Diorganotin(IV) Derivatives of Substituted Benzohydroxamic Acids with High Antitumor Activity

2004 ◽  
Vol 10 (6) ◽  
pp. 1456-1462 ◽  
Author(s):  
Qingshan Li ◽  
M. Fátima C. Guedes da Silva ◽  
Armando J. L. Pombeiro
Keyword(s):  
Antitumor Activity ◽  
High Antitumor Activity ◽  
Derivatives Of

scholarly journals Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles

2021 ◽  
pp. 37-49
Author(s):  
І. І. Мирко ◽  
Ю. І. Горак ◽  
Т. І. Чабан ◽  
І. В. Драпак ◽  
В. С. Матійчук
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Condensed System ◽  
Highly Active ◽  
Therapeutic Program ◽  
Composition And Structure ◽  
Antitumor Properties ◽  
High Antitumor Activity ◽  
Derivatives Of ◽  
Potential Antitumor

One of the promising methods of creating antitumor drugs is the screening of potential antitumor agents among synthesized compounds. Nitrogen-based heterocycle analogues are an extremely important class of organic substances that are widely used in medical chemistry. [1,2,4]Triazolo[3,4-b][1,3,4] thiadiazoles are among the little-studied and hard-to-reach members of this class of compounds. The aim of our work was to synthesize some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, as well as the study of their antitumor activity. The objects of study were 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. The composition and structure of the synthesized compounds were confirmed by the data of elemental analysis and 1H NMR spectroscopy. The antitumor activity of the synthesized compounds was studied in the framework of the international scientific program of the National Cancer Institute (Bethesda, Maryland, USA) DTP NCI (Developmental Therapeutic Program). The synthesis of 11 derivatives of 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles was carried out. These substances are obtained by the interaction of 5-arylfuran-2-carboxylic acids with 5-substituted 4-amino-4H-1,2,4-triazolo-3-thiols. Primary screening revealed individual 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, which showed pronounced selective antitumor activity. The most active among the tested compounds were 3 d, 3 e and 3 j, which were further investigated during secondary screening. The results of these studies confirm the high antitumor activity of these compounds. The proposed approaches and the developed synthesis protocols made it possible to obtain a series of new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. The results of studies of the antitumor activity of the synthesized compounds made it possible to single out 3 highly active compounds with high antitumor activity, which gives reason to consider this condensed system as a promising molecular framework for the design of potential antitumor agents.

ChemInform Abstract: SYNTHESIS AND ANTITUMOR ACTIVITY OF 6-OXO-7-AMINO DERIVATIVES OF 5H-PYRIDO(2,3B)- AND 5H-PYRIMIDO(4,5B)(1,4)THIAZINES

1985 ◽  
Vol 16 (15) ◽  
Author(s):  
N. I. TRAVEN' ◽  
YU. A. ERSHOVA ◽  
A. S. SOKOLOVA ◽  
V. A. CHERNOV ◽  
T. S. SAFONOVA
Keyword(s):  
Antitumor Activity ◽  
Amino Derivatives ◽  
Derivatives Of

Synthesis, in vitro and in vivo antitumor activity of symmetrical bis-Schiff base derivatives of isatin

2014 ◽  
Vol 74 ◽  
pp. 742-750 ◽  
Author(s):  
Chengyuan Liang ◽  
Juan Xia ◽  
Dong Lei ◽  
Xiang Li ◽  
Qizheng Yao ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Schiff Base Derivatives ◽  
In Vivo Antitumor Activity ◽  
Derivatives Of

scholarly journals Preparation and Antitumor Activity of 2''-O-,3''-O-and 2'',3''-Di-O-substituted Derivatives of Etoposide.

1992 ◽  
Vol 40 (7) ◽  
pp. 1783-1788 ◽  
Author(s):  
Takeshi OHNUMA ◽  
Rika OBATA ◽  
Yuji NISHIYAMA ◽  
Tetsuro YAMASAKI ◽  
Hideo KAMEI ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Derivatives Of

The Preparation and Antitumor Activity of Certain Derivatives of 6-Mercaptopurine

1962 ◽  
Vol 5 (3) ◽  
pp. 607-617 ◽  
Author(s):  
Leland R. Lewis ◽  
C. Wayne. Noell ◽  
Alden G. Beaman ◽  
Roland K. Robins
Keyword(s):  
Antitumor Activity ◽  
Derivatives Of

