scholarly journals Microwave Assisted Synthesis of Six Member Ring Azaheterocycles and Their Antimycobacterial and Anticancer Evaluation

2001 ◽  
Vol 71 (3) ◽  
pp. 287-293 ◽  
Author(s):  
Cristina Al Matarneh ◽  
Catalina-Ionica Ciobanu ◽  
Violeta Mangalagiu ◽  
Gheorghita Zbancioc ◽  
Ramona Danac
Keyword(s):  
Breast Cancer ◽  
Prostate Cancer ◽  
Lung Cancer ◽  
Renal Cancer ◽  
Reaction Times ◽  
Antimycobacterial Activity ◽  
Microwave Assisted Synthesis ◽  
Thermal Heating ◽  
Microwave Assisted ◽  
Mw Irradiation

We report herein a comparative study concerning the influence of microwave (MW) irradiation comparative with conventional thermal heating (TH) in the reaction of six member ring azaheterocycles (derived from phenanthroline, quinoline, isoquinoline and phthalazine) with ethyl cyanoformate, and their anticancer and antimycobacterial activity. Under MW irradiation the reactions have some undeniable advantages: the reaction times decrease dramatically (from hours to minutes), the yields are higher, the reactions became selective in some cases (4,7-phenanthrolinium and phthalazinium ylides). The decreasing of reaction time+ from hours to minutes corroborated with the fact that in majority of cases the yield are higher and the selectivity is better, allow us to say that these reactions could be considered as eco-friendly. As far for biological activity, three of the compounds exhibited a significant antitumor activity against some cancer cell lines including prostate cancer, leukemia, renal cancer, lung cancer and breast cancer. The best potency in terms of growth inhibition of tumor cells (~45%) was shown by compound 4a against renal cancer A498 and ovarian cancer SK-OV-3 cells. The tested compounds have not shown any antimycobacterial activity against Mycobacterium tuberculosis.

scholarly journals Anticancer Applications and Pharmacological Properties of Piperidine and Piperine: A Comprehensive Review on Molecular Mechanisms and Therapeutic Perspectives

2022 ◽  
Vol 12 ◽  
Author(s):  
Sicon Mitra ◽  
Uttpal Anand ◽  
Niraj Kumar Jha ◽  
Mahipal S. Shekhawat ◽  
Suchismita Chatterjee Saha ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Prostate Cancer ◽  
Lung Cancer ◽  
Ovarian Cancer ◽  
Molecular Mechanisms ◽  
Therapeutic Potential ◽  
Black Pepper ◽  
Piper Nigrum ◽  
Molecular Formula ◽  
Cycle Arrest

Piperine and piperidine are the two major alkaloids extracted from black pepper (Piper nigrum); piperidine is a heterocyclic moiety that has the molecular formula (CH2)5NH. Over the years, many therapeutic properties including anticancer potential of these two compounds have been observed. Piperine has therapeutic potential against cancers such as breast cancer, ovarian cancer, gastric cancer, gliomal cancer, lung cancer, oral squamous, chronic pancreatitis, prostate cancer, rectal cancer, cervical cancer, and leukemia. Whereas, piperidine acts as a potential clinical agent against cancers, such as breast cancer, prostate cancer, colon cancer, lung cancer, and ovarian cancer, when treated alone or in combination with some novel drugs. Several crucial signalling pathways essential for the establishment of cancers such as STAT-3, NF-κB, PI3k/Aκt, JNK/p38-MAPK, TGF-ß/SMAD, Smac/DIABLO, p-IκB etc., are regulated by these two phytochemicals. Both of these phytochemicals lead to inhibition of cell migration and help in cell cycle arrest to inhibit survivability of cancer cells. The current review highlights the pharmaceutical relevance of both piperine and piperidine against different types of cancers.

