nci-h460

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.

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 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

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.

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

Colcemid (NSC-3096) is a microtubule polymerization inhibitor that primarily targets tubulin, with an IC₅₀ of 2.4 μM. Demecolcine interacts with tubulin dimers, induces antimitotic effects, and inhibits microtubule growth. Colcemid is a classic reagent used in karyotyping, banding techniques, and cell cycle synchronization. Colcemid can induce apoptosis and is used in studies of tumor and embryonic cloning.

Dynamin I inhibitor

GEM144 is a dual inhibitor of DNA polymerase α (POLA1) and HDAC 11. GEM144 induces p53 acetylation, activates p21, arrests the cell cycle in the G1/S phase, and induces apoptosis.

Norartocarpetin is a tyrosinase inhibitor with strong inhibitory activity against tyrosinase (IC₅₀ = 0.47 μM). It can be used as an anti-browning agent in food-related research and also shows significant anti-tumor activity against human lung cancer NCI-H460 cells with an IC₅₀ of 22 μM. Its anti-proliferative mechanisms mainly include regulating the Ras/Raf/MAPK signaling pathway, inducing mitochondria-dependent apoptosis, arresting the cell cycle at S phase, and inhibiting cell migration and invasion.

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.

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.

A-259745 is an orally active antimitotic agent that binds to the colchicine site on tubulin. It exhibits potent in vitro cytotoxic activity against both multidrug-resistant and non-multidrug-resistant cancer cell lines, with ED50 values of 0.018 μM for HCT-15 and 0.028 μM for NCI-H460 cells. A-259745 inhibits tubulin polymerization, disrupting the dynamic equilibrium of the mitotic spindle, causing dividing cells to arrest in the metaphase-anaphase transition, which subsequently induces apoptosis (apoptosis). In mouse tumor models, A-259745 demonstrates dose-dependent antitumor efficacy and is useful for cancer research.

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).