STUDY OF THE BIOLOGICAL PROPERTIES OF SEMI- AND THIOSEMICARBAZONES OF CARBONYL DERIVATIVES OF 4-BUTANOLIDES

2021 ◽  
Vol 55 (2 (255)) ◽  
pp. 103-111
Author(s):  
Tariel V. Ghochikyan ◽  
Armen S. Galstyan ◽  
Hrachik M. Stepanyan ◽  
Irina G. Korpakova ◽  
Alexander S. Kinzirsky
Keyword(s):  
Antitumor Activity ◽  
Green Alga ◽  
Biological Properties ◽  
Lymphocytic Leukemia ◽  
Thiazole Ring ◽  
Lewis Lung ◽  
Ehrlich's Ascites Tumor ◽  
Carbonyl Derivatives ◽  
Derivatives Of ◽  
Test Objects

Based on carbonyl derivatives of 4-substituted-4-butanolides, the appropriate semi- and thiosemicarbazones have been synthesized. It has been found that some representatives of thiosemicarbazones have pronounced algicidal activity against filamentous green alga Cladophora and blue-green alga (cyanobacterium) Synechocystis and some of the semi- and thiosemicarbazones exhibit moderate antitumor activity. The assessment of the antitumor activity of the compounds was carried out using strains of syngeneic and allogeneic tumor systems as test-objects: lymphocytic leukemia P-388, Lewis lung carcinoma, B16 melanoma and Ehrlich’s ascites tumor. It has also been established that some representatives of thiosemi­carbazones exhibit antimutagenic properties. It has been reliably proven that with the formation of a thiazole ring, all properties disappear and a new property in the series of thiazololactones is revealed – antibacterial․

Cemiplimab in a very frail population of patients with advanced or metastatic cutaneous squamous cell carcinoma: A monocenter real-life experience from Italy.

2021 ◽  
Vol 39 (15_suppl) ◽  
pp. e21524-e21524
Author(s):  
Michele Guida ◽  
Annarita Fanizzi ◽  
Davide Quaresmini ◽  
Annalisa Nardone ◽  
Andrea Armenio ◽  
...  
Keyword(s):  
Squamous Cell Carcinoma ◽  
Antitumor Activity ◽  
Cell Carcinoma ◽  
Clinical Outcomes ◽  
Squamous Cell ◽  
Life Experience ◽  
Locally Advanced ◽  
Real Life ◽  
Cutaneous Squamous Cell Carcinoma ◽  
High Antitumor Activity

e21524 Background: Cutaneous squamous cell carcinoma (CSCC) is the second most common skin cancer. Although representing less than 5% of all CSCCs, advanced stages are difficult to treat. Cemiplimab, an antiPD-1 monoclonal antibody, is the first approved immunotherapy in the US and EU for patients with locally advanced (laCSCC) or metastatic (mCSCC) CSCC. Phase I-II studies showed high antitumor activity and good tolerability, but few data are still available regarding cemiplimab in real life experience in non-selected patients. Methods: We recruited 30 consecutive patients with laCSCC (25 pts) and mCSCC (5 pts) treated with cemiplimab from August 2019 to November 2020 at our Institution. Median age was 81 years (range 36-95); 24 males; median ECOG PS 1 (range 0-2). Five patients had an immunosuppressive condition including 3 patients with stable hematologic malignancies and two patients on immunosuppressive therapy for kidney transplantation and Crohn’s disease, respectively. The majority of patients had comorbidities (median 3). Cemiplimab was administered at the flat dose of 350 mg i.v. every 21 days until disease progression or unacceptable toxicity. In all patients we evaluated clinical outcomes, toxicity, and associations between clinical outcomes and peripheral blood parameters. Results: We reported 23 responses (ORR 76.7%) with CR in 5 patients (16.7%). One patient had SD for 5 months. The global DCR was 80%. The median duration of response and PFS was not reached at a median follow-up of 6 months. We observed a higher ORR in head and neck primary tumours (87% vs. 42.9% of others, p = 0.016) and in patients with haemoglobin level > 12 g/dL (87.5% vs. 64.3%). No significative difference in ORR was observed with respect to the median age (81.3% in >81 years vs. 71.4% in < 81 years). Among the 5 patients with immunosuppressive status, a response was obtained in 4 patients (80%), including 1 CR. Nine patients died, 7 for PD and 2 for causes unrelated to the disease. Twenty patients (67.7%) still have an ongoing response. The treatment was well tolerated by the majority of patients. The most common adverse events were fatigue in 7 patients (23.3%) and skin toxicity in 10 patients (33.3%) including pruritus in 6 patients, rash in 3 patients, bullous erythema in 1 patient. Only 3 (10%) patients experienced severe (grade 3/4) toxicity. Three responder patients interrupted treatment (2 for toxicity after 7 and 9 cycles, and one for pre-existing dementia) but maintaining their response. Conclusions: In our real-life experience cemiplimab showed high antitumor activity with acceptable safety profile similar to those in selected patients of trials. Moreover, its antitumor activity resulted not impaired in very elderly patients or in those with immunocompromized status.

Sign in / Sign up

Export Citation Format

Share Document