Discovery of new chiral sulfonamides bearing benzoxadiazole as HIF inhibitors for non-small cell lung cancer therapy: design, microwave-assisted synthesis, binding affinity, in vitro antitumoral activities and in silico studies

2022 ◽  
Author(s):  
Demet Taşdemir ◽  
Ayşegül Karaküçük-İyidoğan ◽  
Yasemin Saygideger ◽  
EMİNE Elçin Emre ◽  
Tuğba Taşkın-Tok ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Treatment Strategies ◽  
Microwave Assisted Synthesis ◽  
Hypoxia Inducible Factors ◽  
Small Cell Lung ◽  
Microwave Assisted ◽  
In Silico Studies ◽  
Lung Cancer Therapy ◽  
Therapy Design

Hypoxia-inducible factors (HIF), one of the targeted treatment strategies with a rising promise in lung cancer, are known to play a role in tumor growth and other oncogenic properties in...

Indole based prostate cancer agents

2022 ◽  
Vol 0 (0) ◽  
Author(s):  
Sunil Kumar ◽  
Madhuri T. Patil ◽  
Deepak B. Salunke
Keyword(s):  
Breast Cancer ◽  
Prostate Cancer ◽  
Lung Cancer ◽  
Immune System ◽  
Anticancer Agents ◽  
Crucial Role ◽  
Heterocyclic Compounds ◽  
Indole Derivatives ◽  
Cancer Chemotherapeutics ◽  
Privileged Structure

Abstract Cancer weakens the immune system which fails to fight against the rapidly growing cells. Among the various types of cancers, prostate cancer (PCa) is causing greater number of deaths in men after lung cancer, demanding advancement to prevent, detect and treat PCa. Several small molecule heterocycles and few peptides are being used as oncological drugs targeting PCa. Heterocycles are playing crucial role in the development of novel cancer chemotherapeutics as well as immunotherapeutics. Indole skeleton, being a privileged structure has been extensively used for the discovery of novel anticancer agents and the application of indole derivatives against breast cancer is well documented. The present article highlights the usefulness of indole linked heterocyclic compounds as well as the fused indole derivatives against prostate cancer.

Microwave-assisted synthesis of zinc 5-(4-carboxyphenyl)-10,15,20-triphenylporphyrin and zinc 5-(4-carboxyphenyl)-10,15,20-triphenylchlorin

2015 ◽  
Vol 19 (04) ◽  
pp. 595-600 ◽  
Author(s):  
Rima Chouikrat ◽  
Aymeric Champion ◽  
Régis Vanderesse ◽  
Céline Frochot ◽  
Albert Moussaron
Keyword(s):  
Reaction Times ◽  
Microwave Assisted Synthesis ◽  
Spectroscopic Techniques ◽  
H Nmr ◽  
Microwave Assisted ◽  
Experimental Protocols ◽  
Time Of Reaction

The microwave-assisted synthesis of zinc 5-(4-carboxyphenyl)-10,15,20-triphenylporphyrin and zinc 5-(4-carboxyphenyl)-10,15,20-triphenylchlrorin are described and compared to classic conditions of synthesis in terms of time of reaction and yields obtained. The new experimental protocols are easy to implement required small amounts of reagents and solvents and lead to short reaction times. All compounds have been characterized by 1 H NMR, MS and spectroscopic techniques.

The changing face of cancer in the elderly—Only a demographic change?

2006 ◽  
Vol 24 (18_suppl) ◽  
pp. 18597-18597
Author(s):  
Y. Rottenberg ◽  
T. Peretz
Keyword(s):  
Breast Cancer ◽  
Prostate Cancer ◽  
Lung Cancer ◽  
Older Women ◽  
Age Groups ◽  
The Elderly ◽  
Age Group ◽  
Industrial Countries ◽  
Cancer Burden ◽  
Two Age Groups

