antitumour

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

Estramustine phosphate sodium (Ro 21-8837 001) is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2 M phase of the cell cycle.

Bropirimine (U-54461) (U-54461) is a biological response modifier that is thought to act through the induction of lymphokines.

Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.

RX-3117 (fluorocyclopentenylcytosine) is a novel a cytidine analog. RX-3117 displays anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.

CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.

CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.

BMS-906024 (Osugacestat) is an orally available and selective inhibitor of γ-secretase, a small molecule Notch inhibitor.BMS-906024 has broad-spectrum antitumour activity against a variety of human cancer xenografts.BMS-906024 prevents the activation of all four Notch receptors, and is active against Notch1, -2, -3 and -4 receptors. BMS-906024 prevents the activation of all four Notch receptors, with IC50s of 1.6, 0.7, 3.4 and 2.9 nM for Notch1, -2, -3 and -4 receptors, respectively.

INCB3619 is a selective and potent inhibitor of ADAM with antitumour effects, inhibiting ADAM10, ADAM17, MMP12 and MMP15.

P22074 is a USP7 inhibitor. It is not an active antagonist like its halogenated related compounds. p22074 has antitumour activity.

Alethine (β-Alethine) is a small molecule compound with antitumour activity and is used to treat tumours and infections. The alethine-induced up-regulation of TNFα increases the cytotoxicity of T cells.

Vamotinib (PF-114) is an orally active and specific tyrosine kinase inhibitor with antiproliferative and antitumour activity.Vamotinib inhibits the phosphorylation of BCR/ABL and BCR/ABL-T315I, which promotes apoptosis. Vamotinib is used to study drug-resistant Philadelphia chromosome-positive (Ph+) leukaemia and Alzheimer's disease.

GPX-100 (13-deoxydoxorubicin) is an analogue of the anthracycline antitumour antibiotic doxorubicin. GPX-100 inserts into DNA and interacts with topoisomerase II to inhibit DNA replication and repair as well as RNA and protein synthesis.

Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.

Ainsliadimer A, a sesquiterpene lactone dimer from Ainsliaea macrocephala, has antitumour activity and induces cell death in various cancer cells.

(R)-BI-2852 can be used as (R)-5-isoindolin-1-one is used as an inhibitor of the RAS family of proteins and as a compound for the treatment and prevention of tumours. (R)-BI-2852 has Antiproliferative and antitumour agent activity.

CTP Synthetase-IN-1 is an orally active and potent cytidine 5'-triphosphate synthetase (CTPS) inhibitor with potential antitumour activity, shows anti-inflammatory activity in animal models of inflammation, inhibits human CTPS1 and human CTPS2, and can be used in studies of arthritis and rheumatoid arthritis.

OTUB1 USP8-IN-1 HCL is a potent dual inhibitor of OTUB1 and USP8 with potential antitumour activity, inhibiting both OTUB1 and USP8. OTUB1 USP8-IN-1 may be used in the study of leukaemia.

IDH2R140Q-IN-2 is an orally active and potent IDH2R140Q inhibitor with an IC50 of 29 nM.IDH2R140Q-IN-2 possesses potential antitumour activity, reducing D2HG production in TF-1 cell lines carrying the IDH2R140Q mutation (IC50 of 10 nM) and inhibiting tumour tissue D2HG levels.IDH2R140Q-IN-2 is suitable for the study of acute myeloid leukaemia (AML).

4-Methoxycoumarine has antitumour effects.

2-Hydroxyanthraquinone is an anthraquinone that has been found inSpermacoce latifoliaand has antibacterial and estrogenic activities.1,2It is active againstB. subtilisandB. cereus(MICs = 1.9 and 62.5 μg ml, respectively).12-Hydroxyanthraquinone (19 μM) induces estrogen receptor α (ERα) activation in a yeast two-hybrid assay.2 1.Luo, Y., Shen, H.-Y., Shen, Q.-X., et al.A new anthraquinone and a new naphthoquinone from the whole plant of Spermacoce latifoliJ. Asian Nat. Prod. Res.19(9)869-876(2017) 2.Kurihara, R., Shiraishi, F., Tanaka, N., et al.Presence and estrogenicity of anthracene derivatives in coastal Japanese watersEnviron. Toxicol. Chem.24(8)1984-1993(2005)

1. Lutein (Xantofyl) has antitumour action. 2. Lutein has antimutagenic action. 3. Lutein has a wide range of antimicrobial action. 4. Lutein is potentially useful for treating macular degeneration.

(-)-α-Terpineol has antitumour, anti-inflammatory, and antimicrobial activities, it inhibits the growth of tumour cells through a mechanism that involves inhibition of the NF-kappaB pathway

N-Methylformamide is a formamide derivative commonly used as an organic solvent and exhibits antitumour activity in mice.