scholarly journals Synthesis and Anticancer Activity of Novel Oxadiazole Functionalized Pyrazolo[3,4-b]pyridine Derivatives

2021 ◽  
Vol 33 (6) ◽  
pp. 1331-1335
Author(s):  
Bhadru Bhukya ◽  
Hanmanthu Guguloth

A series of novel oxadiazole functionalized pyrazolo[3,4-b]pyridine derivatives (6a-n)was synthesized using 6-thiophenyl-4-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridin-3-amine (1) through reaction with 2-bromoethyl acetate, followed by hydrazine hydrate to afford hydrazide derivatives (5). These compounds were further treated with aromatic acids in the presence of phosphoryl chloride and obtained oxadiazole functionalized pyrazolo[3,4-b]pyridine derivatives (6a-n). All the synthesized compounds 6a-n were screened for anticancer activity against four cancer cell lines such as HeLa - cervical cancer (CCL-2); COLO 205-colon cancer (CCL-222); HepG2-liver cancer (HB-8065); MCF7-breast cancer (HTB-22). Compounds 6i, 6m and 6n were found to have more prominent anticancer activity at micromolar concentration.

Author(s):  
Marina Kochiyeva

Data on modern methodological approaches that are used in screening for cancer are summarized. General principles of organizing screening studies are examined from the perspective of evidence-based medicine, target population, research methods, and effectiveness of the implemented screening programs for breast cancer, cervical cancer, and colon cancer are determined.


2013 ◽  
Vol 31 (15_suppl) ◽  
pp. e17512-e17512 ◽  
Author(s):  
Wade T. Swenson ◽  
John M. Lindblom ◽  
John Reber

e17512 Background: Cancer awareness month campaigns are a health promotion tool used to increase public awareness about a specific cancer, its prevention, and treatment. Cancer awareness month campaigns could be most impactful in promoting awareness of cancers for which established screening guidelines exist. Currently, the United States Preventive Task Force endorses screening the general population for colon, cervical and breast cancers. We aimed to assess the effectiveness of campaigns by identifying internet search volume and monthly cancer diagnoses. Methods: GoogleTrends was utilized to identify the relative monthly volume of search terms from 2004 to 2009 as a proxy for public awareness. Search trends for“breast cancer”, “colon cancer”, and “cervical cancer” were analyzed and an average monthly search volume index (SVI) was determined. Surveillance, Epidemiology and End Result (SEER) data was analyzed during the same time period. These data were compared using Pearson's correlation coefficient and the chi square test for seasonality. The monthly trends were compared to corresponding cancer awareness month campaigns (breast cancer-October, colon cancer-March, cervical cancer-January). Results: Internet search volume was highest for colon cancer and breast cancer in the respective cancer awareness campaign months. The frequencies of breast cancer and colon cancer diagnoseswere not significantly higher in the respective cancer awareness months. Cervical cancer search volume and cancer diagnoses did not correlate with awareness campaign months. Search volume and cancer diagnoses were not well correlated for breast cancer (r=0.089) or cervical cancer (r=0.228); however, they were significantly correlated for colon cancer (r=0.386; p-value=0.0008). Conclusions: Cancer awareness month campaigns appear to raise public awareness as estimated by internet search volume for breast cancer and colon cancer. Cervical cancer awareness month campaigns do not have the same effect. There is no significant correlation between cancer awareness campaign months and cancer diagnosis incidence for either breast cancer or cervical cancer, whereas there is a significant correlation for colon cancer.


2018 ◽  
Vol 85 (4) ◽  
pp. 412-452
Author(s):  
William V. Williams ◽  
Louise A. Mitchell ◽  
S. Kathleen Carlson ◽  
Kathleen M. Raviele

Combined estrogen–progestogen contraceptives (oral contraceptives or OCs) and progestogen-only contraceptives (POCs) are synthetic steroids that bind to steroid hormone receptors, which are widespread throughout the body. They have a profound effect on cellular physiology. Combined OCs have been classified by the International Agency for Research on Cancer (IARC) as Group 1 carcinogens, but their findings have not been updated recently. In order to update the information and better understand the impact that OCs and POCs have on the risk of development of cancers, a comprehensive literature search was undertaken, focusing on more recently published papers. In agreement with the IARC, the recent literature confirms an increased risk of breast cancer and cervical cancer with the use of OCs. The recent literature also confirms the IARC conclusion that OCs decrease the risk of ovarian and endometrial cancers. However, there is little support from recent studies for the IARC conclusion that OCs decrease the risk of colorectal cancer or increase the risk of liver cancer. For liver cancer, this may be due to the recent studies having been performed in areas where hepatitis is endemic. In one large observational study, POCs also appear to increase the overall risk of developing cancer. OCs and POCs appear to increase the overall risk of cancer when carefully performed studies with the least intrinsic bias are considered. Summary: OCs have been classified as cancer-causing agents, especially leading to increases in breast cancer and cervical cancer. A review of the recent scientific literature was performed to see whether this still appears to be the case. The recent literature supports the cancer-causing role of OCs especially for breast cancer and cervical cancer. Studies also indicate that progesterone-only contraceptives (such as implants and vaginal rings) also can cause cancer. This is especially true for breast cancer and cervical cancer.


2019 ◽  
Vol 6 (Supplement_2) ◽  
pp. S172-S172
Author(s):  
Kristen Hysell ◽  
Wei He ◽  
Yuchiao Chang ◽  
Scott Dryden-Peterson ◽  
Virginia A Triant

Abstract Background Cancer is now the leading cause of mortality for persons living with HIV (PLWH) in the United States, but it is uncertain whether PLWH access cancer screening that could lower this burden. We sought to assess cancer screening for breast, cervical, and colon cancer among PLWH compared with the HIV-uninfected population at a multicenter healthcare system over the past two decades. Methods Data were obtained from a prospective, observational HIV clinical care cohort comprised of PLWH engaged in care in the Partners Healthcare System. Patients eligible for cancer screening between the years 2002 and 2016 were included. Patients were matched in a maximum of 1:4 ratio with HIV-uninfected patients from the Massachusetts General Primary Care Practice-Based Research Network based on age, sex, race, year of study entry, and length of follow-up. The mean proportion of time in which eligible patients were guideline concordant for cervical, breast, and colon cancer screening was assessed. Non-parametric tests were used to compared screening rates between PLWH and HIV-infected and on the basis of multiple clinical and sociodemographic factors. Results During the observation period, a total of 495 PLWH were eligible for breast cancer screening, 1011 for cervical cancer screening, and 1965 for colon cancer screening. For each screening group, the majority of PLWH were on antiretroviral therapy (ART) and had relatively high CD4 cell counts (Table 1). Screening rates for PLWH compared with controls were 67.3% vs. 82.8% (P < 0.0001) for breast cancer, 49.0% vs. 73.3% (P < 0.0001) for cervical cancer, and 92.7% vs. 91.2% (P = 0.96) for colon cancer (Figure 1). Among PLWH, factors significantly associated with lower rates of screening guideline concordance were older age, lower CD4 count, HIV-1 RNA >1000 copies/mL, and HIV duration < 5 years for breast cancer, and older age, white race, English language, and lack of ART use for cervical cancer. Conclusion Among patients engaged in longitudinal care, PLWH had significantly lower rates of screening for breast and cervical cancer than HIV-uninfected. Disparity is not explained by racial or primary language differences. Further work to improve access to cancer screening for PLWH is needed. Disclosures All authors: No reported disclosures.


2021 ◽  
Vol 33 (10) ◽  
pp. 2327-2332
Author(s):  
Manoj Kumar Mandadi ◽  
Ramana Reddy Bobbala ◽  
Balakrishna Kolli ◽  
Rambabu Gundla

A series of novel amide tagged trifluoromethyl indole and pyrimido indole derivatives 4a-e & 5a-e and 6a-d & 7a-d were synthesized from 4-methyl-2-(methylamino)-6-(trifluoromethyl)isophthalonitrile (1) on reaction with bromoethyl acetate to obtain 2a and 2b isomers. Compound 2a treated with hydrazine hydrate followed by Schiff base reaction to get compounds 4a-e. In another way, compound 2a on reaction with aliphatic primary amine to get compounds 6a-d. For cyclization, compounds 4a-e & 6a-d treated with trifluoroacetic acid to obtain compounds 5a-e and 7a-d, respectively. All the synthesized compounds 4a-e & 5a-e and 6a-d & 7a-d were tested for anticancer activity against four human cancer cell lines such as A549-lung cancer (CCL-185), MCF7-breast cancer (HTB-22), DU145-prostate cancer (HTB-81) and HeLa-cervical cancer (CCL-2). Compounds 9e and 9f were found to have promising anticancer activity at micromolar concentration.


2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Mohamed Jawed Ahsan ◽  
Jyotika Sharma ◽  
Monika Singh ◽  
Surender Singh Jadav ◽  
Sabina Yasmin

In continuance of our search for anticancer agents, we report herein the synthesis and anticancer activity of some novel oxadiazole analogues. The compounds were screened for anticancer activity as per National Cancer Institute (NCI US) protocol on leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancers cell lines.N-(2,4-Dimethylphenyl)-5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-amine (4s) showed maximum activity with mean growth percent (GP) of 62.61 and was found to be the most sensitive on MDA-MB-435 (melanoma), K-562 (leukemia), T-47D (breast cancer), and HCT-15 (colon cancer) cell lines with GP of 15.43, 18.22, 34.27, and 39.77, respectively. Maximum GP was observed on MDA-MB-435 (melanoma) cell line (GP=6.82) by compoundN-(2,4-dimethylphenyl)-5-(4-hydroxyphenyl)-1,3,4-oxadiazol-2-amine (4u).


2017 ◽  
Vol 22 (5) ◽  
pp. 288-291
Author(s):  
Galina B. Smirnova ◽  
S. A Tsurkan ◽  
Yu. A Borisova ◽  
J. R Tcherkassova ◽  
V. I Romanenko ◽  
...  

Experimental studies were carried out with non-covalent complex AIMPILA targeting on AFP receptors (ReCAF). The human subcutaneous xenografts were used with different ReCAF containing transplanted to immunodeficient mice Balb/c nude: colon cancer SW620/ReCAF +, liver cancer HepG2/ReCAF + + and breast cancer T47D/ReCAF + + +. IMPILA was administrated per os under beginning on 4th day after tumor transplantation daily for 5 or 10 days in the total doses of 0.5-2.0 mg/kg or 1.0-4.0 mg/kg, accordingly. The inhibiting effect (T/C < 42%) of AIMPILA was shown to increase in dependence on ReCAF containing on tumor cells: T/C = 70% (SW620/ReCAF +); T/C = 51% (HepG2/ReCAF + +) and T/C = 22% (T47D/ReCAF+++). On the more sensitive model in a series of experiences 10-times course for the treatment with the total dose of 4.0 mg/kg was detected and revealed to T/C = 15-37% (p < 0.05). In the pathomorphological investigation of the T47D/ReCAF+++ tumor there was verified the death of the majority of tumor cells under the treatment of AIMPILA via the apoptosis pathway.


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