18597 Background: In industrial countries, the cancer burden of the elderly is high and is increased. One reason is longer life expectancy. Increasing age standardized rates of cancer in this age group compared to younger groups may also explain this phenomenon. Methods: Two age groups were examined, above and below 65 years. Each age group was further divided into men and women. The age standardized rates for all cancers combined among the Jewish population in Israel were identified through the Israel Cancer Registry during the years 1973–2002. In addition, lung and colorectal cancers according to sexes, prostate cancer in men and breast cancer in women were examined. Results: Between the first 5 years of the study (1973–1977) and the last 5 years (1998–2002) the age standardized rates for all cancers combined were raised by about one third in the two age groups. In males, the overall change was higher in the older group (42% in men aged 65 years and older compared to 31% in men younger than 65). However, the rise in the younger group was more prominent in females (42% in women younger than 65 years compared to 33 % in women aged 65 and older). The most outstanding increase was in prostate cancer in men, but mainly in the younger group (176% in the older group and 368% in the younger group) followed by breast cancer in women, more prominent in the older group (64% in the older group and 50% in the younger group). In both sexes, more noticeable increases were noted in the older groups in colorectal cancer and in lung cancer. Between the years 1993–1997 and 1998–2002 shifts towards stabilization and even a decrease was noted in some of the cancers that were examined. In men aged 65 years and older rates for all cancers combined were decreased by 2.5%, among the specific tumors and a decrease was noted in lung cancer (6.7%) and prostate cancer (5.8%). The rates for all cancers combined among the older women were slightly decreasing (2.0%). No decrease was noted in the specific tumors in this group. Among the younger groups in both sexes, no decrease (defined >0.5%) was noted. Conclusions: These data argue against the hypothesis that the overall change in the cancer burden in the aged could be also explained by differences changes in the risk of developing cancer between these two age groups. No significant financial relationships to disclose.

BMI, long-term changes in BMI, and risk of cancer mortality in a large cohort study.

2012 ◽  
Vol 30 (15_suppl) ◽  
pp. 1502-1502
Author(s):  
Niloofar Taghizadeh ◽  
Judith M. Vonk ◽  
H. Marike Boezen
Keyword(s):  
Breast Cancer ◽  
Prostate Cancer ◽  
Lung Cancer ◽  
Cohort Study ◽  
Mortality Risk ◽  
Cancer Mortality ◽  
Lung Cancer Mortality ◽  
Prostate Cancer Mortality ◽  
Risk Of Mortality ◽  
Cancer Mortality Risk

1502 Background: There are indications of an association between Body Mass Index (BMI) and risk of different cancer types. There is dispute whether this association differs between males and females. Methods: We studied the association of BMI at the first survey with risk of mortality from the most common types of cancer (lung, colorectal, breast and prostate cancer) in a large general population-based cohort study (Vlagtwedde-Vlaardingen, 1965-1990) with follow-up on mortality status until 2009. Additionally, we assessed this association based on tertiles of the annual change in BMI (defined as the difference between BMI at last survey and first survey divided by the time between last and first survey). We used 3 categories of BMI (< 25 kg/m2, 25-30 kg/m2, and ≥ 30 kg/m2) and changes in BMI (< 0.02 kg/m2/yr, 0.02-0.2 kg/m2/yr, and > 0.2 kg/m2/yr) in the analyses. The multivariate Cox regression model was adjusted for age, smoking, gender. Analyses were additionally stratified by gender and smoking. Results: Among all 8645 subjects, 1194 died due to cancer (lung cancer: 275; colorectal cancer: 134; breast cancer: 117; prostate cancer: 83). Mortality from all types of cancer was significantly increased in subjects with BMI > 30 kg/m2 (HR (95 % CI)) = 1.22 (1.00-1.48)), especially in females (1.38 (1.06-1.81)) and in never smokers (1.39 (1.02-1.90)). Prostate cancer mortality was significantly increased in males with BMI 25-30 kg/m2 (2.04 (1.90-3.83)) and > 30 kg/m2 (2.61 (1.02-6.67)). This association between prostate cancer mortality and BMI was higher in smokers. Lung cancer mortality risk was decreased in subjects with BMI 25-30 kg/m2 (0.71 (0.54-0.93)) and > 30 kg/m2 (0.82 (0.50-1.32)), especially in males, in smokers, and in smoking males. There were no significant associations between BMI and colorectal or breast cancer mortality nor between change in BMI and mortality from all analyzed types of cancer. Conclusions: We show that an increase in BMI is associated with an increased risk of mortality from all types of cancer in females and with an increased mortality risk from prostate cancer in males but with a decreased lung cancer mortality risk, especially in males. More research is needed into the biological mechanisms that link BMI to cancer.

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