nci-h460

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2/PLK3 (IC50s: 5/56 nM).

Tubulin inhibitor 8 is an inhibitor of tubulin and various cancer cell lines and inhibits tubulin polymerisation and K562 cell growth with an IC50 of 0.73 μM and 14 nM respectively.

Arcyriaflavin A is derived from Eudistoma sp. It inhibits D1-CDK4, B-CDK1 and CaMKII with IC50 values ​​of 0.14μM, 1.13μM and 0.025μM, respectively. Arcyriaflavin A also inhibits HCT-116 and NCI-H460 cells with IC50 values ​​of 0.85μM and 0.59μM, respectively.

Elinafide, a dinaphthylimide cytotoxic agent, is a DNA-targeted anticancer agent that has shown antitumor activity in in vitro and in vivo assays.

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

Colcemid (NSC-3096) is a microtubule polymerization inhibitor, with the main target being Tubulin and an IC50 of 2.4 μM. Colcemid can induce apoptosis and can be used in the research of tumors and embryo cloning.

Microtubulin-IN-1 (Compound 8g) is an inhibitor of microtubulin, targeting the colchicine-binding site to disrupt tubulin integrity and induce upregulation of p53 protein expression. It exhibits antiproliferative activity across various cancer cell lines, including NCI-H460, BxPC-3, and HT-29, with IC50 values of 2.4, 1.6, and 2.07 nM, respectively. Additionally, Microtubulin-IN-1 induces cell cycle arrest at the G2/M phase and apoptosis in NCI-H460 cells.

Dynamin I inhibitor

Aszonapyrone A is a meroditerpene fungal metabolite that has been found in Neosartorya and has diverse biological activities.1,2,3 It inhibits the growth of MCF-7, NCI H460, and A375-C5 cancer cells (GI50s = 13.6, 11.6, and 10.2 μM, respectively).1 Aszonapyrone A is active against multidrug-resistant isolates of S. aureus, E. faecalis, and E. faecium (MICs = 8, 16, and 16 μg/ml, respectively) and inhibits S. aureus biofilm formation.2 It is also active against P. falciparum in vitro (IC50 = 1.34 μg/ml).3

(S)-α-Methylbenzyl ricinoleamide is a fatty acid amide derived from ricinoleic acid and methyl benzylamine. It demonstrates potent growth inhibition of glioma (U251), breast (MCF-7), ovarian (NCI-ADR/RES and OVCAR-3), kidney (786-0), non-small cell lung (NCI-H460), and prostate (PC-3) cancer cells with a mean GI50 value of 6.9 μM.

Malformin A is a cyclopentapeptide fungal metabolite that has been found in A. niger and has diverse biological activities. It is a plant growth regulator that induces malformations in plant structure. Malformin A inhibits replication of tobacco mosaic virus (TMV) in local lesion and leaf-disc assays (IC50s = 19.7 and 45.4 μg/ml, respectively). It is cytotoxic to NCI-H460, MIA PaCa-2, MCF-7, SF-268, and WI-38 cancer cells (IC50s = 70, 50, 100, 70, and 100 nM, respectively), inhibits proliferation of PC3 and LNCaP cells (IC50s = 130 and 90 nM, respectively), and induces apoptosis and necrosis in PC3 and LNCaP cells. Malformin A also increases the accumulation of reactive oxygen species, decreases the mitochondrial membrane potential, and induces autophagy in PC3 and LNCaP cells. It is toxic to mice when administered intraperitoneally (LD50 = 3.1 mg/kg) but not orally up to doses of 50 mg/kg.

