Synthesis of Some Novel Thieno[3,2-&lt;i&gt;d&lt;/i&gt;]pyrimidines as Potential Cytotoxic Small Molecules against Breast Cancer

Kandeel, M. M.; Abdelhameid, Mohammed K.; Eman, Kamal; Labib, Madlen B.

doi:10.1248/cpb.c13-00089

Cited by 13 publications

(2 citation statements)

References 32 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The focus of patented inventions related to breast cancer was primarily on the development of novel pharmaceutical drugs, biological products, and devices for diagnosis and treatment. Chemical agents or functional groups such as “phenyl” (1995-2017) [54], “pyrazolo” (1995-2003) [55], “thieno” (2008-2013) [56], and “tetrahydroisoquinolines” (2017) [57] were most mentioned in the top 10 topic words and were reported to have antitumor effects in different years. In addition, “antibodies,” “binding,” “base sequence,” “polypeptides,” and “amino acid sequence” were the most frequent keywords of breast cancer mentioned in patents related to antibody therapy [58] and genetic diagnosis and treatment [59,60].…”

Section: Resultsmentioning

confidence: 99%

Technological Innovations in Disease Management: Text Mining US Patent Data From 1995 to 2017

Huang¹,

Zolnoori²,

Balls-Berry³

et al. 2019

J Med Internet Res

View full text Add to dashboard Cite

Background Patents are important intellectual property protecting technological innovations that inspire efficient research and development in biomedicine. The number of awarded patents serves as an important indicator of economic growth and technological innovation. Researchers have mined patents to characterize the focuses and trends of technological innovations in many fields. Objective To expand patent mining to biomedicine and facilitate future resource allocation in biomedical research for the United States, we analyzed US patent documents to determine the focuses and trends of protected technological innovations across the entire disease landscape. Methods We analyzed more than 5 million US patent documents between 1995 and 2017, using summary statistics and dynamic topic modeling. More specifically, we investigated the disease coverage and latent topics in patent documents over time. We also incorporated the patent data into the calculation of our recently developed Research Opportunity Index (ROI) and Public Health Index (PHI), to recalibrate the resource allocation in biomedical research. Results Our analysis showed that protected technological innovations have been primarily focused on socioeconomically critical diseases such as “other cancers” (malignant neoplasm of head, face, neck, abdomen, pelvis, or limb; disseminated malignant neoplasm; Merkel cell carcinoma; and malignant neoplasm, malignant carcinoid tumors, neuroendocrine tumor, and carcinoma in situ of an unspecified site), diabetes mellitus, and obesity. The United States has significantly improved resource allocation to biomedical research and development over the past 17 years, as illustrated by the decreasing PHI. Diseases with positive ROI, such as ankle and foot fracture, indicate potential research opportunities for the future. Development of novel chemical or biological drugs and electrical devices for diagnosis and disease management is the dominating topic in patented inventions. Conclusions This multifaceted analysis of patent documents provides a deep understanding of the focuses and trends of technological innovations in disease management in patents. Our findings offer insights into future research and innovation opportunities and provide actionable information to facilitate policy makers, payers, and investors to make better evidence-based decisions regarding resource allocation in biomedicine.

show abstract

Section: Resultsmentioning

confidence: 99%

Technological Innovations in Disease Management: Text Mining US Patent Data From 1995 to 2017

Huang¹,

Zolnoori²,

Balls-Berry³

et al. 2019

J Med Internet Res

View full text Add to dashboard Cite

show abstract

“…Antiproliferative activity of test compounds ( 4–14 , 18–20 ) was screened against hepatic liver cancer cell line (HepG2) and resistant hepatic liver cancer cell line (R'HepG2) and noncancer cell line (WI‐38) for the most active compound 5 , applying MTT assay according to previously reported procedures (Kandeel et al, 2013). Cells were obtained from American Type Culture Collection and were cultured using DMEM (Invitrogen/Life Technologies) supplemented with 10% FBS (Hyclone), 10 µg/mL of insulin (Sigma), and 1% penicillin‐streptomycin.…”

Section: Methodsmentioning

confidence: 99%

Design, synthesis of novel chromene‐based scaffolds targeting hepatocellular carcinoma: Cell cycle arrest, cytotoxic effect against resistant cancer cells, apoptosis induction, and c‐Src inhibition

Abdelall,

Elshemy,

Labib

et al. 2023

Drug Development Research

View full text Add to dashboard Cite

New chromene derivatives were synthesized based on 4‐(3,4‐dimethoxy)‐4H‐chromene scaffold. All target compounds exhibited cytotoxic activity against HepG2 cells (IC50 = 2.40–141.22 μM). Chromens 5 and 9 showed superior cytotoxicity over staurosporine (IC50 = 18.27 μM) and vinblastine (IC50 = 5.20 μM). c‐Src kinase inhibition assay of compounds 5 and 9 displayed the dominant c‐Src inhibitory activity of 5 (IC50 = 0.184 μM) over 9 (IC50 = 0.288 μM). The safety of the most potent compound 5 against normal WI‐38 cells was confirmed via its IC50 of 115.75 μM comparable with 5‐FU (IC50 = 16.28 μM). Moreover, the promising chromene 5 displayed potent cytotoxicity against resistant HepG2 cells with IC50 of 26.03 μM comparable with 5‐FU (IC50 = 42.68 μM). The most active chromene 5 arrested the HepG2 cell cycle at the S phase and induced a 29‐fold increase in the total number of apoptotic cells indicating pre‐G1 apoptosis. The ability of compound 5 to induce apoptosis was supported via elevation of caspase‐3, caspase‐7, caspase‐9 and proapoptotic Bax protein levels in addition to downregulation of the antiapoptotic Bcl2 protein. Molecular docking studies of compound 5 showed good binding interaction pattern inside c‐Src kinase enzyme active site.

show abstract

ChemInform Abstract: Synthesis of Some Novel Thieno[3,2‐d]pyrimidines as Potential Cytotoxic Small Molecules Against Breast Cancer.

et al. 2013

View full text Add to dashboard Cite

Synthesis of Some Novel Thieno[3,2-d]pyrimidines as Potential Cytotoxic SmallMolecules Against Breast Cancer. -The design of the title compounds as small molecules with antitumor activity is based on DNA-interchelating properties by hydrogen bond formation. The results of cytotoxic screenings are in good agreement with the design rationale. The in vitro cytotoxicity results against human breast cancer reveal three levels of activity compared to the reference drug; compounds (VII), (IX), (XII), and (XIII) show significant activity, even higher than that of the reference compound. Compound (VIIa) is the most potent one while (Xc) is equipotent to Doxorubicin. The remaining compounds are less active. -(KANDEEL, M.; ABDELHAMEID*, M. K.; EMAN, K.; LABIB, M. B.; Chem. Pharm. Bull. 61 (2013) 6, 637-647, http://dx.doi.org/10.

show abstract

Synthesis of Some Novel Thieno[3,2-<i>d</i>]pyrimidines as Potential Cytotoxic Small Molecules against Breast Cancer

Cited by 13 publications

References 32 publications

Technological Innovations in Disease Management: Text Mining US Patent Data From 1995 to 2017

Technological Innovations in Disease Management: Text Mining US Patent Data From 1995 to 2017

Design, synthesis of novel chromene‐based scaffolds targeting hepatocellular carcinoma: Cell cycle arrest, cytotoxic effect against resistant cancer cells, apoptosis induction, and c‐Src inhibition

ChemInform Abstract: Synthesis of Some Novel Thieno[3,2‐d]pyrimidines as Potential Cytotoxic Small Molecules Against Breast Cancer.

Contact Info

Product

Resources

About