anti-neoplastic

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Cisplatin (CDDP) is a chemotherapeutic agent with antitumor activity and is a classic DNA crosslinker. It inhibits DNA synthesis and induces DNA damage in cancer cells by forming DNA adducts, ultimately leading to cell death. In addition, Cisplatin can activate ferroptosis and induce autophagy. In animal studies, it is commonly used to establish models of chronic kidney injury and acute renal failure.

Dacarbazine (DTIC-Dome) is an antineoplastic agent. It has significant activity against melanomas.

Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.

Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ γ δ with low activity (IC50=250 290 1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.

Pemigatinib (INCB054828) is an orally active, selective inhibitor of FGFR, with IC50 values of 0.4 nM for FGFR1, 0.5 nM for FGFR2, 1.2 nM for FGFR3, and 30 nM for FGFR4.

Estramustine (LEO-275) is a nitrogen mustard linked to estradiol, usually as phosphate. Estramustine has been used to treat prostatic neoplasms; also has radiation protective properties. Estramustine is selectively taken up by prostate cells and exerts antineoplastic effects by interfering with microtubule of dynamics and by reducing plasma levels of testosterone.

Bexarotene (LGD1069) is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL).

Taurolidine is a synthetic taurine analog with antimicrobial and anti-neoplastic actions. It displays broad bactericidal and fungicidal activity.

SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride can induce cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 hydrochloride treatment inhibited the calcium calmodulin-dependent protein kinase IIγ (CaMKIIγ) AKT signaling cascade in vitro and in vivo. Overexpression of CaMKIIγ or AKT abolished the effects of SKF-96365 on Y cells, suggesting a critical role of the CaMKIIγ AKT signaling pathway in SFK-96365-induced biological effects. SKF-96365 hydrochloride inhibited hERG current in a concentration-dependent manner.

1. Ethyl trans-caffeate (Caffeic Acid Ethyl Ester) has anti-inflammatory activity. 2. Ethyl trans-caffeate may as a promising natural compound for future application in chronic liver disease. 3. Ethyl trans-caffeate is a potent chemopreventive compound against skin carcinogenesis caused by solar UV exposure. 4. Ethyl trans-caffeate is the high-resolution structures of representative inhibitors in complex with human pancreatic α-amylase. 5. Ethyl trans-caffeate strongly inhibits neoplastic transformation of JB6 Cl41 cells without toxicity. PI3K, ERK1 2, and p38 kinase activities were suppressed by direct binding with HOEC in vitro.

Aniline mustard (Mesylerythrol) is alkylating mustard with anti-neoplastic activity.

CMLD012072 is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor with potent anti-neoplastic activity. It can induce RNA clamping of eIF4A1 and eIF4A2.

Lobaplatin (D-19466) (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin (D-19466) is a third-generation platinum anti-neoplastic agent which shows activity for a variety of tumour types and is a promising antitumour chemotherapeutic agent[1][2]. It is a platinum complex with DNA alkylating activity.

Didemnin C is used as an anti-neoplastic agent.

Bimolane is a topoisomerase II inhibitor.

SH-BC-893, an orally active sphingolipid analog with anti-neoplastic properties, offers protection against ceramide-induced mitochondrial dysfunction and mitigates diet-induced obesity. This compound is utilized in the research of cancer and obesity.

PI3K-IN-47 (Compound 27) is a potent bivalent inhibitor targeting the phosphoinositide 3-kinases (PI3K) family, with IC50 values of 0.44 nM for PI3Kα, and 7.18 nM, 13.92 nM, and 22.83 nM for PI3Kβ, PI3Kγ, and PI3Kδ respectively. It induces G1 phase cell cycle arrest and exhibits anti-neoplastic properties by restraining colony formation and cell migration. Additionally, PI3K-IN-47 has demonstrated the ability to suppress tumor growth in HGC-27 xenograft mouse models [1].