Previridicatumtoxin is a fungal metabolite that has been found inP. aethiopicumand has diverse biological activities.1,2It is an intermediate in the biosynthesis of the mycotoxin viridicatumtoxin . Previridicatumtoxin is active against methicillin-resistantS. aureus(MRSA) and vancomycin-resistantE. faecalis(IC50s = 4.4 and 4.8 μM, respectively), as well asC. albicansandS. cerevisiae(MIC = 32 μg ml for both).2,1It is cytotoxic to NCI H460, KB-3-1, and SW620 cancer cells (IC50s = 5.3, 4.1, and 6 μM, respectively).2 1.Chooi, Y.H., Wang, P., Fang, J., et al.Discovery and characterization of a group of fungal polycyclic polyketide prenyltransferasesJ. Am. Chem. Soc.134(22)9428-9437(2012) 2.Shang, Z., Salim, A.A., Khalil, Z., et al.Viridicatumtoxins: Expanding on a rare tetracycline antibiotic scaffoldJ. Org. Chem.80(24)12501-12508(2015)

Amycolatopsin A is a macrolide polyketide originally isolated fromAmycolatopsisthat has antimycobacterial and anticancer activities.1It is active againstM. bovisandM. tuberculosis(IC50s = 0.4 and 4.4 μM, respectively) but notB. subtilis,S. aureus,E. coli, orP. aeruginosa(IC50s = >30 μM for all). Amycolatopsin A is cytotoxic to SW620 colorectal and NCI H460 lung cancer cells (IC50s = 0.08 and 1.2 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

Amycolatopsin B is a bacterial metabolite originally isolated fromAmycolatopsisthat has anticancer activity.1It is cytotoxic to NCI H460 lung and SW620 colon cancer cells (IC50s = 0.28 and 0.14 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

Amycolatopsin C is a polyketide macrolide originally isolated fromAmycolatopsisthat has antimycobacterial and anticancer activities.1It is active againstM. bovisandM. tuberculosis(IC50s = 2.7 and 5.7 μM, respectively) but notB. subtilis,S. aureus,E. coli, orP. aeruginosa(IC50s = >30 μM for all). Amycolatopsin C is cytotoxic to SW620 colorectal and NCI H460 lung cancer cells (IC50s = 10 and 5.9 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

ATR-IN-4, a potent inhibitor of ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase), restricts the growth of DU145 prostate cancer cells and NCI-H460 lung cancer cells, with IC 50 values of 130.9 nM and 41.33 nM, respectively.

Microtubule inhibitor 5 (compound 17f) is a highly potent cytotoxic agent that inhibits microtubule function, exhibiting a substantial cytotoxic effect on NCI-H460 cells with an IC50 value of 154.5 nM. Additionally, this compound demonstrates excellent cell permeability [1].

Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor exhibiting cytotoxicity against NCI-H460, BxPC-3, and HT-29 cells, with IC50 values of 14.0, 6.6, and 7.0 nM, respectively. It effectively inhibits microtubule polymerization.

Compounds 17o (IC50= 14.0 nM, NCI-H460) and 17p (IC50= 2.9 nM, NCI-H460) with furan moieties show potent nanomolar levels of cytotoxic activity against various human cancer cell lines.

Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor that prevents microtubule protein polymerization and exhibits cytotoxicity in HT-29 cells (IC50: 2.1 nM).

Compounds 17o (IC50: 14.0 nM, NCI-H460) and 17p (IC50: 2.9 nM, NCI-H460) with furan moieties showed potent cytotoxic effects at the nanomolar level against various human cancer cell lines.

Anticancer agent 16 showed good cytotoxic effects on HCT-116 cell line (IC50: 8.55 μM), NCI-H460 cell line (IC50: 5.41 μM) and SKOV3 cell line (IC50: 6.4 μM).

PSB-15160 is a compound that inhibits the growth of MCF7 (breast), NCI-H460 (lung) and SF-268 (NCS) cells in the treatment of estrogen-dependent tumours.

Norartocarpetin is a potent tyrosinase inhibitor exhibiting significant antibrowning properties useful for food system research, with an IC50 of 0.47 μM. Furthermore, it demonstrates substantial anticancer activity specifically in lung carcinoma cells (NCI-H460), achieving an IC50 of 22 μM. The antiproliferative effects of Norartocarpetin are achieved through targeting the Ras Raf MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, facilitating S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells.