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Drug Screening Assays, Antitumor

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Design and synthesis of new phthalazine-based derivatives as potential EGFR inhibitors for the treatment of hepatocellular carcinoma.

Bioorganic chemistry
Searching for new leads in the battle of cancer will never ends, we herein disclose the design and synthesis of new phthalazine derivatives and their in vitro and in vivo testing for their antiproliferative activity. Phthalazine was selected as a pri...

Chemical findings and in vitro biological studies to uphold the use of Ficus exasperata Vahl leaf and stem bark.

Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association
Ficus exasperata Vahl, commonly known as sandpaper, is a terrestrial Afro-tropical tree used in popular medicine. Despite the existence of some works on the biological activities of this species, its chemical composition is still poorly known. The ai...

Chemical characterization, antioxidant, genotoxic and in vitro cytotoxic activity assessment of Juniperus communis var. saxatilis.

Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association
Chemical composition and antioxidative, genotoxic and cytotoxic potential of essential oil (EO) and post-distillation waste (PDW) of Serbian Juniperus communis L. var. saxatilis Pall. was studied in human lung carcinoma (A549) and normal lung fibrobl...

Effects of salinity on bacterial communities, Maillard reactions, isoflavone composition, antioxidation and antiproliferation in Korean fermented soybean paste (doenjang).

Food chemistry
The purpose of this study was to investigate bacterial communities and health-benefit-related parameters in doenjang prepared with various brine concentrations (8, 12, 16, and 20%). Phenolic, flavonoid, melanoidin and isoflavone contents, antioxidati...

5-fluorouracil combined with cisplatin and mitomycin C as an optimized regimen for hyperthermic intraperitoneal chemotherapy in gastric cancer.

Journal of surgical oncology
BACKGROUND AND OBJECTIVES: Optimized drug regimens for hyperthermic intraperitoneal chemotherapy (HIPEC) have not been standardized completely in patients with advanced gastric cancer (GC). We evaluated an optimized anti-tumor protocol comprising 5-f...

Anticancer and anti-inflammatory activities of girinimbine isolated from .

Drug design, development and therapy
Therapy that directly targets apoptosis and/or inflammation could be highly effective for the treatment of cancer. is an edible herb that has been traditionally used for cancer treatment as well as inflammation. Here, we describe that girinimbine, a...

Machine learning prioritizes synthesis of primaquine ureidoamides with high antimalarial activity and attenuated cytotoxicity.

European journal of medicinal chemistry
Primaquine (PQ) is a commonly used drug that can prevent the transmission of Plasmodium falciparum malaria, however toxicity limits its use. We prepared five groups of PQ derivatives: amides 1a-k, ureas 2a-k, semicarbazides 3a,b, acylsemicarbazides 4...

A Functional Signature Ontology (FUSION) screen detects an AMPK inhibitor with selective toxicity toward human colon tumor cells.

Scientific reports
AMPK is a serine threonine kinase composed of a heterotrimer of a catalytic, kinase-containing α and regulatory β and γ subunits. Here we show that individual AMPK subunit expression and requirement for survival varies across colon cancer cell lines....

Time-dependent AI-Modeling of the anticancer efficacy of synthesized gallic acid analogues.

Computational biology and chemistry
BACKGROUND/AIM: Main objective of this study is mapping of the anticancer efficacy of synthesized gallic acid analogues using modeling and artificial intelligence (AI) over a large range of concentrations and exposure times to explore the underline m...