone marrow biopsies showed a decrease in mast cell involvement and CD30 intensity with improved normal marrow cellularity (Fig 2). His only treatment-related toxicities were grade II neuropathy and neutropenia for which his dose was reduced to 1.2 mg/kg. He is currently asymptomatic with ECOG performance status of 0 and does not require any growth factor support at Cycle 12 of this regimen. Case #2: A 79 yr old white male with significant medical history of hypertension, obstructive sleep apnea, coronary artery disease s/p CABG was referred for new diagnosis of ASM on BM biopsy (60–70% marrow involvement with 3+ mast cell density). His initial tryptase level was 224ng/ml. He was enrolled on the same clinical protocol as described above. His sequential BM biopsies revealed significant reduction in mast cell density with mild improvement in overall normal cellularity after 3 cycles of treatment. (Fig 3). Conclusion: Brentuximab vedotin is a promising targeted therapy for SM and needs to be confirmed further by a prospective multicenter clinical trial. In two patients reported here treatment is well tolerated, targets the malignant mast cells and seems to prevent disease progression in a rare disorder with few treatment options and limited response rates. Disclosures: Off Label Use: Brentuximab vedotin (ADCETRIS®) is an antibody-drug conjugate compound consisting of a chimeric monoclonal antibody against CD30 linked to the antimitotic agent monomethyl auristatin E (MMAE). It is not FDA approved for use in Mastocytosis.

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