T62448
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Microtubule inhibitor 6 (compound 17o) 是一种有效的微管抑制剂。Microtubule inhibitor 6 对 NCI-H460 细胞、BxPC-3 细胞、HT-29 细胞表现出细胞毒性,他们的 IC50 值分别为 14.0、6.6、7.0 nM。Microtubule inhibitor 6 能够有效抑制微管聚合。 |
T79451
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Carbonic Anhydrase
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WES-1(Compound 8g)是一种针对碳酸酐酶IX的抑制剂,其抑制常数(Ki)为55.9 μM。该化合物对包括白血病细胞系(K-562、MOLT-4)、非小细胞肺癌(NCI-H460)、结肠癌(HCT 116、HCT-15)以及黑色素瘤(LOX IMVI)在内的多种癌细胞表现出抗增殖效果。 |
T78780
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Anticanceragent 139(Compound 6h)展现了针对多种癌细胞株的抗癌效能。该化合物能够与Tubulin的Lys352残基发生π-阳离子相互作用。在对SNB-19、OVCAR-8和NCI-H460细胞株的测试中,Anticanceragent 139展现出较高的生长抑制率(PGI),数值分别为86.61、85.26和75.99。同时,该化合物对于HOP-62、SNB-75、ACHN、NCI/ADR-RES、786-O、A549/ATCC、HCT-116以及MDA-MB-231细胞株亦表现出中等的生长抑制作用,其PGI值分别为67.55、65.46、59.09、59.02、57.88、56.88、56.53和56.4、51.88。 |
T70856
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3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg/ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg/ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg/ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50 = 13.4 µM). It is also active against L. donovani amastigotes when used at a concentration of 50 µM. |
TN5930
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Ocotillone has potent antibacterial activity against Gram-negative bacteria, P. aeruginosa and S. typhimurium, that are without hemolytic activity, whereas it has weak antimicrobial activity against Gram-positive bacteria and fungi. Ocotillone shows only |
T35675
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SW203668 is an irreversible inhibitor of stearoyl-CoA desaturase (IC50 = 54 nM). It is selectively cytotoxic to H2122, H460, HCC44, and HCC95 cell lines that express cytochrome P450 (CYP) isoform CYP4F11 over eight other cancer cell lines that lack CYP4F11 in vitro (IC50s = 22-116 and >10,000 nM, respectively) and ectopic expression of CYP4F11 in SW203668-insensitive H1155 cells results in sensitization to SW203668. In vivo, SW203668 reduces tumor growth rate without reducing sebocyte production in the H2122 wild-type and nonobese diabetic severe combined immunodeficiency (NOD-SCID) mouse xenograft models when administered at doses of 20 and 6 mg/kg, respectively. |
T81201
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Sartorypyrone B为Chevalone C的2β-乙酰氧基衍生物,由海绵源真菌Neosartorya tsunodae(KUFC 9213)的培养物中乙酸乙酯提取得到。该化合物对MCF-7、NCI-H460和A375-C5细胞系展示出较强的生长抑制活性,GI50s值分别为17.8、20.5和25.0 μM,显示其在乳腺癌、非小细胞肺癌和黑色素瘤研究中的应用潜力。 |
T35754
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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 |
T37006
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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) |
T36489
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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. |